Language：English   Publisher：Biochemical and Biophysical Research Communications  

Hericenone C is one of the most abundant secondary metabolites derived from Hericium erinaceus, under investigation for medicinal properties. Here, we report that Hericenone C inhibits the second phase of formalin-induced nociceptive behavior in mice. As the second phase is involved in inflammation, in a mechanistic analysis on cultured cells targeting NF-κB response element (NRE): luciferase (Luc)-expressing cells, lipopolysaccharide (LPS)-induced NRE::Luc luciferase activity was found to be significantly inhibited by Hericenone C. Phosphorylation of p65, which is involved in the inflammatory responses of the NF-κB signaling pathway, was also induced by LPS and significantly reduced by Hericenone C. Additionally, in mice, the number of CD11c-positive cells increased in the paw during the peak of the second phase of the formalin test, which decreased upon Hericenone C intake. Our findings confirm the possibility of Hericenone C as a novel therapeutic target for pain-associated inflammation.

DOI： 10.1016/j.bbrc.2024.150077

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Publisher：Cytotechnology  

Sea cucumbers are both versatile marine organisms and an Asian marine food known to have several medicinal effects. We evaluated the anti-allergic potential of some major purified holostane-type saponins from the body wall of the black sea cucumber, Holothuria atra. Six saponin compounds were isolated, holothurin B (1), holothurin A (2), 24-dehydro echinoside A (3), desholothurin A1 (4), desholothurin A (5), and des 24-dehydro echinoside A (6). The structures were identified based on spectroscopic methods and by comparison with the literature. Each compound’s inhibitory activity toward the release of β-hexosaminidase was evaluated. Among the six compounds, holothurin B (1) showed the strongest inhibition of the degranulation at all tested concentrations in a dose-dependent manner, compared to the positive control, quercetin. We also observed that holothurin B (1) was able to alleviate the inflammatory mediators interleukin (IL)-6, IL-13, and tumor necrosis factor-alpha (TNF-α). Holothurin B (1) also inhibited the Ca2+ influx stimulated by the calcium ionophore A23187, by suppressing the expression of inositol-1,4,5-triphosphate receptor (IP3R) mRNA. These results suggest that (i) holothurin B (1) has good anti-allergy activity without cytotoxicity at effective concentrations, and (ii) this compound could be a lead compound for the treatment of allergic diseases and associated inflammation. We also performed a molecular docking study for the tested compounds to correlate their binding modes and affinity for the IP3R with the in vitro results. The results concluded that the holostane-type saponins could be used as anti-allergy agents, which may be attributed to their holostane group.

DOI： 10.1007/s10616-024-00649-8

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Language：English   Publisher：Journal of Agricultural and Food Chemistry  

Flammulina velutipes (enokitake) is widely recognized for its nutritional and medicinal properties. Understanding the biochemical processes, such as lipid metabolism during fruiting body formation, is essential for enhancing mushroom cultivation and utilization. This study aimed at elucidating the dynamic lipidomic changes during seven growth stages of F. velutipes using ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry. Our results revealed significant increases in ceramides along with the growth and a sharp decline in phosphatidylinositols from mycelial to primordial stages. Fatty acid esters of hydroxy fatty acids, recently discovered for their bioactivities, showed high intensities in the mycelial and primordial stages but decreased rapidly thereafter. These findings provide profound insights into the lipid profiles associated with mushroom morphology and development. This lipidomics study establishes a foundational understanding for future research in agricultural and food chemistry applications, potentially improving industrial production and quality control of F. velutipes.

DOI： 10.1021/acs.jafc.4c03863

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Language：English  

Language：English   Publisher：Metabolomics  

Introduction: Microbial communities affect several aspects of the earth’s ecosystem through their metabolic interaction. The dynamics of this interaction emerge from complex multilevel networks of crosstalk. Elucidation of this interaction could help us to maintain the balance for a sustainable future. Objectives: To investigate the chemical language among highly abundant microbial genera in the rhizospheres of medicinal plants based on the metabolomic analysis at the interaction level. Methods: Coculturing experiments involving three microbial species: Aspergillus (A), Trichoderma (T), and Bacillus (B), representing fungi (A, T) and bacteria (B), respectively. These experiments encompassed various interaction levels, including dual cultures (AB, AT, TB) and triple cultures (ATB). Metabolic profiling by LC-QTOFMS revealed the effect of interaction level on the productivity and diversity of microbial specialized metabolites. Results: The ATB interaction had the richest profile, while the bacterial profile in the monoculture condition had the lowest. Two native compounds of the Aspergillus genus, aspergillic acid and the dipeptide asperopiperazine B, exhibited decreased levels in the presence of the AT interaction and were undetectable in the presence of bacteria during the interaction. Trichodermarin N and Trichodermatide D isolated from Trichoderma species exclusively detected during coexistence with bacteria (TB and ATB). These findings indicate that the presence of Bacillus activates cryptic biosynthetic gene clusters in Trichoderma. The antibacterial activity of mixed culture extracts was stronger than that of the monoculture extracts. The TB extract exhibited strong antifungal activity compared to the monoculture extract and other mixed culture treatments. Conclusion: The elucidation of medicinal plant microbiome interaction chemistry and its effect on the environment will also be of great interest in the context of medicinal plant health Additionally, it sheds light on the content of bioactive constituents, and facilitating the discovery of novel antimicrobials.

DOI： 10.1007/s11306-024-02138-7

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Language：English   Publisher：Inflammopharmacology  

Parkinsonism is an age-related neurodegenerative illness that affects motor coordination leading to loss of dopaminergic neurons. Many medications are used for the treatment of Parkinson’s disease but are only symptomatic and have a limited effect on the progression of this ailment. Therefore, bioactive compounds which derived from plants have been examined for their ability to improve the neuronal damage and cell death happened in parkinsonian patients. In this study the iridoids-rich fraction isolated from Pentas lanceolata (PIRF) leaves was investigated for its phytoconstituents. Seven iridoids (1–7) and one flavonol diglycoside (8) were isolated, and their chemical structures were achieved by 1H and 13C nuclear magnetic resonance and ESI–MS spectral data. Compound 1 (6β,7β-epoxy-8-epi-splendoside) and 5 (gaertneroside) were isolated for the first time from Pentas genus as well as compound 8 (kaempferol-3-O-robinobioside). The current study aims to investigate the possible anti-parkinsonian effect of PIRF using a rotenone model of Parkinsonism in mice. Behavioural tests (wirehanging, stair and wooden-walking tests) were done to examine the motor coordination in mice after treatment. Biochemical and histopathological examinations for brain striatum in different groups were also evaluated. Results revealed that rotenone-treated mice had poor motor functions described by depletion of dopamine and Ach levels, a significant increase in proinflammatory cytokines, IL-1B, TNF-α and Mcp-1 and oxidative biomarkers with subsequent reduction in antioxidant mediators. Disorganization of striatum, degenerated neurocytes, slight vacuolation, shrunken neurons with pyknotic nuclei and apoptotic cells are displayed by histopathological examinations. Treatment with PIRF ameliorates the neurodegeneration-induced by rotenone in the brain of mice. The anti-parkinsonian effect of PIRF could be attributed to their bioactive constituents of iridoids.

DOI： 10.1007/s10787-024-01509-9

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Language：English   Publisher：Phytomedicine  

Background: Pulmonary Fibrosis (PF) is a progressive lung disease characterized by the diffuse interstitial tissue, leading to severe breathing difficulties. The existing treatment methods are primarily aimed at slowing the progression of the disease, underscoring the urgent need to discover new drug interventions targeting novel sites. The "gut-lung axis" represents a complex bidirectional communication system where the gut microbiota not only influences lung immunity but also responds to lung-derived signals. Recent advances have uncovered that alterations in gut microbiota composition can significantly impact respiratory diseases, offering new insights into their pathogenesis and potential therapeutic approaches. Methods: This study is based on the fundamental concepts of the lung-gut axis and our previous research, further exploring the potential mechanisms of 20(S)-Protopanaxadiol (PPD) in ginseng against PF. We utilized a bleomycin-induced mouse model of PF and employed metabolomics and 16S rRNA sequencing to investigate the pathways through which PPD regulates the pulmonary fibrosis process via the gut-lung axis. Finally, we employed strategies such as antibiotic-induced microbiota disruption and fecal microbiota transplantation (FMT) to provide a comprehensive perspective on how PPD regulates pulmonary fibrosis through gut microbiota. Results: The results of the bleomycin (BLM) mouse model of PF proved that PPD can directly act on the glycolysis- related metabolic reprogramming process in lung and the AMPK/STING pathway to improve PF. Combined the analysis of gut microbiota and related metabolites, we found that PPD can regulate the process of PF through the gut-lung axis target points G6PD and SPHK1. FMT and antibiotic-induced microbiota disruption further confirmed intermediate effect of gut microbiota in PF process and the treatment of PPD. Our study suggests that PPD can alleviate the process of pulmonary fibrosis either by directly acting on the lungs or by regulating the gut microbiota. Conclusion: This study positions PPD as a vanguard in the therapeutic landscape for pulmonary fibrosis, offering a dual mechanism of action that encompasses both modulation of gut microbiota and direct intervention at molecular targets. These insights highlight the immense therapeutic potential of harnessing the gut-lung axis.

DOI： 10.1016/j.phymed.2024.155699

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Publisher：Records of Natural Products  

Four new polyoxygenated cucurbitane triterpene glycosides named kedrojiftene A-D (4-7), were isolated via different chromatographic techniques along with three phenolic compounds (1-3) from the crude extract of Kedrostis gijef. The isolated compounds were elucidated based on 1D, 2D-NMR spectroscopic analyses, HRESIMS and comparison with the related metabolites in literature. In bioassay, the α-glucosidase inhibitory assay for the isolated compounds was carried out and compounds (1-3) showed significant inhibitory activities.

DOI： 10.25135/rnp.468.2405.3236

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Language：English   Publisher：Natural Product Research  

Two new cucurbitane-type triterpenoids (2,3), together with two known compounds (1,4), were isolated from the aerial parts of Kedrostis gijef. The structure of all compounds was elucidated based on NMR, HRESIMS analyses, and by comparison with the literature. Additionally, the cytotoxic activity against HeLa, Caco-2, and SH-SY5Y cell lines was determined using MTT colorimetric assay.

DOI： 10.1080/14786419.2024.2367236

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Language：English   Publisher：Phytomedicine  

Background: Pulmonary fibrosis (PF) is an escalating global health issue, characterized by rising rates of morbidity and mortality annually. Consequently, further investigation of potential damage mechanisms and potential preventive strategies for PF are warranted. Specnuezhenide (SPN), a prominent secoiridoid compound derived from Ligustrum lucidum Ait, exhibits anti-inflammatory and anti-oxidative capacities, indicating the potential therapeutic actions on PF. However, the underlying mechanisms of SPN on PF remain unclear. Purpose: This work was aimed at investigating the protective actions of SPN on PF and the potential mechanism. Methods: In vivo, mice were administrated with bleomycin (BLM) to establish PF model. PF mice were treated with SPN (45/90 mg/kg) by gavage. In vitro, we employed TGF-β1 (10 ng/mL)-induced MLE-12 and PLFs cells, which then were treated with SPN (5, 10, 20 µM). DARTS assay, biofilm interference experiment and molecular docking were performed to investigate the molecular target of SPN. Results: In vivo, we found SPN treatment improved survival rate, alleviated pathological changes through reducing BLM-induced extracellular matrix (ECM) deposition, as well as BLM-induced epithelial-mesenchymal transition (EMT). In vitro, SPN inhibited EMT and lung fibroblast transdifferentiation. Mechanistically, SPN activated the AMPK protein to decrease the abnormally high level of PD-L1. Furthermore, the compound C, known as an AMPK inhibitor, exhibited a significant hindrance to the inhibition of SPN on TGF-β1-caused fibroblast transdifferentiation and proliferation. This outcome could be attributed to the fact that compound C could eliminate the inhibitory effects of SPN on PD-L1 expression. Interestingly, DARTS assay, biofilm interference experiment and molecular docking results all indicated that SPN could bind to AMPK, which suggested that SPN might be a potential agonist targeting AMPK protein. Conclusion: Altogether, the results in our work illustrated that SPN promoted AMPK-dependent reduction of PD-L1 protein, contributing to the inhibition of fibrosis progression. Thus, SPN may represent a potential AMPK agonist for PF treatment.

DOI： 10.1016/j.phymed.2023.155318

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Publisher：Phytochemistry Letters  

Megastigmanes are structurally-diverse molecules that are widely distributed in nature and occurring mainly in plant kingdom. They are oxidative degradation products from β-carotenoids with C13 skeleton and their diversity has been attributed to different functionalization at the carbon atoms, as well as glycosylation pattern. The object of this review is to summarize the published literature on megastigmane glycosides regarding their sources, 13C NMR data and biological activities. This review covers the literature published between the first report that appeared in 1968 till May 2022. It combines about 357 megastigmane glycosides with their classification, sources, biological activities, and 13C NMR data. The biological activities of megastigmane glycosides have been reported, including anti-melanogenic, anti-inflammatory, neuroprotective, antioxidant, antitumor, antimicrobial, and hepatoprotective. Anti-melanogenic and hepatoprotective activities are the most promising reported bioactivities. Besides, biosynthetic pathways as well as chemotaxonomic significance are also discussed. The present review is expected to provide a comprehensive guide on this particular class of natural products.

DOI： 10.1016/j.phytol.2024.01.008

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Publisher：Food Bioscience  

This study investigated the inhibitory effects and mechanisms of strawberry fruit extracts (SFE) and leaf extracts (SLE) on advanced glycation end products (AGEs) formation. The results revealed that SLE exhibited a higher inhibitory efficiency compared to SFE on AGEs formation in bovine serum albumin (BSA)-fructose, -methylglyoxal (MGO) and -glyoxal (GO) models. Additionally, SLE displayed remarkable trapping capabilities of MGO and GO, surpassing those of SFE. Both SFE and SLE were found to combine with BSA for static quenching, SLE showed a stronger binding force. Moreover, SLE outperformed SFE in terms of protecting the secondary structure of proteins and preventing protein cross-linking. Finally, the high-resolution mass spectrometry analysis revealed that SLE could reduce glycation sites and significantly improve the degree of glycation. Our study suggests that SLE may serve as a superior inhibitor of glycation compared to SFE, thereby providing new insights into its potential applications.

DOI： 10.1016/j.fbio.2024.103691

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Language：English   Publisher：Food Chemistry: X  

Numerous health hazards have been connected to advanced glycation end products (AGEs). In this investigation, using reaction models including BSA-fructose, BSA- methylglyoxal (MGO), and BSA-glyoxal (GO), we examined the anti-glycation potential of eight different berry species on AGEs formation. Our results indicate that black chokeberry (Aronia melanocarpa) exhibited the highest inhibitory effects, with IC50 values of 0.35 ± 0.02, 0.45 ± 0.03, and 0.48 ± 0.11 mg/mL, respectively. Furthermore, our findings suggest that black chokeberry inhibits AGE formation by binding to BSA, which alleviates the conformation alteration, prevents protein cross-linking, and traps reactive α-dicarbonyls to form adducts. Notably, three major polyphenols, including cyanidin-3-O-galactoside, cyanidin-3-O-arabinoside, and procyanidin B2 from black chokeberry, showed remarkably inhibitory effect on MGO/GO capture, and new adducts formation was verified through LC-MS/MS analysis. In summary, our research provides a theoretical basis for the use of berries, particularly black chokeberry, as natural functional food components with potential anti-glycation effects.

DOI： 10.1016/j.fochx.2023.101032

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Language：English   Publisher：Fitoterapia  

The eelgrass Zostera marina L. has several economic roles, from its earlier usage in the insulation industry to protecting the earth from global warming. In this study, we aimed to discover the cosmetic potential of Z. marina. A methanolic extract of Z. marina showed anti-phototoxicity and anti-melanogenesis activity with an IC50 of 17.5 μM, followed by a phytochemical analysis of its phenolic constituents. Ten compounds (1−10) were isolated by several chromatographic techniques and identified by means of nuclear magnetic resonance spectroscopy (NMR) as well as high-resolution mass spectrometry (HR/MS). The identified compounds are caffeic acid (1), 3,4-dihydroxybenzoic acid (protocatechuic acid) (2), luteolin (3), diosmetin (4), 4-coumaroyl-4′-hydroxyl phenyllactic acid (5), rosmarinic acid (6), caffeoyl-4′-hydroxy-phenyllactic acid (isorinic acid) (7), apigenin 7-O-β-D-glucopyranoside (8), luteolin 7-O-β-D-glucopyranoside (9), and luteolin 7-sulfate (10). This is the first report to identify compounds 5 and 7 from the family Zosteraceae. The isolated compounds were assessed for their anti-aging abilities and were found to exhibit good anti-phototoxicity and anti-melanogenesis activities by increasing the viability of UVB-irradiated HaCaT cells by 6% to 34% and by inhibiting melanin synthesis in B16 melanoma cells by 44% to 65%.

DOI： 10.1016/j.fitote.2023.105817

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Language：English   Publisher：Molecules  

DOI： 10.3390/molecules29051008

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Language：English   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publisher：(株)医事出版社  

ブタプラセンタエキス100mgを含有するサプリメント(2錠/1日)の4週間摂取が心理的ストレス症状に与える効果を検証するため、35歳以上60歳未満の女性40名を対象に無作為化二重盲検並行群間比較試験を行った。心理的ストレス反応測定尺度(SRS-18)において、プラセンタサプリメント摂取群では特に「不機嫌・怒り」の反応に多くの改善効果が認められたが、「抑うつ・不安」「無気力」の反応には明確な改善効果は示されなかった。今回、より幅広い年齢層および多様な心理ストレス症状を有する対象者にブタプラセンタエキスの摂取効果が示され、プラセンタエキス摂取群で示された「ストレス場面における心理ストレス反応」の軽減結果は、脳由来神経栄養因子産生促進効果やコルチゾール調整機能が関与した可能性が示された。

Publisher：Food Science and Human Wellness  

In the face of increasingly serious environmental pollution, the health of human lung tissues is also facing serious threats. Mogroside IIE (M2E) is the main metabolite of sweetening agents mogrosides from the anti-tussive Chinese herbal Siraitia grosvenori. The study elucidated the anti-inflammatory action and molecular mechanism of M2E against acute lung injury (ALI). A lipopolysaccharide (LPS)-induced ALI model was established in mice and MH-S cells were employed to explore the protective mechanism of M2E through the western blotting, co-immunoprecipitation, and quantitative real time-PCR analysis. The results indicated that M2E alleviated LPS-induced lung injury through restraining the activation of secreted phospholipase A2 type IIA (Pla2g2a)-epidermal growth factor receptor (EGFR). The interaction of Pla2g2a and EGFR was identified by co-immunoprecipitation. In addition, M2E protected ALI induced with LPS against inflammatory and damage which were significantly dependent upon the downregulation of AKT and mTOR via the inhibition of Pla2g2a-EGFR. Pla2g2a may represent a potential target for M2E in the improvement of LPS-induced lung injury which may represent a promising strategy to treat ALI.

DOI： 10.26599/FSHW.2022.9250025

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Publisher：Functional Foods in Health and Disease  

Background: Sorghum is consumed in Africa, North and South America, India, and other parts of the world, but it is one of several millets in Japan, and its physiological function for Japanese is not well known. In this study, we examined the effect of sorghum on postprandial blood glucose levels in healthy Japanese. Objective: This study aims to investigate the effect of sorghum intake on postprandial blood glucose in healthy adults. Methods: A double-blind crossover study was done on 17 healthy adult men and women recruited from the general population. After an early morning fasting blood glucose test, a placebo or sorghum porridge was administered and blood glucose levels were measured at 30, 60, and 120 minutes after the first washout period. Result: At 60 and 120 minutes after intake, the blood glucose level of people who were administered sorghum porridge was significantly lower than that of those who were administered the placebo. The area under the blood glucose curve was also significantly lower for the test product than for the placebo. Conclusion: Sorghum consumption can suppress the increase in postprandial blood glucose, suggesting that sorghum is useful in preventing the development of diabetes mellitus.

DOI： 10.31989/ffhd.v14i1.1266

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Language：English   Publisher：Toxicon  

Three prenylated flavonoids (1–3) were isolated from Tetragonula biroi propolis. The structures of the isolated compounds were characterized by NMR, IR, and UV spectroscopic and mass spectrometric analyses. The cytotoxicity activity of the crude extracts, fractions and the isolated compounds were established against four cell lines such as Caco-2, HeLa, MCF-7, and OVK-18. Among the tested compounds, compound 1 showed cytotoxicity activity against MCF-7 cell lines, whereas compound 2 showed good activity against Caco-2 and OVK-18 cell lines with IC50 values of 14.73 and 14.44, respectively. Moreover, compound 3 exhibited strong activity against OVK-18 cell lines. These findings contribute to the phytochemical understanding of the T. biroi propolis, and their cytotoxicity effects for future pharmaceutical purposes.

DOI： 10.1016/j.toxicon.2023.107352

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Language：English   Publisher：Animal Science Journal  

The purpose of this study was to investigate the time-dependent change in Reishi (Ganoderma lingzhi) triterpenoids in rumen fluid. G. lingzhi fruiting bodies were milled and incubated in a tube with rumen fluid for 0, 4, 8, 12, 24, and 48 h at 39°C. After incubation, all the tubes were freeze-dried and extracted by ethanol. The contents of 18 triterpenoids in the ethanol extract were quantitated by liquid chromatography-mass spectrometry (LC-MS/MS). Based on the results, triterpenoids were categorized into three groups: (1) rapid decrease, indicating reductions of more than 50% within 8 h; (2) mild decrease, with reductions of more than 50% within 48 h; and (3) minimal change, even after 48 h, there was not much change. Ganoderic acid C6, DM, H, K, and TR as well as Ganoderenic acid D were classified in (1); Ganoderic acid LM2 and T-Q as well as Ganoderiol F in (2); and Ganoderic acid A, B, C1, C2, I, and TN; Gnoderenic acid C; and Ganodermanontriol in (3). In addition, a relationship between chemical structure and metabolic speed was observed in some cases. The results of this study revealed that G. lingzhi triterpenoids are digested and metabolized at different speeds in ruminant fluid.

DOI： 10.1111/asj.13957

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：SPRINGER JAPAN KK  

Odor environments in living spaces can influence human physiological and psychological states. To elucidate the effect of volatile organic compounds (VOCs) of wood in living spaces on the modulations of cognitive processing, we built two experimental huts to simulate wooden construction living spaces. One hut was made of cedarwood (Cryptomeria japonica), and the other was made of resin. We used cedarwood and resin, because they are often used as construction materials in Japan. In both huts, we measured the participants' first positivity in the early visual cortex (P1), the third positivity elicited by voluntary attention (P3b), and the automatic occipital negativity to infrequent visual stimuli in event-related potentials (ERPs), while they performed a visual discrimination task. The VOCs in both huts were measured by gas chromatography-mass spectrometry. The concentration of volatile sesquiterpenes was significantly increased in the cedarwood hut. Neither P1 nor P3b was affected by the cedarwood hut. Compared to the resin hut, we observed significantly larger occipital negativities to the infrequent stimuli in the cedarwood hut in the time windows of 280-300 ms at the mid-occipital region. These findings suggest that the increased concentration of volatile sesquiterpenes emitted from cedarwood facilitates the human brain's response to changes in visual stimuli.

DOI： 10.1186/s10086-023-02083-4

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Language：English   Publisher：Journal of Chromatography A  

An eco-friendly dispersive liquid-liquid microextraction mediated with a reverse micelle and coupled to an HPLC-DAD was developed for the simultaneous determination of venlafaxine and agomelatine in dosage forms and human plasma. All the parameters affecting the extraction efficiencies of both drugs were investigated and optimized. Under the optimal conditions, an effective analytes’ preconcentration with enrichment factors (EFs) up to 72 was achieved. The linearity of the method was established over the concentration range of 0.50−70.0 and 3.0−100.0 ng/mL for venlafaxine and agomelatine, respectively with good correlation coefficients > 0.998. The method exhibited low detection limits in the range of 0.15-0.89 ng/mL and excellent precisions expressed in %RSD < 3% with average recoveries between 95.0 to 101.0%. The proposed method was employed to analyze the targeted analytes in dosage forms and human plasma samples with favorable characteristics like excellent enrichment, high sensitivity, great accuracy, and high precision. Finally, the greenness of the developed method was assessed using three distinct metric tools, confirming the greenness of the proposed method. The findings of this research could have more general implications for the extraction of other analytes from various matrices.

DOI： 10.1016/j.chroma.2023.464441

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Language：English   Publisher：Scientific Reports  

Loquat (Eriobotrya japonica) leaves contain many bioactive components such as ursolic acid (UA) and amygdalin. We investigated the effects of loquat leaf powder and methanol extract in human neuroglioma H4 cells stably expressing the Swedish-type APP695 (APPNL-H4 cells) and C57BL/6 J mice. Surprisingly, the extract greatly enhanced cellular amyloid-beta peptide (Aβ) 42 productions in APPNL-H4 cells. Administration of leaf powder increased Aβ42 levels after 3 months and decreased levels after 12 months compared to control mice. Leaf powder had no effect on working memory after 3 months, but improved working memory after 12 months. Administration of UA decreased Aβ42 and P-tau levels and improved working memory after 12 months, similar to the administration of leave powder for 12 months. Amygdalin enhanced cellular Aβ42 production in APPNL-H4 cells, which was the same as the extract. Three-month administration of amygdalin increased Aβ42 levels slightly but did not significantly increase them, which is similar to the trend observed with the administration of leaf powder for 3 months. UA was likely the main compound contained in loquat leaves responsible for the decrease in intracerebral Aβ42 and P-tau levels. Also, amygdalin might be one of the compounds responsible for the transiently increased intracerebral Aβ42 levels.

DOI： 10.1038/s41598-023-44098-3

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Life Sciences  

Aims: Idiopathic pulmonary fibrosis (IPF) is a severe pulmonary interstitial pneumonia. Our study focuses on the role of PLA2 enzyme in the IPF to explore a more effective diagnosis and treatment mechanism of IPF. Main methods: Transcriptome data of IPF from GEO database and bleomycin-induced pulmonary fibrosis mice were analyzed to identify PLA2 enzyme and their metabolite, lysophosphatidylcholines 18:0, in IPF. Based on PLA2G2A and PLA2G2D / PLA2G2A-associated cell death genes (PCDs), the consensus clustering analysis was used to identify the subtypes of IPF and the correlation between PLA2G2A and prognosis was analyzed. The machine learning (ML) models and artificial neural network (ANN) model was used to validate the diagnostic accuracy of PLA2s and PCDs in diagnosing IPF. The gene and protein expression of NLRP3, GSDMD, and CASP-1 was estimated in recombinant PLA2G2A protein induced MLE-12 cells. Key findings: The expression of PLA2G2D, PLA2G2A, and LPC18 significantly changed in IPF. Furtherly, PLA2G2A has a significant correlation with poor patient prognosis, which could predict the 2 or 3-years mortality rates of IPF. Two subtypes of IPF patients, identified based on PCDs, showed significant different immunoinfiltration. Recombinant PLA2G2A protein could induce the pyrotosis in the MLE-12 cell. The generalized linear model and ANN model of PLA2s or PCDs accurate diagnosis IPF. Significance: PLA2G2A is the most robustly associated gene with IPF among the PLA2s, which demonstrates a potential in diagnosing and prognostic value in IPF, and provides a foundation for further understanding and breakthroughs in IPF diagnosis and treatment.

DOI： 10.1016/j.lfs.2023.122071

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Language：English   Publisher：Planta Medica  

A large variety of natural plants are widely produced and utilised because of their remarkable pharmacological effects. In this study, two phenolic glycosides were isolated for the first time from Vanilla pompona Schiede (Orchidaceae) from Kyushu, Japan: bis [4-(β -D - O-glucopyranosyloxy)-benzyl] (S)-2-isopropylmalate (1) and bis 4-[ β -D- O -glucopyranosyloxy)-benzyl]-(2 R,3 S)-2-isopropyl tartrate (2). We have discovered that the crude extract of V. pompona leaves and stems and its two phenolic glycosides (compounds 1  -  2) are highly effective in reversing skin senescence. V. pompona and compounds 1  -  2 were found to promote the synthesis of collagen, hyaluronic acid, and elastin in skin fibroblasts in a normal skin cell model; in a replicative senescence model, V. pompona and compounds 1  -  2 significantly reduced the ageing phenotype in skin fibroblasts. These compounds also demonstrated a significant protective effect in a UV-induced photo-senescence model; the possible mechanisms of this effect were investigated in this study. To the best of our knowledge, this study is the first to develop V. pompona leaves and stems as new sources of bioactive compounds and to examine their therapeutic potential for skin senescence. The development potential of V. pompona leaves and stems for use in the cosmetics, cosmeceutical, and pharmaceutical industries remains to be investigated.

DOI： 10.1055/a-2117-9233

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：ACS Omega  

Sixteen chemically varied metabolites were isolated from the bulbs of Hippeastrum vittatum (L’Her.) Herb., including eight flavonoids [3′-methyl isoliquiritigenin (2), 7-hydroxyflavan (8), 7-hydroxyflavanone (9), 7-hydroxyflavan-3-ol (10), 7-methoxy-3′,4′-methylenedioxyflavan-3-ol (11), 7-hydroxy-3′,4′-methylenedioxy flavan (12), 2′,4′-dihydroxy-3′-methyl-3,4-methylenedioxychalcone (13), and isoliquiritigenin (14)], four acetophenones [2,6-dimethoxy-4-hydroxyacetophenone (3), 2,4-dihydroxyacetophenone (4), 2,4-dihydroxy-6-methoxy-3-methylacetophenone (6), and 2,4,6-trimethoxyacetophenone (7)], two alkaloids [lycorine (1) and narciprimine (15)], one phenol derivative [p-nitrophenol (5)], and one steroid [β-sitosterol 3-O-β-glucopyranoside (16)]. Their structures were elucidated by combining one- and two-dimensional NMR and ESI-MS techniques and by comparison with the reported literature data and some authentic samples. Except for lycorine (1), the isolated metabolites were obtained herein for the first time from Hippeastrum plants, among which compound 13 was identified as a new chalcone derivative. Additionally, the total phenolic and flavonoid contents of the total ethanol extract and different fractions of the bulbs were determined by the Folin-Ciocalteu and aluminum chloride colorimetric methods, respectively, whereas their antioxidant potential was compared using the phosphomolybdenum and 2,2′-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assays. Finally, the binding affinities of compounds 1-16 to some key target proteins of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), namely, main protease (Mpro), papain-like protease (PLpro), and RNA-dependent RNA polymerase (RdRp), were screened and compared using molecular docking analysis. The possible chemotaxonomic significance of the identified metabolites was also discussed.

DOI： 10.1021/acsomega.2c07886

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Language：Japanese   Publisher：(株)インフォノーツパブリッシング  

Language：English   Publishing type：Research paper (scientific journal)   Publisher：RSC Advances  

Oil spills that contaminate the environment can harm the surrounding ecosystem. The oil contains petroleum hydrocarbon which is toxic to the environment hence it needs to be removed. The use of bacteria as remediation media was modified by immobilizing into a matrix hence the bacteria can survive in harsh conditions. In this research, the ability of biosurfactant-producing bacteria (Pseudomonas aeruginosa, Bacillus subtilis, and Ralstonia pickettii) immobilized in the PVA/SA/bentonite matrix was tested in remediation on oil-contaminated soil. The immobilized beads filled with bacteria were added to the original soil sample, as well as washed soil. The beads were characterized by using FTIR and SEM. Based on FTIR analysis, the PVA/SA/bentonite@bacteria beads had similar functional groups compared to each other. SEM analysis showed that the beads had non-smooth structure, while the bacteria were spread outside and agglomerated. Furthermore, GC-MS analysis results showed that immobilized B. subtilis and R. pickettii completely degraded tetratriacontane and heneicosane, respectively. Meanwhile, after soil washing pre-treatment, immobilized bacteria could completely degrade octadecane (P. aeruginosa and R. pickettii) and tetratriacontane (P. aeruginosa and B. subtilis). Based on those results, immobilized bacteria could degrade oil compounds. The degradation result was influenced by the enzymes produced, the ability of the bacteria, the suitability of the test media, and the matrix used. Therefore, this study can be a reference for further soil remediation using eco-friendly methods.

DOI： 10.1039/d3ra02249h

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Molecules  

Hericium erinaceus, a mushroom species commonly known as Yamabushitake in Japan, is known to have a stimulatory effect on neurotrophic factors, such as brain-derived neurotrophic factor (BDNF) and nerve growth factor (NGF). Hericenone C, a meroterpenoid with palmitic acid as the fatty acid side chain, is reported to be one such stimulant. However, according to the structure of the compound, the fatty acid side chain seems highly susceptible to lipase decomposition, under in vivo metabolic conditions. To study this phenomenon, hericenone C from the ethanol extract of the fruiting body was subjected to lipase enzyme treatment and observed for changes in the chemical structure. The compound formed after the lipase enzyme digestion was isolated and identified using LC-QTOF-MS combined with 1H-NMR analysis. It was found to be a derivative of hericenone C without its fatty acid side chain and was named deacylhericenone. Interestingly, a comparative investigation of the neuroprotective properties of hericenone C and deacylhericenone showed that the BDNF mRNA expression in human astrocytoma cells (1321N1) and the protection against H2O2-induced oxidative stress was considerably higher in the case of deacylhericenone. These findings suggest that the stronger bioactive form of the hericenone C compound is in fact deacylhericenone.

DOI： 10.3390/molecules28114549

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researchmap

Language：English   Publishing type：Research paper (scientific journal)   Publisher：Cosmetics  

Nutritional foods are concentrated sources of molecules with a nutritional or physiological effect which contain nutrients. There is a category, “nutricosmetics”, defined as ingestible natural health products that enhance the function and appearance of human skin, nails, and hair. A new variety of Flammulina velutipes (F. velutipes), Oki-Shirayuki 919, was explored to ascertain whether its components have functions of nutricosmetics. We focused on physiological effects for enhancing the human skin condition, such as moisturizing or barrier functions in F. velutipes. A randomized, double-blind, placebo-controlled clinical study was performed between January and March 2022. Among healthy men and women (n = 30) aged 20 to 59 years, the test group (n = 15) took a test product which included F. velutipes dry powder, and the placebo group (n = 15) took a placebo (a similar product in which the F. velutipes dry powder was replaced with plum fruit paste). Since the amount of increase in skin hydration over four weeks in the test group was significantly larger than that in the placebo group, a significant difference between the two groups was observed (p = 0.033). F. velutipe was suggested to have some physiological functions such as improving skin moisture.

DOI： 10.3390/cosmetics10020057

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Planta Medica  

Although considered an abundant source of agricultural by-products, avocado (Persea americana Mill.) seed, with several biological activities and bioactive components, might become a promising resource for phytopharmaceutical development. In this study, through bioassay-guided isolation of the main α -glucosidase inhibitors in avocado seed, we discovered the major α -glucosidase inhibitor to be avocado seed oligomeric proanthocyanidin complex (ASOPC). Thiolysis and UPLC-DAD-HRESIMS showed the presence of A- and B-type procyanidins, and B-type propelargonidin with (epi)afzelechin as extension unit. Mean degree of polymerization (mDP) of ASOPC was calculated as 7.3 ± 1. Furthermore, ASOPC appeared to be a strong, reversible, competitive inhibitor of α -glucosidase, with IC 50value of 0.1 μg/mL, which was significantly lower than Acarbose (IC 50= 75.6 μg/mL), indicated that ASOPC is a potential natural α -glucosidase inhibitor. These findings would contribute to the direction of utilizing avocado seed bioactive components with the possibility to be used as natural anti-diabetic agents.

DOI： 10.1055/a-1878-3916

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Natural Product Communications  

Since the recent coronavirus disease 2019 pandemic and the lifestyle changes it necessitated, the demand for mental health treatment has skyrocketed, with long wait lists for both psychological and psychiatric care. Over-the-counter supplements and home remedies are increasingly sought. In this study, we screened natural materials and blended supplements from Asia that may improve the mood and mental health of humans by testing cell viability and expression of the proopiomelanocortin gene as a marker of β-endorphin production in rat hypothalamus neuron cells. Among 23 tested samples, 3 samples produced significantly higher cell viability in R-HTH-507 cells than the control treatment. In a real-time-polymerase chain reaction (RT-PCR) experiment, 7 samples showed significant β-endorphin synthesis activity. This is the first report that the Asian natural materials Areca catechu, Moringa oleifera, Lignosis rhinocerus, and Aegle marmelos promote β-endorphin synthesis; further investigation will identify the active ingredients in the blended samples. These results suggested that these Asian natural materials have great potential to expand the range of treatments for mental health.

DOI： 10.1177/1934578X231152964

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Science of the Total Environment  

Accumulating evidences show that the hazardous substance atmospheric nanoplastics increase the respiratory risk of individuals, but the inside toxicity mechanisms to lung tissue remain unclear. This study aims at investigating the potential mechanisms of inhaled cationic polystyrene nanoplastics (amine-polystyrene nanoplastics, APS-NPs)-induced pulmonary toxicity on mice. In vivo, the mice intratracheal administrated with APS-NPs suspension (5 mg/kg) were found inflammatory infiltrates in lung tissues through histopathology analysis. Furthermore, transcriptome analysis demonstrated that 1821 differentially expressed mRNA between APS group and control group were dominantly associated with 288 known KEGG pathways, indicating that APS-NPs might cause early inflammatory responses in lung tissue by activating the NLRP3/capase-1/IL-1β signaling pathway. Moreover, in vitro results also showed that NLRP3 inflammasome could be activated to induce pyroptosis in MLE-12 cells after exposure to APS-NPs. And, MH-S cells after exposure to APS-NPs exhibited increased Irg1 proteins, leading to the increasing generation of ROS and inflammatory factors (e.g., tnf-α, il-6, il-1β). In conclusion, these results revealed that Irg1/NF-κB/NLRP3/Caspase-1 signaling pathway was activated significantly after exposing to APS-NPs, leading to pulmonary toxicity on mice. Intriguingly, prior administration of the clinical antioxidant N-acetylcysteine (NAC) could serve as a possible candidate for the prevention and treatment of pulmonary toxicity induced by APS-NPs. The study contributes to a better understanding of the potential risks of environmental nanoplastics to humans and its improvement measure.

DOI： 10.1016/j.scitotenv.2022.158851

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Language：English   Publishing type：Research paper (scientific journal)  

DOI： DOI: 10.1002/jssc.202200717

Language：English   Publishing type：Research paper (scientific journal)   Publisher：Microchemical Journal  

A green vortex-assisted dispersive liquid–liquid microextraction (VA-DLLME) method based on a hydrophobic natural deep eutectic solvent (NaDES) was developed and applied for the preconcentration of anti-prostate cancer triple therapy (flutamide, resveratrol, and ethynylestradiol) from river water and spiked human plasma for the first time. A hydrophobic NaDES based on α-terpineol and octanoic acid was prepared in a molar ratio of 1:1 and applied as an extracting solvent. High-performance liquid chromatography with a photodiode array detector (HPLC-PDA), coupled with a core–shell-based column was used for the final analysis. The significant factors affecting the extraction efficiency were optimized by means of a systematic methodology of one-variable-at-a-time (OVAT) followed by experimental design. The optimal extraction conditions were as follows: 400 μL of DES, vortex time of 50 sec, pH 2.5, and 3 % of NaCl. Under optimal conditions, the method was validated through matrix-matched calibration, limits of detection and quantitation, accuracy, and precision studies. The method exhibited excellent linearity (r2 > 0.999) over a range of 1–30 μg/L for ethynylestradiol and 0.5–30 μg/L for both flutamide and resveratrol with % relative standard deviation (%RSD) values ≤ 4.87 %. The method was successfully applied for the analysis of the concerned drugs in spiked human plasma and river water samples. Finally, the procedure's greenness was assessed using three various greenness metrics which confirmed its greenness and safety.

DOI： 10.1016/j.microc.2022.108124

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Fitoterapia  

We collected stingless bee propolis Tetragonula biroi in order to find materials for medicine and cosmetics applications from tropical rainforest resources. Even though this bee has some biological functions including a cancer cell line, hair growth promotion, asthma remedy, α-glucosidase enzyme inhibition, and antiviral action, the investigation on anti-acne has not been reported yet. This study was to focus on propolis Tetragonula biroi extracts and leads us to isolate active compounds for antioxidant, anti-inflammatory, and anti-acne. We used methanol to obtain the extract from this propolis and assayed it with antioxidants, anti-inflammation, and anti-acne. The extract showed strong activity in antioxidants by DPPH radical scavenging activity (82.31% in 6.25 μg/ml). Via a column chromatography and Reveleris PREP purification system, we isolated 3’–O–methyldiplacone, nymphaeol A, and 5,7,3′,4′–tetrahydroxy–6–geranyl flavonol. These compounds showed potential biological activity with IC50 for antioxidant 6.33, 15.49, 17.32 μM; and antiinflammatory 121.54, 121.20, 117.31 μM. The isolated compounds showed anti-acne properties with properties 0.00, 14.11, and 13.78 mm for the inhibition zone (at a concentration of 1 μg/well), respectively. The results indicated that the propolis extract of Tetragonula biroi has the potential to be developed as a cosmetic agent; however, further work needs to be done to clarify its application.

DOI： 10.1016/j.fitote.2022.105375

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Molecules  

This study targets the evaluation of melanin synthesis inhibition activity of the bamboo shoot skin as agro-waste. The total methanolic extract of bamboo peel extract was evaluated for its skin protective effects via measuring its melanin inhibitory activity and its suppression activity on the expression of tyrosinase mRNA levels. Results showed that bamboo peel extract has a good ability for the inhibition of melanin synthesis so further studies were performed for the isolation of its constituents. Twelve compounds have been isolated from the shoot skin of Phyllostachys pubescens. Their structures were elucidated based on extensive spectroscopic methods. The melanin inhibition potential of the isolates was tested with their collagen-production-promoting activity for the determination of active principles. Results showed that Betulinic acid, tachioside, and 1,2-dilinolenin significantly suppressed melanin production per cell compared to control. Triacontanol, tricin, and (+)-lyoniresinol 9′-O-glucoside also tended to decrease melanin production per cell. These findings indicated that the skin of bamboo shoots, a significant agricultural waste, is a useful natural source for further research on its potential for aging problems such hyperpigmentation and cognitive function impairment.

DOI： 10.3390/molecules28010023

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Natural Product Research  

Four new natural compounds named hericenone O (1), hericenone P (2), hericenone Q (3), and hericenone R (4), two of them were reported synthetically (3–4), together with eleven known compounds were isolated from the fruiting bodies of Hericium erinaceus. The chemical structures of the isolated compounds were elucidated by using NMR analysis and mass spectrometry, as well as comparisons with the reported data in the literature. The bioactivity evaluation revealed that hericenone Q showed significant cytotoxic activity against Hep-G2 with IC50 values of 23.89 μM, and against HCT-116 with IC50 values of 65.64 μM.

DOI： 10.1080/14786419.2023.2169687

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Natural Product Research  

Juncus decipiens is a member of the Juncaceae family and has culinary, medicinal, and decorative properties. It is also used in traditional Chinese Medicines for many years that promotes diuresis for strangury and clears out heart fire. This species has recently gained medicinal attention as a source of phenanthrenes, phenolic compounds, glycerides, flavonoids, and cycloartane triterpenes. This plant was also shown to be active, and researchers explored its antioxidant, anti-inflammatory, antialgal, antibacterial, and psychological behaviour-boosting properties. Preliminary research suggests that this species might be used for skin protection and brain disorders if proper clinical trials are conducted. The ethnomedicinal, phytochemistry, biological potencies, dangers, and scopes of Juncus decipiens have been examined in this respect.

DOI： 10.1080/14786419.2023.2223749

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Language：English   Publisher：Journal of Separation Science  

New ternary deep eutectic solvents were prepared and applied as efficient green dispersing solvents in miniaturized matrix solid-phase dispersion to extract chlorophenols from river sediments for the first time. High-performance liquid chromatography coupled with a photodiode array detector was used to analyze the target analytes. The significant factors affecting the extraction were optimized as follows: dispersant (100 mg), sample (100 mg), ternary eutectic solvents (150 μl), grinding for 1 min, 450 μl of acetonitrile as the elution solvent, and vortex mixing for 20 s. Under the optimal conditions, the method exhibited excellent linearity (correlation coefficient > 0.9980), low limits of detection between 1.039–2.478 μg/g, and extraction recoveries between 93.9% and 99.2%. Furthermore, the method demonstrated excellent precision in the intra- and inter-day analysis with a relative standard deviation below 6%. When compared to conventional extraction techniques, the miniaturized matrix solid-phase dispersion considerably reduced samples and solvent usag, offering important environmental benefits. The green profile of the method was assessed using the complementary green analytical procedure index tool confirming its eco-friendship. The technique was finally employed to evaluate sediment samples from three distinct locations along the Zuibaiji River, indicating its applicability for monitoring environmental samples.

DOI： 10.1002/jssc.202200717

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Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)   Publisher：Natural Product Communications  

Bassia indica (Wight) A.J. Scott, family Amaranthaceae, is a halophyte herb growing in extreme environments and hence deemed as a potential economic source of bioactive chemicals with functional properties. In our study, 25 compounds were obtained from B. indica. We aimed to assess the inhibitory effect of the methanol extract of B. indica and its isolated compounds on COX-2 and cytotoxicity activity against MCF-7, OVK-18, HepG2, and HCT116 tumor cells. Among the isolates, the triterpene oleanane saponin (23) displayed promising anti-inflammatory activity with an IC50 = 3.05 ± 0.15 μg/mL. Additionally, N-trans-feruloyl tyramine (11) exhibited significant cytotoxicity to OVK-18 with IC50 = 1.74 ± 1.56 μg/mL, whereas 6,7-dihydroxy coumarin (7) exhibited potent inhibition against the MCF-7 cell line with IC50 = 1.47 ± 0.22 μg/mL. Interestingly, compounds 1 and 25 exhibited remarkable cytotoxicity against HepG2 and HCT116 cells with IC50 < 0.1 μg/mL, while compounds 2, 4, 5, 6, and 9 exerted potent cytotoxicity against HepG2. Finally, B. indica is a potential source of candidate compounds for the development of anti-inflammatory and antitumor therapies.

DOI： 10.1177/1934578X221137412

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：International Journal of Molecular Sciences  

Hyperpigmentation is a skin condition where patches of skin become darker in color due to excess melanin production upon UV exposure leading to melasma, which are lentigines or post inflammatory hyperpigmentation that psychologically affecting a great number of people. The present study investigates the anti-melanogenic effect of Butyroside D and the underling mechanism. After the confirmation of the non-cytotoxic effect of Butyroside D on B16F10 cells, we proceeded with analyzing the impact of the treatment at low and high concentration (i.e., 0.2 μM and 2 μM) using gene profiling analysis and examined the differentiation in gene expression. Our results identify cyclic adenosine monophosphate (cAMP), Wnt/β-catenin and Mitogen-Activated Protein Kinase (MAPK) signaling pathways to be downregulated upon treatment with Butyroside D. These pathways were targeted to further validate the effect of Butyroside D on membrane receptors melanocortin 1 receptor (MC1R) and receptor tyrosine kinase (c-Kit), related microphthalmia-associated transcription factor (MITF) and consequently tyrosinase (TYR), and tyrosine-related protein-1 (TYRP-1) that were all shown to be downregulated and, therefore, leading to the repression of melanin biosynthesis. Finally, the anti-melanogenic effect of Butyroside D was confirmed on human epidermal melanocytes (HEM) cells by inhibiting the activation of cAMP pathway generally mediated through α-melanocyte-stimulating hormone (α-MSH) and MC1R. Overall, this study suggests the potential applicability of this purified compound for the prevention of hyperpigmentation conditions.

DOI： 10.3390/ijms232416021

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Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publisher：(株)医事出版社  

肌トラブルの予防や軽減対策となる健康食品のヒト皮膚に及ぼす影響を明らかにするため、ヒハツモドキ(Piper retrofractum)果実抽出物の臨床試験を実施し、角層水分量、経皮水分蒸散量、メラニン・紅斑量の変化を調査した。令和2年10月～令和2年12月にかけて、日常的な肌の乾燥を感じている健康な成人女性39名を被験者とし、試験品群20名(平均48.9±6.9歳)とプラセボ群19名(平均48.4±6.1歳)に割り付けた。試験品はヒハツモドキ抽出物含有サプリメント(300mg/1粒)およびプラセボ(300mg/1粒)の2種、それぞれ1日あたり4粒(1200mg)とした。水分量、経皮水分蒸散量およびメラニンは時間(事前0週、中間4週、事後8週)と群の二要因間に有意な交互作用は認められず、試験品群、プラセボ群の測定値は同様の変化パターンを示した。紅斑について2群間に異なる変化パターンがみられた。肌状態の主観的評価の前後比較では、試験品群では13項目中7項目、プラセボ群では3項目が改善を示した。本試験の期間中、副作用または有害事象は観察されなかった。

Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)   Publisher：Molecules  

Chemical investigation of the total extract of the Egyptian soft coral Heteroxenia fuscescens, led to the isolation of eight compounds, including two new metabolites, sesquiterpene fusceterpene A (1) and a sterol fuscesterol A (4), along with six known compounds. The structures of 1–8 were elucidated via intensive studies of their 1D, 2D-NMR, and HR-MS analyses, as well as a comparison of their spectral data with those mentioned in the literature. Subsequent comprehensive in-silico-based investigations against almost all viral proteins, including those of the new variants, e.g., Omicron, revealed the most probable target for these isolated compounds, which was found to be Mpro. Additionally, the dynamic modes of interaction of the putatively active compounds were highlighted, depending on 50-ns-long MDS. In conclusion, the structural information provided in the current investigation highlights the antiviral potential of H. fuscescens metabolites with 3β,5α,6β-trihydroxy steroids with different nuclei against SARS-CoV-2, including newly widespread variants.

DOI： 10.3390/molecules27217369

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Language：English   Publishing type：Research paper (scientific journal)  

The phytochemical study of Agathophora alopecuroides (Chenopodiaceae) led to the isolation of previously undescribed glucosylceramide, flavonol triglycoside, and triterpene oleanane saponin, together with eight known compounds. Their structures were elucidated using NMR analysis and HR-MS as (2′R, 12E) N-[(2S, 3S, 4R)-1-(β-D-glucopyranosyloxy)-3,4-dihydroxy-octadec-2-yl]-2-hydroxytetracos-12-enamide, namely Agathophamide A; isorhamnetin-3-O-[β-D-xylopyranosyl-(1→3)-α-L-rhamnopyranosyl-(1→6)]-β-D-galactopyranoside, namely Agathophoroside A; and 3-O-[4'-(β-D-xylopyranosyl)-β-D-glucuronopyranosyl]-28-O-β-D-glucopyranosyl-olean-12-en-3β-ol-28-oic acid, namely Solysaponin A. We evaluated the effect of extract and isolates on ceramide levels via the up-regulated expression of the enzyme for ceramide synthesis in HaCaT keratinocytes. Interestingly, the study results revealed that the methanol extract of A. alopecuroides, together with some isolated compounds significantly up-regulated the mRNA expression of ceramide synthase-3 by 1.2- to 4.3-fold compared with the control in HaCaT cells. These findings indicate that the halophyte A. alopecuroides is a promising source of candidate compounds that can contribute to ceramide synthesis via the up-regulated expression levels of ceramide synthase-3 in the ceramide synthesis pathway.

DOI： doi:10.1016/j.phytochem.2022.113320

Language：English   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publisher：ライフサイエンス出版(株)  

薬用化粧品「白陽クリーム」を、30歳以上59歳以下の健常な女性を対象として1日2回朝・晩に顔の片側の目尻にのみに4週間使用し、目尻の写真から専門の検査員がシワグレードを判定するとともに被験者へのアンケートによって肌の状態の変化を検査した。解析対象数はn=14であり、対象者の年齢は38～54歳、平均47.8±5.0歳であった。試験品使用4週間前後における目尻のシワの変化について解析した。その結果、試験品使用側の目尻においては統計的有意なシワグレードの減少(シワの改善)が観測された。不使用側のシワグレードはわずかな増加を示した。使用側/不使用側シワ変化の群間比較からも統計的有意な差異が示唆され、試験品使用側の目尻におけるシワの改善効果が明らかとなった。被験者アンケートからはシワの改善に関しては統計的有意には至らなかったものの、試験品不使用側の得点が減少(状態の悪化)を示すのに対して、使用側の得点は上昇を示していた。

Language：English   Publishing type：Research paper (scientific journal)   Publisher：Sustainable Chemistry and Pharmacy  

Herein, a green dispersive liquid-liquid microextraction (DLLME) based on hydrophilic and hydrophobic deep eutectic solvents (DESs) was developed for the enrichment of bicalutamide (BIC) from water and spiked human plasma. Six hydrophobic and three hydrophilic DESs were synthesized and evaluated. The hydrophilic DES, composed of tetrabutylammonium bromide and acetic acid in a molar ratio of 1:2, was used as a dispersive solvent. Moreover, the hydrophobic DES, composed of borneol and capric acid in a molar ratio of 1:2, was applied as an extracting solvent. Significant factors affecting the extraction efficiency were investigated through the one-factor-at-a-time (OFAT) strategy. The optimized method was validated in terms of linearity, limits of detection and quantitation, accuracy, precision, and matrix effect. Good linearity with an excellent correlation coefficient (r2 > 0.9999 and 0.9987) was achieved as well as low limits of detection of 0.022 and 0.048 μg/mL and preconcentration up to 53.2 and 92.1 folds for water and plasma, respectively. The proposed DLLME method was coupled with spectrophotometric detection and applied for the analysis of BIC in river water and spiked human plasma with satisfactory recoveries (92.54–99.39%). Finally, the greenness of the developed procedure was evaluated using Complex Green Analytical Procedure Index (ComplexGAPI) and Analytical GREEnness (AGREEprep) tools, exhibiting excellent greenness in comparison to the previously reported methods.

DOI： 10.1016/j.scp.2022.100825

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Natural Product Research  

Two new compounds, 11S-methoxy-11,12-dihydro phytuberin (2) and 9S-methoxy-benzocyclononan-7-one (6), together with twenty-six known ones were isolated from Lycium schweinfurthii (Solanaceae). Their planar structure was established by extensive spectroscopic analyses. The absolute configuration of compound 6 was determined by time dependent density functional theory calculations (TDDFT). The cytotoxic potential of the isolates was assessed in cultured skin cancer (G-361) and colon cancer (HCT-116 and CaCo-2) cell lines. Certain flavonoids showed the highest cytotoxic activity, with IC50 values ranging from 7.1 to 63.3µM; meanwhile 5-flurouracil showed IC50 values ranging from 62.4 to >100 µM. All compounds showed minimal toxicity towards normal cells from skin (NHDF-4) and colon (CCD-841), indicating their potential selectivity and safety as cytotoxic candidates.

DOI： 10.1080/14786419.2021.1922902

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Language：English   Publisher：Phytochemistry  

The phytochemical study of Agathophora alopecuroides (Chenopodiaceae) led to the isolation of previously undescribed glucosylceramide, flavonol triglycoside, and triterpene oleanane saponin, together with eight known compounds. Their structures were elucidated using NMR analysis and HR-MS as (2′R, 12E) N-[(2S, 3S, 4R)-1-(β-D-glucopyranosyloxy)-3,4-dihydroxy-octadec-2-yl]-2-hydroxytetracos-12-enamide, namely Agathophamide A; isorhamnetin-3-O-[β-D-xylopyranosyl-(1→3)-α-L-rhamnopyranosyl-(1→6)]-β-D-galactopyranoside, namely Agathophoroside A; and 3-O-[4'-(β-D-xylopyranosyl)-β-D-glucuronopyranosyl]-28-O-β-D-glucopyranosyl-olean-12-en-3β-ol-28-oic acid, namely Solysaponin A. We evaluated the effect of extract and isolates on ceramide levels via the up-regulated expression of the enzyme for ceramide synthesis in HaCaT keratinocytes. Interestingly, the study results revealed that the methanol extract of A. alopecuroides, together with some isolated compounds significantly up-regulated the mRNA expression of ceramide synthase-3 by 1.2- to 4.3-fold compared with the control in HaCaT cells. These findings indicate that the halophyte A. alopecuroides is a promising source of candidate compounds that can contribute to ceramide synthesis via the up-regulated expression levels of ceramide synthase-3 in the ceramide synthesis pathway.

DOI： 10.1016/j.phytochem.2022.113320

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Publisher：Journal of Forest Research  

Although Chamaecyparis obtusa reduces soil pH and cation levels, limited information is available regarding their alterations after clear-cutting. We examined the soil pH and base cations on the upslopes and downslopes of individual trees and stumps of C. obtusa at two distances (0.5 m and 1.0 m) and three depths (0–5, 5–10, and 10–30 cm) in intact- and cut-tree plots. The soil pH was higher in the cut-tree plot than in the intact-tree plot, indicating the recovery of soil pH after clear-cutting. The recovery was more evident in the surface soils (0–5 cm) of downslope areas (0.5 m) than in other soil depths, which implies that the recovery of soil pH was caused by the lack of H+ supply from stumps after clear-cutting. The results of H+ (in H2O: water-soluble and KCl: exchangeable) suggested a lack of soluble H+ in the cut-tree plot. Soil Ca2+ and Mg2+ levels in the surface soil (0–5 cm) were 1.86-fold and 1.93-fold higher in the cut-tree plot than in the intact-tree plot, respectively, implying that the recovery of divalent cations after clear-cutting was caused by a reduction in cation loss through cation exchange with H+ derived from the stemflow. Collectively, soil pH and divalent cations were recovered after clear-cutting because the stemflow had ceased.

DOI： 10.1080/13416979.2022.2048987

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Molecules  

Hibiscus sabdariffa L. (HS) has a long history of edible and medicinal uses. In this study, the biological activities of the extracts, chromatographic fractions, and hibiscus acid obtained from HS were evaluated for their potential bioactivities. Their ability to promote extracellular matrix synthesis in skin fibroblasts was evaluated by enzyme-linked immunosorbent assays. Their anti-inflammatory activity was evaluated in a nitric oxide (NO)–Griess inflammatory experiment. Furthermore, hibiscus acid was found to have a strong anti-oxidative stress effect through the establishment of an oxidative stress model induced by hydrogen peroxide. Several assays indicated that hibiscus acid treatment can effectively reduce extracellular adenosine triphosphate (ATP) secretion and carbonyl protein production, as well as maintain a high level of reduced/oxidized glutathione (GSH/GSSG) in skin cells, thus providing a possible mechanism by which hibiscus acid can counter antioxidative stress. The present study is the first to explore the reversing skin aging potential and the contributory component of HS.

DOI： 10.3390/molecules27186076

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Language：Japanese   Publisher：ライフサイエンス出版(株)  

サジー果汁飲料の摂取による心身の疲労感に対する改善効果を検証するために、健常中年女性を対象に、4週間のプラセボ対照二重盲検ランダム化並行群間比較試験を実施した。対象者39名を無作為に割り付け、9名を除外し最終的に介入群14名(平均45.1±0.3歳)、プラセボ群16名(平均44.8±0.3歳)と設定した。対象者は、与えられた試験食品またはプラセボを1日30mL、4週間摂取した。心身の疲労に関する評価(visual analogue scale法)は心身疲労に関する自己評価アンケートにより実施した。心身の疲労時に現れる症状12項目(全体の疲労感、精神的疲労感、身体的疲労感、自覚的ストレス、緊張度、眠気、退屈度、意欲、空腹度、のどの渇き、イライラ感、爽快感)について、VAS法を使用した。心身の疲労に関する評価VASの結果、介入前後の差では「空腹感」のみに、介入群とプラセボ群で有意な差がみられた。介入前後の変化では、介入群のみに有意な減少がみられ、プラセボ群は有意でないものの平均値の上昇がみられた。安全性評価において、試験期間中に有害事象は認められなかった。

Language：Japanese   Publishing type：Research paper (bulletin of university, research institution)   Publisher：Faculty of Agriculture, Kyushu University  

Allergies are caused by abnormalities in the immune tolerance mechanism mediated by regulatory T cells (Treg), and the metabolites of the dietary fibers are important for the oral immune tolerance mechanism. Inulin acts as a dietary fiber and changes the intestinal microflora, which is expected to regulate the immune tolerance mechanism and to be a new treatment for allergies. In this study, we conducted a randomized, placebo-controlled, double-blind, parallel-group study in 49 adult subjects (13 males and 36 females) with various allergic symptoms to examine the effects of the supplementation of Fuji FF, a enzymatic synthesized soluble inulin, on allergic symptoms and mucosal immunity. Subjects took Fuji FF or placebo for 4 weeks, and changes in immune function were verified by two questionnaires and saliva tests. Though no clear improvements were found from Dermatology Life Quality Index (DLQI) and the saliva tests, the result of Japan Allergic Rhinitis Standard Quality of Life Questionnaire (JRQLQ) suggested the effectiveness in the suppression of allergic rhinitis symptoms. Our study indicates that Fuji FF can be applied as a treatment for nasal allergy-like symptoms.

DOI： 10.15017/4797835

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Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publisher：Molecules  

Averrhoa carambola L. is reported for its anti-obese and anti-diabetic activities. The present study aimed to investigate its aqueous methanol leaf extract (CLL) in vivo anti-obese activity along with the isolation and identification of bioactive compounds and their in vitro α-glucosidase inhibition assessment. CLL improved all obesity complications and exhibited significant activity in an obese rat model. Fourteen compounds, including four flavone glycosides (1–4) and ten dihydrochalcone glycosides (5–12), were isolated and identified using spectroscopic techniques. New compounds identified in planta included (1) apigenin 6-C-(2-deoxy-β-D-galactopyranoside)-7-O-β-D-quinovopyranoside, (8) phloretin 3′-C-(2-O-(E)-cinnamoyl-3-O-β-D-fucopyranosyl-4-O-acetyl)-β-D-fucopyranosyl-6′-O-β-D fucopyranosyl-(1/2)-α-L arabinofuranoside, (11a) phloretin3′-C-(2-O-(E)-p-coumaroyl-3-O-β-D-fucosyl-4-O-acetyl)-β-D-fucosyl-6′-O-(2-O-β-D-fucosyl)-α-L-arabinofuranoside, (11b) phloretin3′-C-(2-O-(Z)-p-coumaroyl-3-O-β-D-fucosyl-4-O-acetyl)-β-D-fucosyl-6′-O-(2-O-β-D-fucosyl)-α-L-arabinofuranoside. Carambolaside M (5), carambolaside Ia (6), carambolaside J (7), carambolaside I (9), carambolaside P (10a), carambolaside O (10b), and carambolaside Q (12), which are reported for the first time from A. carambola L. leaves, whereas luteolin 6-C-α-L-rhamnopyranosyl-(1-2)-β-D-fucopyranoside (2), apigenin 6-C-β-D-galactopyranoside (3), and apigenin 6-C-α-L-rhamnopyranosyl-(1-2)-β-L-fucopyranoside (4) are isolated for the first time from Family. Oxalidaceae. In vitro α-glucosidase inhibitory activity revealed the potential efficacy of flavone glycosides, viz., 1, 2, 3, and 4 as antidiabetic agents. In contrast, dihydrochalcone glycosides (5–11) showed weak activity, except for compound 12, which showed relatively strong activity.

DOI： 10.3390/molecules27165159

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Publisher：Revista Brasileira de Farmacognosia  

Phytochemical investigation of Ficus benghalensis L., Moraceae, leaves revealed three known compounds, carpachromene, mucusoside, and 2-O-α-l-rhamnopyranosyl-(2R)-hydroxyhexacosanoate-β-d-glucopyranosyl ester. Herein, the cytotoxic activity of the isolated compounds was measured against the HL60 cancer cell line. Our findings revealed that carpachromene exerted potent anti-proliferative activity. Also, this compound induced apoptosis and cell cycle arrest at the G2/M phase. Docking analysis revealed the potential interaction of carpachromene with topoisomerase I. This was confirmed by western blotting where carpachromene inhibited topoisomerase I protein expression. Additionally, carpachromene upregulated the expression of pro-apoptotic genes. In conclusion, F. benghalensis leaves exerted potent anti-proliferative activity against HL60 cancer cells. [Figure not available: see fulltext.]

DOI： 10.1007/s43450-022-00267-5

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Language：English   Publishing type：Research paper (scientific journal)   Publisher：Scientific Reports  

We examined the association of serum s-adenosylmethionine (SAM), s-adenosylhomocysteine (SAH) (methionine metabolites), and their ratio on the risk of dementia and death in a community-dwelling population of older Japanese individuals. 1371 residents of Hisayama, Japan, aged 65 years or older and without dementia, were followed for a median of 10.2 years (2007-2017). We divided serum SAM, SAH, and SAM/SAH ratio into quartiles. Cox proportional hazards models were used to estimate the hazard ratios (HRs) and their 95% confidence intervals (CIs) of serum SAM, SAH, and SAM/SAH ratio levels on the risk of a composite outcome of all-cause dementia or death, and each outcome. During the follow-up, 635 participants developed all-cause dementia and/or died, of which 379 participants developed dementia and 394 deaths occurred. The multivariable-adjusted HRs of the composite outcome decreased significantly with increasing serum SAM levels (P for trend = 0.01), while they increased significantly with higher serum SAH levels (P for trend = 0.03). Higher serum SAM/SAH ratio levels were significantly associated with a lower risk of the composite outcome (P for trend = 0.002), as well as with lower risk of each outcome. Our findings suggest that the balance of methionine metabolites may closely associate with the risk of dementia and death.

DOI： 10.1038/s41598-022-16242-y

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DOI： 10.1016/j.sajb.2022.01.028

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.1016/j.sajb.2022.01.028

Language：English   Publisher：RSC Advances  

In Alzheimer's disease (AD), the accumulation of amyloid-β plaques, overactivity of MAO-B, and phosphorylated tau protein in the central nervous system result in neuroinflammation and cognitive impairments. Therefore, the multi-targeting of these therapeutic targets has emerged as a promising strategy for the development of AD treatments. The current study reports the isolation and identification of seven amide alkaloids, namely, N-trans-feruloyl-3-methoxytyramine (1), N-trans-feruloyltyramine (2), S-(−)-N-trans-feruloylnormetanephrine (3), S-(−)-N-trans-feruloyloctopamine (4), R-(+)-N-trans-feruloyloctopamine (5), N-trans-caffeoyltyramine (6), and S-(−)-3-(4-hydroxy-3-methoxyphenyl)-N-[2-(4-hydroxyphenyl)-methoxyethyl]acrylamide (7), from B. indica and A. alopecuroides, which are halophytic plants that have been reported to contain diverse phytochemicals. Additionally, the study explores the potential inhibition effects of the isolates on β-secretase, monoamine oxidase enzymes, and phosphorylated tau protein, and their anti-aggregation effects on amyloid-β fibrils. Compounds 1, 2, and 7 showed potent inhibitory activity against BACE1, MAO-B, and phosphorylated tau protein, as well as anti-aggregation activity against Aβ-peptides. Additionally, compound 6 displayed promising inhibition activity against MAO-B enzyme. Further in-depth in silico and modeling analyses (i.e., docking, absolute binding free energy calculations, and molecular dynamics simulations) were carried out to reveal the binding mode of each active compound inside the corresponding enzyme (i.e., MAO-B and BACE1). The results indicate that B. indica, A. alopecuroides, and the isolated amide alkaloids might be useful in the development of lead compounds for the prevention of neurodegenerative diseases, especially AD.

DOI： 10.1039/d2ra02275c

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Publisher：Journal of Alloys and Compounds  

Photocatalytic treatment is a remarkable process that is popular for the degradation of several organic contaminants in wastewater. In this work, a series of graphitic carbon nitride/ZnTi-mixed metal oxide (CN/ZnTi-MMO) composites were prepared as photocatalysts through simple calcination. The CN-MMO samples were characterized and applied for photocatalytic degradation of ciprofloxacin (CIP), which is an antibiotic model pollutant. The optimized CN/ZnTi-MMO composite showed complete degradation of CIP within 20 min, leading to a rate constant that is approximately 6 times that of pristine CN and 7 times that of ZnTi-MMO. The increase in the degradation rate of the optimized CN/ZnTi-MMO composite was attributed to the excellent separation and transportation of photogenerated electron-holes pairs, as proven by the photoluminescence, photocurrent density, and electrochemical impedance spectroscopy results. Moreover, the energy-resolved distribution of the electron trap (ERDT) pattern of the composite sample suggests the formation of an interfacial electron trap state due to interfacial contraction in the composite, resulting in the excited electrons being trapped and avoiding charge recombination. Based on the optical properties, ERDT results, and activity test, a photocatalytic degradation mechanism of CIP over a CN/ZnTi-MMO composite was proposed. Additionally, the degraded solution showed less bio-toxicity than the original CIP solution. Thus, the CN/ZnTi-MMO composite can be employed as a potential visible-light-driven photocatalyst for the detoxification of pharmaceutical wastewater.

DOI： 10.1016/j.jallcom.2022.164294

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Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publisher：(株)医事出版社  

目的および方法:イヌリン含有食品の摂取により、心身の疲労感を自覚する健常人の疲労感・ストレスおよび粘膜免疫に与える効果を検証するために、心身の疲労感を自覚する健常人50名[解析対象者48名(男性24名、女性24名)]を対象にランダム化プラセボ対照二重盲検並行群間比較試験を実施した。摂取前後に唾液検査および質問紙検査を実施した。結果:その結果、POMS2における「疲労-無気力」「緊張-不安」「TMD得点」のスコアが有意に低下および「活気-活力」のスコアが有意に上昇した。視覚的評価スケール(VAS)においては、疲労感に関する項目の低下が認められた。風邪症状においては、「鼻づまり」「頭痛」「倦怠感」「寒気」「総合的な臨床症状」の有症日数に有意な低値が認められた。唾液検査においては、唾液分泌量が有意に増加、さらに唾液IgA分泌速度についても、有意な差は認められなかったもののプラセボ群と比較して増加した。結論:これらの結果からイヌリン含有食品の摂取により疲労感やストレスを軽減し活動的な気分を維持する効果が示唆された。さらに免疫機能向上および風邪症状の発症抑制、軽減効果が示唆された。(著者抄録)

Language：English   Publisher：Journal of Natural Medicines  

DOI： 10.1007/s11418-022-01611-8

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Language：Japanese   Publisher：ライフサイエンス出版(株)  

サジー果汁飲料の4週間摂取前後における免疫機能の変化を、血液検査、唾液検査、風邪症状や睡眠、腸内環境等を評価する質問紙検査の3種類の検査を実施することにより検証した。被験者37名を対象とし、試験品群18人(男性9人、女性9人、平均44.6歳)、プラセボ群19人(男性9人、女性10人、平均43.1歳)に割り付けた。サジー果汁飲料の常飲が血中の白血球成分に働きかけることで、自然免疫、獲得免疫を活性化している可能性が示唆され、唾液中におけるsIgA濃度の保持にサジー果汁飲料摂取が効果的であることが示された。試験品群にのみ睡眠の質の改善が認められ、気分の改善も確認された。このほか、サジー果汁飲料の常飲によって腸内環境が改善した可能性が考えられ、風邪にかかりにくく、かかったとしても回復のしやすい体調が整えられていることが示唆された。

Language：English   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publisher：ライフサイエンス出版(株)  

イヌリン5g含有サプリメントを4週間摂取した際の腸内環境や排便症状、肌質に及ぼす影響について検討するため、便秘傾向にある20歳以上の健康な女性を対象として、プラセボ対照二重盲検ランダム化並行群間比較試験を行った。イヌリン群15名、プラセボ群13名における便の性状と肌状態主観的評価のvisual analogue scale、dermatology life quality index(DLQI)、肌質検査、有害事象を評価した。その結果、イヌリン摂取によって排便に関する指標が改善し、DLQIでは「家事への支障」「仕事効率」への影響が減少した。肌のシワ、たるみ、透明感や化粧のり、顔色などが改善され、経表皮水分蒸散量と皮膚弾力性の変化率に有意な群間差を認めた。本試験において有害事象は認めなかった。イヌリンは肌バリア機能や肌の粘弾性を改善し、肌質を改善することが示された。

Language：English   Publisher：ライフサイエンス出版(株)  

Tongkat Ali(TA)補充がストレスマーカーと睡眠の質に与える影響について、4週間の並行二重盲検プラセボ比較対照試験を行った。健常者33名(30～60歳)をベースラインの年齢とBMIに基づいて、TAサプリメントを摂取するTA群とプラセボ錠を摂取するプラセボ群に配分した。気分プロフィール検査(POMS)とOSA睡眠調査表MA版(OSA-MA)を用いて比較した。4週間目にTA群だけPOMSの活気と友好のスコアが有意に改善した。TA群だけに4週目にOSA-MAの睡眠と起床に、有意なスコアの改善が認められた。

Language：English   Publisher：European Journal of Pharmacology  

Pulmonary fibrosis (PF) is a chronic interstitial lung disease with unknown etiology. In the present study, we evaluated the anti-fibrotic effects of heterophyllin B, a natural product from Radix Pseudostellariae having anti-inflammatory and tyrosinase inhibitory activities. In bleomycin (BLM)-induced PF mouse model, heterophyllin B treatments (5 or 20 mg/kg/d) significantly attenuated BLM-induced alveolar cavity collapse, inflammatory cell infiltration, alveolar wall thickening and collagen deposition. When compared to model group, heterophyllin B treatments also increased adenosine 5′-monophosphate (AMP)-activated protein kinase (AMPK) phosphorylation levels by 359% (P < 0.001) and reduced the expression of stimulator of interferon genes (STING) by 73% (P < 0.001). Furthermore, co-administration of heterophyllin B with AMPK inhibitor dorsomorphin (Compound C) significantly blocked the improvement effects of heterophyllin B on BLM-damaged lung tissue, and also increased the protein expression of STING which was inhibited by heterophyllin B in fibrotic lungs (P < 0.001). It is known that alveolar epithelia and lung fibroblasts exert prominent roles in the fibrosis progression. In the present study we found that, in vitro, heterophyllin B significantly inhibited alveolar epithelial mesenchymal transition (EMT) and lung fibroblast transdifferentiation. We also found that the inhibition of heterophyllin B on lung fibroblast transdifferentiation and STING expression was reversed by Compound C. To summarize, heterophyllin B exhibited protective effects on BLM-induced lung fibrosis potentially by inhibiting TGF-Smad2/3 signalings and AMPK-mediated STING signalings.

DOI： 10.1016/j.ejphar.2022.174825

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Language：English   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publisher：(株)医事出版社  

目的:本試験では、「膝に痛みまたは違和感のある者」を対象として、化粧品の塗布とマッサージを併用することにより、持続的な関節(肩、腰、膝))の痛みの緩和効果を検証することを目的とした。試験デザイン:ランダム化・プラセボ対照・二重盲検・並行群間比較試験。方法:30名をランダムに2群に割り付け、試験品またはプラセボの塗布とマッサージを28日間併用し、前後に質問紙検査(NRS、FRS、VRS、VAS)を実施した。結果:各質問紙検査において試験品群の関節(肩、腰、膝)の痛みに有意な低下または低下傾向が認められた。結論:試験品とマッサージを28日間併用することで、関節(肩、腰、膝))に対する痛み緩和効果が示唆された。さらにそれらは持続的にも有効であっことが確認された。(著者抄録)

Language：English   Publishing type：Research paper (scientific journal)   Publisher：Journal of Chromatography A  

四重極飛行時間型質量分析計と組み合わせた液体クロマトグラフィー（LCQTOFMS）に基づく包括的な非ターゲットスクリーニングワークフローを構築した。本研究により、廃液処理の流出水中内に、さまざまなクラス（主に医薬品と農薬）の74の化合物が同定された。同定された化合物の廃液処理中の生成と除去のプロセスを解明した。さらに、確認された化合物中、いくつかの医薬品がすべてのサンプルで最大の全体濃度を示し、次に難燃剤が多く定量された。非ステロイド系抗アンドロゲンであるビカルタミドは、難燃剤であるリン酸トリス（2-ブトキシエチル）が337.2〜1304.6の範囲の濃度を示した廃水流出液で、最高濃度（843.9〜3838 ng / L）で検出された。医薬品であるテルミサルタンは、潜在的な毒性を示す量存在していることが示された。多変量解析を適用して、廃水処理の効率を評価するとともに、メタボロミクスアプローチにより、流入サンプルと流出サンプルを明確に区別することができ、効果的な排水処理システムについての新規評価方法を提案した。

DOI： 10.1016/j.chroma.2022.462905

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Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Publisher：Natural Product Communications  

Chronic ultraviolet (UV) exposure produces oxidative stress, molecular damage, and aging-related signal transduction, all of which contribute to skin photoaging. In this study, the antioxidant and anti-inflammatory activities of Entada phaseoloides are reported. High-performance liquid chromatography (HPLC) detected 7 phenolic compounds: gallic acid, protocatechuic acid, 4-hydroxybenzoic acid, quercetin, luteolin, kaempferol, and apigenin. We investigated the antioxidant and protective effect of the acetone extract of E. phaseoloides leaves (AEP) on UVB-irradiated human epidermal keratinocytes (HaCaT cells). AEP showed antioxidant activity in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays. AEP at a concentration of 40 μg/mL increased cell survival rate of the UVB-damaged cells. Moreover, AEP blocked gene expression of nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in UVB-induced HaCaT cells and decreased UVB-induced apoptosis in HaCaT cells by regulating the gene expression of caspase-3. These results suggest that AEP has the potential to protect against UVB irradiation and antioxidant.

DOI： 10.1177/1934578X221078627

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Language：English   Publisher：Health Science Reports  

Introduction: Placenta extract is used as an ingredient in ointments for treating dermatological diseases, skin dryness, and for skin beautification. However, the clinical effects of the equine placenta on humans and the underlying mechanism of action are unclear. This randomized, controlled, double-blind study aimed to clinically evaluate the effect of oral intake of equine placental extract on human skin quality. Methods: Healthy women volunteers between the ages of 30 and 59 years (n = 29) were randomly assigned to receive 220 mg of equine placental extract–placebo orally, once daily for 4 weeks. Skin quality parameters such as skin hydration, skin barrier function (transepidermal water loss [TEWL]), and melanin index were assessed at baseline and after 4 weeks of administration. Results: The melanin index was significantly increased in the placebo group, whereas it remained unchanged in the equine placenta group. The pattern of melanin index change was significantly different due to intake or no intake of equine placenta supplements over 4 weeks. No significant difference was found in skin hydration and TEWL between the two groups at 4 weeks of postadministration. It was shown that the intake of the equine placenta was more effective in protecting the skin condition against the change of ultraviolet (UV) sensitively than the change in temperature and humidity. Conclusions: Effect of equine placental extract intake was evident on the cheek skin of the equine placenta group where participants were protected from UV-induced pigmentation. Equine placental extract is useful for decreasing melanin synthesis and melanin content in the human skin and can be used as an effective food supplement to maintain human skin quality.

DOI： 10.1002/hsr2.522

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Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)   Publisher：International Journal of Environmental Research and Public Health  

This study compared the participants' physiological responses and subjective evaluations of air scented with different concentrations of common rush (Juncus effusus L. var. decipiens Buchen.) (30 g and 15 g, with fresh air as a control). We asked 20 participants to complete a series of visual discrimination tasks while inhaling two different air samples. We evaluated (1) brain activity, (2) autonomic nervous activity, and (3) blood pressure and pulse rate, (4) in combination with self-evaluation. In addition, we quantified the concentrations of volatile organic compounds. The participants reported the scent to be sour, pungent, and smelly; this impression was likely caused by hexanal and acetic acid. Although the self-evaluations showed that participants did not enjoy the scent, their alpha amplitudes of electroencephalogram and parasympathetic nervous activity were increased, suggesting that participants were relaxed in this atmosphere. Moreover, a lower concentration resulted in a greater induction of relaxation. While the air was not pleasant-smelling, the volatile organic compounds present had a positive psychophysiological impact.

DOI： 10.3390/ijerph19031856

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Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publisher：Molecules  

The extract from Entada phaseoloides was employed as active ingredients of natural origin into cosmetic products, while the components analysis was barely reported. Using LC-DAD-MS/qTOF analysis, eleven compounds (1–11) were proposed or identified from acetone extract of E. phaseoloides leaves (AE). Among them, six phenolic compounds, protocatechuic acid (2), 4-hydroxybenzoic acid (3), luteolin-7-O-β-d-glucoside (5), cirsimaritin (6), dihydrokaempferol (9), and apigenin (10), were isolated by various chromatographic techniques. Protocatechuic acid (2), epicatechin (4), and kaempferol (11) at a concentration 100 μM increased the HaCaT cells viability of the UVB-irradiated cell without any cytotoxicity effect and reduced the expression of COX-2 and iNOS inflammation gene. Moreover, compounds 2 and 4 could have potent effects on cell migration during wound closure. These results suggest that compounds 2, 4, and 11 from AE have anti-photoaging properties and could be employed in pharmaceutical and cosmeceutical products.

DOI： 10.3390/molecules27020440

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Language：English   Publisher：Phytomedicine  

Background: Bryodulcosigenin (BDG) a cucurbitane-type triterpenoid has been isolated from the roots of Bryonia dioca and possesses marked anti-inflammatory effects, although its beneficial effect against intestinal disorders remains unclear. Purpose: To explore the underlying mechanism of BDG on the dysbiosis of chronic ulcerative colitis (UC) and its associated side-effects on lung tissues. Methods: A chronic UC model was established using 2.5% dextran sulfate sodium (DSS) in mice treated for 64 days and diagnostic assessments, western blot analysis and quantitative real time-PCR were employed to determine the protective mechanism of BDG. Results: Oral administration of BDG (10 mg/kg/day) significantly improved colon length, disease activity index, and alleviated colonic histopathological damage in the DSS-induced colitis mice. BDG not only reversed the TNF-α-induced degradation of tight junction proteins (occludin and ZO-1) but also suppressed the elevated apoptosis seen in intestinal epithelial cells (NCM460). In addition, BDG significantly attenuated damage in alveolar epithelial cells (MLE-12) co-cultured with NCM460 cells under inflammatory conditions. Furthermore, BDG in vivo significantly prevented the symptoms of respiratory disorders and repressed alveolar inflammation by regulating DSS-induced chronic colitis in mice. Conclusion: BDG effectively inhibited the apoptosis of intestinal epithelial cells and suppressed the activation of the NLRP3 inflammasome which resulted in the restoration of the intestinal barrier. Therefore, the enhanced integrity of intestinal epithelial cells produced by BDG intervention contributed to its anti-colitis effects, indicating its great potential as an inhibitor of UC and lung injury. Therefore, restoring intestinal integrity may represent a promising strategy in the prevention of pulmonary disease.

DOI： 10.1016/j.phymed.2021.153814

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Publisher：Journal of Food and Drug Analysis  

Shiikuwasha (Citrus depressa Hayata) essential oil (SEO) extracted from Shiikuwasha fruit pulp contains two major volatile components, limonene and g-terpinene (56.56e57.31 and 24.41e24.98%, respectively). In this study, we showed that the aroma streams of SEO, limonene, and g-terpinene exhibited significant physiological stress amelioration effects in nine healthy female panelists tested in a 30-min visual display task. While SEO administration significantly reduced work errors by 15 min compared to the odorless control condition, the limonene stream reduced work errors only at the first and fourth 5-min intervals, and the g-terpinene effect lasted only for the initial 5-min. However, g-terpinene inhalation reduced stress by significantly increasing post-work electrocardiogram ReR interval variability and lowering electroencephalogram beta wave powers at the midline occipital Oz position. Additionally, SEO, limonene, and g-terpinene displayed anti-inflammatory activity in vitro by suppressing the pro-inflammatory markers NO and IL-1b in BV- 2 microglial cells in a dose-dependent manner.

DOI： 10.38212/2224-6614.3414

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Language：English   Publisher：Malaysian Journal of Medical Sciences  

The broader objective of this study is to identify natural materials that might inhibit the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection. We have focused on stingless bee honey, which has a unique taste that is both sweet and sour and sometimes bitter. We screened 12 samples of honey from 11 species of stingless bees using an angiotensin-converting enzyme 2 (ACE2)-spike protein-binding assay and phytochemical analysis. Ten of the samples showed inhibition above 50% in this assay system. Most of the honey contained tannins, alkaloids, flavonoids, triterpenoids, carotenoids and carbohydrates. Our findings in this in vitro study showed that honey from stingless bees may have a potent effect against SARS-CoV-2 infection by inhibiting the ACE2-spike protein-binding.

DOI： 10.21315/mjms2022.29.5.15

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Publisher：International Journal of Medicinal Mushrooms  

Epidemiologic studies have shown a high prevalence of multiple sclerosis (MS) in Europe and North America, and a low prevalence in East Asia. Mushrooms contain various biological response modifiers (BRMs) and are widely used in traditional Chinese medicine in East Asian countries. To investigate whether mushrooms have potential beneficial effects on MS, we administered mushrooms to cuprizone (bis-cyclohexanone-oxalyldihydrazone, CPZ)-in-duced MS model mice. This model is used to study the processes of demyelination in the CNS. The CPZ-induced de-myelination is involved in the apoptotic death of mature oligodendrocytes, neuroinflammation, and motor dysfunction. Mice were fed a powdered diet containing 5% each mushroom and CPZ diet for 5 weeks, which coincides with peak demyelination. We measured the body weight of the mice, evaluated their motor function using a rotarod, and quanti-fied the myelin levels using Black-Gold II staining. Ganoderma lucidum and Hericium erinaceus treatments showed recovery from weight loss. Pleurotus eryngii, G. lucidum, and Flammulina velutipes treatments significantly improved CPZ-induced motor dysfunction. P. eryngii, G. lucidum, F. velutipes, and H. erinaceus treatments effectively suppressed CPZ-induced demyelination. The four medicinal mushrooms may be promising BRMs for prevention and alleviation of the symptoms of MS.

DOI： 10.1615/IntJMedMushrooms.2022044840

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Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.3390/molecules26247646

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DOI： 10.1016/j.cej.2021.130502

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DOI： 10.1016/j.sjbs.2021.08.017

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DOI： doi:10.3390/molecules26237406

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DOI： 10.1039/d1ra03937g

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DOI： 10.1039/d1ra05927k

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DOI： 10.1016/j.fitote.2021.104907

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DOI： 10.1080/14786419.2019.1663513

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1039/d0ra06565j

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.1080/14786419.2019.1616730

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DOI： 10.1080/14786419.2019.1687477

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DOI： 10.1177/1934578X211023363

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1080/14786419.2019.1655017

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1016/j.jchromb.2021.122555

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.13057/biodiv/d220412

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1016/j.jff.2020.104280

Language：English   Publishing type：Research paper (scientific journal)   Publisher：Natural Product Research  

N-[(3-(3-methyl-1-oxo-butyl)amino)propyl]-3-(3,4-dihydroxyphenyl)prop-2-enamide (7), named ‘Bassiamide A’, a new alkaloid, together with six known compounds including one lignan (1) and five lignanamides (2–6), were isolated from the aerial parts of Bassia indica Wight. The study also reported an optimal separation of a rare occurring R-isomer lignanamide derivative (6) from a natural origin, in addition to its known corresponding S-isomer (5). Structures of isolated compounds were elucidated based on NMR spectroscopic data, HR-MS, and comparison with known related ones, and they were identified as syringaresinol (1), N-trans-feruloyl-3-methoxytyramine (2), N-trans-feruloyltyramine (3), S-(-)-N-trans-feruloyl normetanephrine (4), S-(-)-N-trans-feruloyl octopamine (5), R-(+)-N-trans-feruloyl octopamine (6). The isolated compounds were evaluated for their anti-acetylcholinesterase activity, and they showed weak inhibitory activity.

DOI： 10.1080/14786419.2021.1872572

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Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1080/14786419.2019.1624958

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1016/j.phymed.2020.153427

Language：Japanese   Publishing type：Research paper (scientific journal)   Publisher：Natural Product Research  

In our promising project toward discovery of secondary metabolites with potential anticancer activity against human cervical cancer, seven marine organisms were screened for their cytotoxic activity against HeLa cancer cell line using MTT colorimetric assay. The crude extract of the outer shell of Diadema setosum showed promising activity with 88.02% inhibition at a concentration 250 µg/ml. Chromatographic investigation of the Ethyl acetate fraction, which is the main contributor to the activity (IC50= 43.1 ± 5.94 µg/ml), led to isolation of five compounds. Structures of the isolates (1-5) were elucidated by 1 D and 2 D NMR spectroscopy and HR-ESI-MS analysis. 5α,8α-epidioxycholest-6-en-3β ol (2) and 5α,8α-epidioxycholest-6,9(11)-en-3β ol (3) showed the highest cytotoxic activity with IC50 values 12.1 ± 2.74 µg/ml and 21.8 ± 6.32 µg/ml, respectively. Epidioxy steroids with cholestane nucleus could be a prospective candidate for the development of drugs for treatment of human cervical cancer.

DOI： 10.1080/14786419.2020.1855162

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Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1016/j.jphs.2020.08.002

Language：Japanese   Publishing type：Research paper (scientific journal)  

A green air-assisted dispersive liquid-liquid microextraction based on floating organic droplet solidification (DLLME-SFOD) was introduced for the enrichment of five endocrine disrupting compounds (EDCs) from water using a ternary deep eutectic solvent (TDES) as an extracting solvent prior to their determination by HPLC-PDA. The eutectic solvents were synthesized by combining various fatty acids which can concurrently act as both hydrogen bond acceptors (HBA) and hydrogen bond donors (HBD). Adding a third component to classical two-component eutectic solvents allows to purposefully control density, melting point, and viscosity of the synthesized solvents. Ternary and binary eutectic solvents with C9 acid provided excellent extraction efficiency in comparison with other eutectic solvents with C8 acid, while ternary solvents provided superior extraction efficiency to binary ones. Different variables that could influence the microextraction efficiency were optimized applying central composite face-centered design (CCF). At the optimum conditions, the method had low detection limits ranging from 0.96–2.30 µg/L with a preconcentration up to 134-folds. The method showed good linearity from the linear regression with an excellent correlation coefficient (r2 > 0.999). A good inter- and intraday precision (%RSD < 7%) and%recovery > 90% were achieved proving the method high precision and accuracy. Furthermore, the potential of using the TDES for determining the EDCs from five real water samples was proved through the higher extraction efficiency of the EDCs (90.06–104.43%) with results uncertainty < 20% for most of the compounds. Finally, the method greenness was evaluated by Raynie pictogram, analytical eco-scale, and Green Analytical Procedure Index (GAPI) approaches which confirm the superior eco-friendship of our method in comparison with other reported methods.

DOI： 10.1016/j.chroma.2020.461498

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.13057/biodiv/d211021

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.17707/AgricultForest.66.3.08

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.1186/s10086-020-01910-2

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1039/d0ra05265e

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1021/acsomega.0c01622

Language：Japanese   Publishing type：Research paper (scientific journal)   Publisher：Natural Product Research  

New cycloartane-type triterpene 23 R/S-3β-hydroxycycloart-24-ene-23-methyl ether 1a,b (as an C-23 epimeric mixture), along with ten known compounds, including 1 steroid, 3 fatty acids and 6 triterpenoids were isolated from the aerial parts of Euphorbia dendroides L. (Euphorbiaceae). The known compounds (2–11) were identified using 1 D & 2 D-NMR spectra and by comparison with data reported in the literature as well as using GC-MS for the isolated fatty acids. The new compound 1 (a,b) was elucidated by comprehensive 1 D & 2 D NMR experiments as well as LR & HR-FAB-MS. In addition, the isolated cycloartane-type triterpenoids have been tested for in vitro cytotoxicity against different cell lines. The new compound 1 (a,b) exhibited good to weak selective cytotoxic activities against HepG2, Huh-7, KLM-1, 1321N1 and HeLa cell lines with IC50 values of 20.67 ± 0.72, 16.24 ± 0.53, 22.59 ± 0.94, 25.99 ± 0.31 and 40.50 ± 3.14 μM, respectively.

DOI： 10.1080/14786419.2020.1800693

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Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.3390/nu12061671

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1080/14786419.2018.1530231

Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Eucalyptol is one of the most popular volatile components. It is used in many essential oils for relieving
sinus and lung congestion caused by a variety of conditions. This pilot study sought to analyze clinical
evidence for the effect of the scent of eucalyptol on the cognitive function of elderly people. Seventy
nursing-home residents with cognitive impairment were recruited. Three one-week experiments were
performed: eucalyptol scent was diffused in bedrooms with a diffuser only at wake-up time in the first
experiment, and at wake-up time and bedtime in the second and third experiments. Results showed
that although an improvement was not seen when using Mini Mental State Examination (MMSE) and
Cohen-Mansfild Agitation Inventory (CMAI) measures, Dementia Behavior Disturbance Scale (DBD)
scores improved significantly, even though no subject reported perceiving the scent. The significant
improvements of the behaviour were found not only among the subjects whose room had a diffuser but
also among the subjects who were exposed to an unperceivable level of eucalyptol drifted in the living
room.

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.25135/rnp.142.19.04.1264

Language：English   Publishing type：Research paper (scientific journal)  

DOI： doi:10.4005/jjfs.102.191

Language：English   Publishing type：Research paper (scientific journal)  

Propolis from 4 stingless bees (Homotrigona apicalis, Wallacetrigona incisa, Tetragonula fuscobalteata, and Tetragonula fuscibasis) was investigated in the search for medicinal and cosmetic materials from tropical rainforest resources. Methanol extracts of the propolis were screened using antioxidant and antimelanogenesis assays (tyrosinase enzyme activity and melanin inhibitor in B16 melanoma). The extract of H. apicalis showed the strongest antioxidant activity, both in the 2,2-diphenyl-1-picrylhydrazyl and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) assays, with half-maximal inhibitory concentration values of 0.72 ± 0.01 (mg/mL) and 0.26 ± 0.00 (mg/mL), respectively. The H. apicalis extract also displayed the strongest inhibition of tyrosinase (53% at 100 µg/mL). In the B16 melanoma cell assay, the W. incisa extract showed the strongest inhibition of melanin (21%) and was less cytotoxic. The W. incisa extract was fractioned to isolate the compounds with biological activities. Two prenylated flavonoids were obtained, named broussoflavonol F and glyasperin A. Both showed potent antioxidant activities, as well as inhibiting melanin in B16 melanoma, but not tyrosinase activity. These results indicated the potential of methanol extract of W. incisa to be developed for cosmetic material, but further experiments are needed to verify the function.

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1007/s00044-020-02520-9

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1186/s10086-020-01910-2

Language：English   Publishing type：Research paper (scientific journal)  

In order to discover new anti-obesity agents, twenty two natural extracts from medicinal plants and agricultural wastes were screened by pancreatic lipase inhibition assay. The methanolic extract of poplar wood (Populus alba L.), an important raw material for paper industry, showed promising inhibitory activity, its IC₅₀ value was 7.15 μg/mL. Through bio-guided fractionation, the ethyl acetate fraction (E) was found to be the major contributor to the activity, IC₅₀ = 4.7 μg/mL. Hence, it was subjected to bio-guided isolation and nine compounds (1–9) were identified from the active sub-fractions. The isolates were identified by means of one- and two-dimensional nuclear magnetic spectroscopy (1D, 2D-NMR), as well as high-performance liquid chromatography quadrupole time-of flight mass spectrometry (HPLC-QTOF-MS). (+)-Taxifolin (5) and (+)-ampelopsin (4) showed the highest activity, their IC₅₀ values were 23.2 and 46.2 μM, respectively. The results indicated that flavonoids and phenolic acids in poplar wood could serve as potential candidates for development of new anti-obesity agents.

DOI： https://doi.org/10.1016/j.indcrop.2019.111778

Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

DOI： https://doi.org/10.1016/j.microc.2019.103988

Language：English   Publishing type：Research paper (scientific journal)  

Plant derived compounds are a source of long term research focus due to their applications in a variety of fields, particularly food preservation. One key way in which phytochemicals are crucial in this area is by disrupting enzyme functionality. In this work, essential oil was extracted by steam distillation from the fresh leaves of Polygonum odoratum (Polygonaceae), commonly known as Vietnamese coriander, and shown to effectively inhibit the oxidation of L-3,4-dihydroxyphenylalanine (L-DOPA) catalyzed by mushroom tyrosinase (EC1.14.18.1). Using GC-MS analysis, twenty five compounds were identified in the essential oil. The most abundant compounds in the essential oil were Alkanals - dodecanal (55.49%), and decanal (11.57%) - followed by anisaldehyde (6.35%); these compounds were individually investigated for inhibitory activity by performing single-compound screening. Each of the top three most abundant compounds inhibited the tyrosinase-catalyzed oxidation of L-DOPA, as identified by UV-VIS spectroscopy and oxygen consumption assays. The inhibitory activity of the major com- pounds increased when pre-incubated with tyrosinase and without significant additional oxygen consumption, suggesting kcat-type inactivation is not involved. Interactions of the head and tail components of the major alkanals may disrupt the tertiary structure of the enzyme, presenting a potential inhibitory mechanism. 

DOI： https://doi.org/10.1016/j.heliyon.2019.e02817

Language：English   Publishing type：Research paper (scientific journal)  

Mushrooms have garnered immense popularity for their nutritional as well as medicinal values. The therapeutic potential of mushrooms in Nepal, a country well known for its biodiversity and natural medicinal resources, remains largely unstudied. Therefore, this study attempts to unveil the antioxidative properties of Nepalese wild mushrooms. Sixty-two wild mushroom samples were collected from several forests in different parts of Nepal. Ethanol and water extracts of the dried samples were tested for their antioxidative activities using total phenolic content (TPC), oxygen radical absorbance capacity (ORAC) assay, 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and reducing power (RP) assays. Ethanol extracts of samples belonging to the order Hymenochaetales showed significantly high activity in all the assays. Inonotus clemensiae had an exceptionally high TPC of 643.2 mg gallic acid equivalent (GAE)/g extract and also exhibited the lowest EC50 values in DPPH (0.081 mg/mL), ABTS (0.409 mg/mL), and EC0.5 value in reducing power (RP; 0.031 mg/mL) assays. High-performance liquid chromatography (HPLC) analysis of the top ten samples with the highest TPC was done to identify the phenolic compounds in the extracts, followed by liquid chromatography-mass spectrometry (LC-MS) analysis for some unknown compounds. These findings highlight the very strong antioxidative activity of Nepalese mushrooms, and paves the way for further research to explore their economic potential.

DOI： 10.1007/s11418-016-1013-1. Epub 2016 Jun 4.

Language：English   Publishing type：Research paper (scientific journal)  

A series of new isoxazolyl, triazolyl and phenyl based 3-thiophen-2-yl-quinoline derivatives were synthesized adopting click chemistry approach. In addition, the synthesis of new useful synthon, (2-chloroquinolin-3-yl) (thiophen-2-yl) methanol, is reported. The obtained compounds were characterized by spectral data analysis and evaluated for their anticancer activity. All the derivatives were subjected to in vitro MTT cytotoxicity screening assay against a panel of four different human cancer cell lines, liver (HepG-2), colon (HCT-116), human cervical cancer (HeLa) and breast (MCF-7). Out of a library of 17 compounds, two compounds have been identified as potent and selective cytotoxic agents against HeLa and MCF-7 cell lines. SAR studies for such hybridized analogues were investigated and phenyl derivatives were proved to be more potent than isoxazole and triazole derivatives. Furthermore, the promising compounds were selected for in vitro inhibition of EGFR-TK and Topo II enzymes. Also, they were subjected to cell cycle arrest analysis and apoptosis assay on MCF-7 cells. Our recent finding highlights these thiophene-quinoline analogues as a promising class of compounds for further studies concerning new anticancer therapies.

DOI： 10.1016/j.bmc.2019.07.042

Language：English   Publishing type：Research paper (scientific journal)  

A series of new isoxazolyl, triazolyl and phenyl based 3-thiophen-2-yl-quinoline derivatives were synthesized
adopting click chemistry approach. In addition, the synthesis of new useful synthon, (2-chloroquinolin-3-yl)
(thiophen-2-yl) methanol, is reported. The obtained compounds were characterized by spectral data analysis and
evaluated for their anticancer activity. All the derivatives were subjected to in vitro MTT cytotoxicity screening
assay against a panel of four different human cancer cell lines, liver (HepG-2), colon (HCT-116), human cervical
cancer (HeLa) and breast (MCF-7). Out of a library of 17 compounds, two compounds have been identified as
potent and selective cytotoxic agents against HeLa and MCF-7 cell lines. SAR studies for such hybridized analogues
were investigated and phenyl derivatives were proved to be more potent than isoxazole and triazole derivatives.
Furthermore, the promising compounds were selected for in vitro inhibition of EGFR-TK and Topo II enzymes.
Also, they were subjected to cell cycle arrest analysis and apoptosis assay on MCF-7 cells. Our recent
finding highlights these thiophene-quinoline analogues as a promising class of compounds for further studies concerning
new anticancer therapies.

DOI： https://doi.org/10.1016/j.bmc.2019.07.042

Language：English   Publishing type：Research paper (bulletin of university, research institution)  

Language：English   Publishing type：Research paper (scientific journal)  

Soil water repellency (SWR) is a cause of low water infiltration, overland flow and soil erosion in mountainous coniferous plantations in Japan. The factors determining SWR intensity were investigated in two coniferous plantations of Chamaecyparis obtusa (Siebold et Zucc.) Endl. and Cryptomeria japonica (L.f.) D. Don, using intact tree plots and cut tree plots on the same hillslope. The SWR of Ch. obtusa plots was stronger than that of Cr. japonica plots. SWR intensity decreased after tree cutting. There were no significant differences in SWR upslope and downslope of individual trees/stumps for both tree species, though areas downslope of individual Ch. obtusa trees had higher SWR intensity than those upslope. SWR intensity and soil aggregate stability were positively correlated in the Ch. obtusa intact tree plot (r = 0.88, p < 0.01), whereas in the cut tree plot, this correlation was weak with no significance (r = 0.29, p = 0.41). Soil aggregate size had a non-significant influence on SWR intensity. These findings suggest that SWR intensity was not related to the soil aggregate size, but SWR intensity seemed have a role in soil aggregation in the Ch. obtusa intact tree plot. Destruction of soil aggregates could occur after tree cutting because of physical disturbances or increased input of different types of organic matter from other vegetation into soil. The presence of Ch. obtusa introduces a source of SWR, although uncertainty remains about how water repellency is distributed around soil aggregates. The distribution pattern of soil water content and soil hydraulic conductivity around Cr. japonica was related to other factors such as the litter layer and non-water-repellant soil.

DOI： 10.3390/f10090730

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.1016/j.microc.2019.103988

Language：English   Publishing type：Research paper (scientific journal)  

We examined the association between serum concentrations of β-alanine, a metabolite of carnosine and anserine, and the risk of dementia
in a general population of elderly Japanese persons. In 2007, 1,475 residents of Hisayama, Japan, aged 60–79 years and without dementia were divided into 4 groups according to quartiles of serum β-alanine concentrations (quartile 1, lowest; quartile 4, highest) and followed for a median of 5.3 years. During follow-up, 117 subjects developed all-cause dementia (Alzheimer in 77 cases and vascular dementia in 31).
The risk of all-cause dementia decreased with increasing serum β-alanine levels after adjustment for potential confounding factors
(quartile 2, hazard ratio (HR) = 0.73 (95% confidence interval (CI): 0.45, 1.18); quartile 3, HR = 0.50 (95% CI: 0.28, 0.89); quartile 4,
HR = 0.50 (95% CI: 0.27, 0.92); P = 0.01 for trend). A similar inverse association was observed for Alzheimer disease (quartile 2, HR = 0.78 (95% CI: 0.44, 1.38); quartile 3, HR = 0.53 (95% CI: 0.26, 1.06); quartile 4, HR = 0.53 (95% CI: 0.25, 1.10); P = 0.04 for trend)
but not for vascular dementia. We found that higher serum β-alanine levels were significantly associated with lower risks of all-cause dementia and Alzheimer disease. Because serum β-alanine levels reflect intakes of carnosine/anserine, higher intakes of carnosine/anserine might be beneficial for the prevention of dementia.

DOI： https://doi.org/10.1093/aje/kwz116

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.1016/j.phytol.2019.04.017

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.1002/cbdv.201900237

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Lotus root (Nelumbo nucifera) is a popular food in Japan and southeast Asia. It is reported that lotus root includes dietary fiber, vitamin C, and abundant polyphenolic compounds. In Chinese medicine, lotus powder is also utilized in anti-tussive or anti- inflammatory drugs. In this study, we focused on the effects of lotus root powder on allergy symptoms in mice. First, we assessed nasal allergy symptoms in 2,4-diisocyanic acid toluene (TDI)- sensitized nasal allergy model mice. We found that lotus root powder alleviated nasal allergy symptoms in the mice. In addition, we estimated serum inflammatory parameters such as serum total IgE, histamine, and leukotriene B4. Lotus root powder intake significantly decreased serum total IgE and leukotriene B4 compared with standard food intake. We suggest that lotus root powder intake may alleviate allergic symptoms.

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.1016/j.jff.2019.04.058

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.1177/1934578X19867192

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1093/chromsci/bmz020

Language：Japanese   Publishing type：Research paper (scientific journal)  

As a construction material, Sugi (Cryptomeria japonica) is widely used in Japan. Present study focused on how wooden dwelling spaces with Sugi wood material influence quality of human sleep. To clarify this, Room A where naturally processed Sugi wood boards were used for the interiors and the Room B where chemically processed wood materials comprised of bonded or coated woods were used for the interiors were investigated for comparison. Volatile organic compounds (mainly sesqui-terpenes) emitted from both rooms were analyzed by Gas Chromatography/Mass Spectrometry. Ten participants were asked to take a sleep in the two rooms, respectively. Salivary stress markers, sleep time, blood pressure, questionnaires were measured. Humidity and temperature of the both rooms were recorded. The participants’ lifestyles were also investigated. Compared to several characters of Room B, humidity of Room A was lower, and concentration of sesqui-terpenes emitted from Room A were higher. Participants felt more “natural” in Room A. Participant with poor daily sleep quality showed higher morning diastolic pressure only when participants slept in Room B. These results indicate that, high emitting of sesqui-terpenes, high moisture-absorption performance or the combination of them of naturally processed Sugi wood can help people prevent diastolic pressure increasing in the morning caused by low sleep quality.

Language：English   Publishing type：Research paper (scientific journal)  

Skeletal muscle fiber is largely classified into two types: type 1 (slow‐twitch) and type 2 (fast‐twitch) fibers. Meat quality and composition of fiber types are thought to be closely related. Previous research showed that overexpression of constitutively active peroxisome proliferator‐activated receptor (PPAR)δ, a nuclear receptor present in skeletal muscle, increased type 1 fibers in mice. In this study, we found that hexane extracts of Yamabushitake mushroom (Hericium erinaceus) showed PPARδ agonistic activity in vitro. Eight‐week‐old C57BL/6J mice were fed a diet supplemented with 5% (w/w) freeze‐dried Yamabushitake mushroom for 24 hr. After the treatment period, the extensor digitorum longus (EDL) muscles were excised. The Yamabushitake‐supplemented diet up‐regulated the PPARδ target genes Pdk4 and Ucp3 in mouse skeletal muscles in vivo. Furthermore, feeding the Yamabushitake‐supplemented diet to mice for 8 weeks resulted in a significant increase in muscle endurance. These results indicate that Yamabushitake mushroom contains PPARδ agonistic ligands and that dietary intake of Yamabushitake mushroom could activate PPARδ in skeletal muscle of mice. Unexpectedly, we observed no significant alterations in composition of muscle fiber types between the mice fed control and Yamabushitake‐supplemented diets.

DOI： 10.1111/asj.13199

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

This study investigated in vitro the α-glucosidase inhibitory activity of resin from the Sakhalin fir tree (Abies sachalinensis). The resin showed extremely high activity (IC50 of 17.3 µg/mL). We isolated 8 compounds from the resin and identified them. All of the compounds isolated from A. sachalinensis resin are reported for the first time in the present study. In an α-glucosidase inhibitory assay, 6 compounds—(holophyllane C (1), (−) -(24 E)-23-oxo-3,4- seco-9βH-lanosta-4(28),6,8(14),24-tetraen-3,26-dioic acid (2), abiesonic acid (3), (−)-(24 E)-23-oxo-3,4- seco-9β H-lanosta-4(28),7,24-triene-3,26-dioic acid (4), 3,4-seco-4(28),6,8(14),22Z,24-mariesapentaen-26,23-olide-3-oic acid (5), and (−)-abiesonic acid 3-methyl ester (6))—showed high activity (their IC50 values were 25.1, 20.9, 82.4, 20.5, 27.3, and 20.5 µg/mL, respectively). These compounds should contribute to the resin’s α-glucosidase inhibitory activity. From an industrial point of view, these findings provide new data to support that the resin of A. sachalinensis is a rich source of α-glucosidase inhibitors, which are highly valuable for their potential to be developed as functional health foods.

DOI： 10.1177/1934578X19858460

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

This pilot study aims to analyze effects on the
short-term memory and mood of the scent of
bornyl acetate and eucalyptol, two volatile
which are commonly used in many essential
oils. The 44 participants in this study were from
Nagasaki University’s School of Fisheries and
Environmental Sciences (19 male, 25 female),
and ranged in age from 18-20 with a mean
age of 19. Effects on short-term memory by a
memory test and changes in mood by the Profile
of Mood States (POMS) questionnaire were
examined. Results showed that the average
score of females and the combination of males
and females was significantly better in the
room with eucalyptol scent compared to the
unscented room. The scent of eucalyptol was
more effective than bornyl acetate in improving
short-term memory, whereas bornyl acetate
was effective in reducing vigor. This effect was
particularly apparent among female subjects.

Language：English   Publishing type：Research paper (scientific journal)  

DOI： https://doi.org/10.1080/14786419.2019.1616730

Language：English   Publishing type：Research paper (scientific journal)  

This study aimed to reveal chemical components and screen antioxidant activity of methanolic extract of Syzygium
polycephalum stem bark. The chemical components were isolated by using column chromatographic techniques and
determined by spectroscopic methods (UV-Vis, FTIR, MS, and NMR) and comparison with literature data, in which the
antioxidant activity was performed using 2,2’-diphenyl-1-picrylhydrazyl (DPPH). The present investigation resulted in four
compounds involving gallic acid, pinostrobin, 3,4,3’-tri-O-methylellagic acid, and 3,3’-di-O-methylellagic acid. The four
compounds were all in the form of phenolic compounds found from the extract whereas 3,4,3’-tri-O-methylellagic acid and
3,3’-di-O-methylellagic acid were ellagic acid derivatives. The methanolic extract, the four compounds, and vitamin C (as
positive control) showed antioxidant activity against DPPH with the IC50 value of 99.9; 10.0; 183.2; 72.1; 63.3; and 13.9
µg/mL, respectively. The antioxidant activity of gallic acid was more active than that of vitamin C. The present study
confirms that Syzygium polycephalumis rich in phenolic compounds and natural antioxidants.

Language：English   Publishing type：Research paper (scientific journal)  

Lingzhi is a Ganoderma mushroom species which has a wide range of bioactivities. Analysis of the changes in metabolites during the developmental stages of lingzhi is important to understand the underlying mechanism of its biosynthesis, as well as its bioactivity. It may also provide valuable information for the cultivation efficiency of lingzhi. In this study, mass spectrometry based untargeted metabolomics was carried out to analyze the alteration of metabolites during developmental stages of lingzhi. Eight developmental stages were categorized on the basis of morphological changes; starting from mycelium stage to post-mature stage. GC/MS and LC/MS analyses along with multivariate analysis of lingzhi developmental stages were performed. Amino acids, organic acids, sugars, polyols, fatty acids, fatty alcohols, and some small polar metabolites were extracted as marker metabolites from GC/MS analysis, while, lanostane-type triterpenoids were observed in LC/MS analysis of lingzhi. The marker metabolites from untargeted analysis of lingzhi developmental stages were correlated with the α-glucosidase inhibitory activity. Two metabolites, compounds 34 and 35, were identified as potential contributors of the α-glucosidase inhibitory activity. The current result shows that some metabolites are involved in the developmental process and α-glucosidase inhibitory activity of lingzhi.

DOI： 10.3390/molecules24112044.

Language：English   Publishing type：Research paper (scientific journal)  

We examined the association between serum concentrations of β-alanine, a metabolite of carnosine and anserine, and the risk of dementia in a general population of elderly Japanese persons. In 2007, 1,475 residents of Hisayama, Japan, aged 60–79 years and without dementia were divided into 4 groups according to quartiles of serum β-alanine concentrations (quartile 1, lowest; quartile 4, highest) and followed for a median of 5.3 years. During follow-up, 117 subjects developed all-cause dementia (Alzheimer in 77 cases and vascular dementia in 31).The risk of all-cause dementia decreased with increasing serum β-alanine levels after adjustment for potential confounding factors (quartile 2, hazard ratio (HR) = 0.73 (95% confidence interval (CI): 0.45, 1.18); quartile 3, HR =0.50 (95% CI: 0.28, 0.89); quartile 4, HR = 0.50 (95% CI: 0.27, 0.92); P = 0.01 for trend). A similar inverse association was observed for Alzheimer disease (quartile 2, HR = 0.78 (95% CI: 0.44, 1.38); quartile 3, HR = 0.53 (95% CI:0.26, 1.06); quartile 4, HR = 0.53 (95% CI: 0.25, 1.10); P = 0.04 for trend) but not for vascular dementia. We found that higher serum β-alanine levels were significantly associated with lower risks of all-cause dementia and Alzheimer disease. Because serum β-alanine levels reflect intakes of carnosine/anserine, higher intakes of carnosine/anserine might be beneficial for the prevention of dementia.β-alanine; Alzheimer disease; cohort study; dementia; imidazole dipeptides

DOI： 10.1093/aje/kwz116

Language：English   Publishing type：Research paper (scientific journal)  

This article describes the biological activities of heartwood extracts from Yakushima native cedar (Cryptomeria japonica) and identifies their main active compounds. Black heartwood and red heartwood were each divided into two parts from the center (the pith) to outer heartwood (the cambium). The methanol extracts of those parts were screened for antioxidant and anti-lipase activities. The extract from the pith of the red heartwood showed the highest ORAC activity among the samples. Regarding anti-lipase activity, all the extracts showed relatively high activity (the IC50 value were 9.71–37.24 μg mL−1). In addition, four compounds were isolated and identified from the pith of red heartwood by NMR and MS analyses. Agatharesinol (3) and sequirin C (4) were thought to be the main active compounds responsible for the antioxidant and anti-lipase activities.

DOI： https://doi.org/10.1080/02773813.2019.1578806

Language：English   Publishing type：Research paper (scientific journal)  

One of the conventional strategies for treating osteoporosis is to eliminate the multinucleated osteoclasts that are responsible for bone resorption. Our previous study revealed that ursolic acid, isolated from leaves of loquat that is used as tasty tea in Japan, suppressed osteoclastogenesis. We confirmed that ursolic acid exhibited osteoclast differentiation inhibitory activity with an 50% inhibitory concentration (IC50) value of 5.4 ± 0.96 μM. To disclose its mechanism of action, this study first uses polymer-coated magnetic nanobeads to identify potential target proteins. As a result, we identified a nuclear exporter protein named exportin 5 (XPO5). Further studies demonstrated that knockdown of XPO5 significantly blocks osteoclast differentiation (P < 0.01). Expression profiling of mature microRNAs in the cells revealed that downregulation of XPO5 by small interfering RNA or by ursolic acid could downregulate the expression of mature microRNA let-7g-5p during osteoclast differentiation (P < 0.01). Collectively, our findings suggest that ursolic acid inhibits osteoclast differentiation through targeting XPO5, which provides further evidence for the healthy function of the tea. This study also provides new insights into the role of XPO5 and its mediated microRNAs in treatment for bone resorption diseases.

DOI： 10.1021/acs.jafc.8b06954

Language：Japanese   Publishing type：Research paper (scientific journal)  

DOI： 10.1089/jmf.2018.4267

Language：English   Publishing type：Research paper (scientific journal)  

Two new flavonoid glycosides, kaempferol 3-O-α-L-rhamnopyranosyl (1→6) (3′′-acetyl)-β-D-galactopyranoside 1 and kaempferol 3-O-α-L-arabinopyranosyl-5-O-α-L-rhamnopyranoside 2, along with six known ones 3–8 were isolated from the flowers of Vicia faba L. (Fabaceae). Methanol extract and the isolated compounds were tested against lipase and melanogenesis inhibition activities and resulted in that compound 2 showed 53 and 77% lipase inhibition activity in concentrations of 400 and 800 μg/mL, respectively. For melanogenesis, compounds 2, 3 and 4 exhibited potent melanogenesis inhibition activity where the melanin content in melanoma cells was decreased to be about 57.5, 56 and 61%, respectively, with no obvious melanocytotoxicity. The rest of compounds showed weak to moderate activity. The results of melanogenesis inhibition activity of this study suggested the potential use of Vicia faba flowers as a skin-whitening agent and reveal the flowers to be a rich source of important phytochemicals with antilipase and melanogenesis inhibitory activity.

Language：English   Publishing type：Research paper (scientific journal)  

In the present study, ethanol extracts of 90 wild mushroom samples from Nepal, and the pure compound hispidin, were screened for their ability to inhibit β-hexosaminidase release (BHR) from rat basophilic leukemia-2H3 cells. Simultaneously, the toxicity of the extracts toward the cells was also determined, using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Samples belonging to the groups Hymenochaetales and Polyporales showed promising anti-allergic activity, with Phellinus adamantinus and Ganoderma lingzhi 3 allowing a mere 19.4% and 16.7% BHR, respectively, without any cell cytotoxicity. Moreover, the 50% inhibitory concentration (IC50) values for Inonotus clemensiae and P. adamantinus were determined to be 51.24 and 50.65 μg/mL, respectively; whereas hispidin, the major bioactive compound in I. clemensiae showed an IC50 value of 82.47 μg/mL. These findings are crucial in underscoring the medicinal value of the wild mushrooms of Nepal, as a source of strong antiallergic agents.

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.1080/14786419.2018.1440229

Language：English   Publishing type：Research paper (scientific journal)  

In the present study, ethanol extracts of 90 wild mushroom samples from Nepal, and the pure compound hispidin, were screened for their ability to inhibit β-hexosaminidase release (BHR) from rat basophilic leukemia-2H3 cells. Simultaneously, the toxicity of the extracts toward the cells was also determined, using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Samples belonging to the groups Hymenochaetales and Polyporales showed promising anti-allergic activity, with Phellinus adamantinus and Ganoderma lingzhi 3 allowing a mere 19.4% and 16.7% BHR, respectively, without any cell cytotoxicity. Moreover, the 50% inhibitory concentration (IC ₅₀ ) values for Inonotus clemensiae and P. adamantinus were determined to be 51.24 and 50.65 μg/mL, respectively; whereas hispidin, the major bioactive compound in I. clemensiae showed an IC ₅₀ value of 82.47 μg/mL. These findings are crucial in underscoring the medicinal value of the wild mushrooms of Nepal, as a source of strong antiallergic agents.

DOI： 10.1089/jmf.2018.4267

Language：English   Publishing type：Research paper (scientific journal)  

A new simple and robust HPLC-DAD method was developed for the concurrent analysis of hydroquinone (HQ), hydrocortisone acetate (HCA) and tretinoin (TRN) triple combination for the first time using an Inertsil ODS 3-C18 column (150 mm × 4.6 mm, 5 μm particle size) column with 0.05 M phosphate buffer (pH 5.0) and acetonitrile at a ratio of (10:90, v/v) as a mobile phase, eluted by an isocratic elution mode at a flow rate of 1.0 mL/min and detected at 265 nm. Mefenamic acid was used as an internal standard (I.S.). The method produced linear responses in the concentration range of 10-200, 5-100 and 1-40 μg/mL, with detection limits of 2.01, 1.13 and 0.28 × 10-3 and quantitation limits of 6.11, 3.41 and 0.87 × 10-3 μg/mL for HQ, HCA and TRN, respectively, and a correlation coefficient higher than 0.9998. All validation requirements were satisfied by proving its linearity, precision, accuracy, robustness and specificity. The method was extended for application in triple combination cream, HQ/TRN co-formulated cream and HQ and TRN single ingredient cream with a recovery >97%.

Language：English   Publishing type：Research paper (scientific journal)  

Lingzhi is a Ganoderma mushroom species which has a wide range of bioactivities. Analysis of the changes in metabolites during the developmental stages of lingzhi is important to understand the underlying mechanism of its biosynthesis, as well as its bioactivity. It may also provide valuable information for the cultivation efficiency of lingzhi. In this study, mass spectrometry based untargeted metabolomics was carried out to analyze the alteration of metabolites during developmental stages of lingzhi. Eight developmental stages were categorized on the basis of morphological changes; starting from mycelium stage to post-mature stage. GC/MS and LC/MS analyses along with multivariate analysis of lingzhi developmental stages were performed. Amino acids, organic acids, sugars, polyols, fatty acids, fatty alcohols, and some small polar metabolites were extracted as marker metabolites from GC/MS analysis, while, lanostane-type triterpenoids were observed in LC/MS analysis of lingzhi. The marker metabolites from untargeted analysis of lingzhi developmental stages were correlated with the α-glucosidase inhibitory activity. Two metabolites, compounds 34 and 35, were identified as potential contributors of the α-glucosidase inhibitory activity. The current result shows that some metabolites are involved in the developmental process and α-glucosidase inhibitory activity of lingzhi.

DOI： 10.3390/molecules24112044

Language：English   Publishing type：Research paper (scientific journal)  

Hericium erinaceus has been recognized as medical mushroom since ancient time, but its scientific evidence for human health has been still uncertain. In this study, we tested a randomized, double-blind, placebo-controlled parallel-group comparative study to evaluate the improvement of the cognitive functions by taking supplements containing fruiting body of H. erinaceus for 12 weeks. We performed three kinds of tests: Mini Mental State Examination (MMSE), Benton visual retention test, and Standard verbal paired-associate learning test (S-PA). MMSE alone showed that oral intake of H. erinaceus significantly improved cognitive functions and prevented from the deterioration. We speculate that various chemical compounds, including hericenones, in the mushroom have multiple effects to the brain neural networks and improve cognitive functions. Oral intake of H.erinaceus is safe and convenient method for dementia prevention so far.

DOI： 10.2220/biomedres.40.125

Language：English   Publishing type：Research paper (scientific journal)  

Objectives The purpose of this present study was to investigated effect of ginseng-containing tea intake on cognitive performance. (UMIN000034367) Methods Subjects was 40 volunteers, aged between 13 and 18 years, were randomly allocated to either the placebo group, in which subjects consumed placebo tea, or the ginseng group, in which subjects consumed the ginseng-containing tea. The cognitive performances measured by Benton Visual Retention Test (BVRT), Uchida-Kraepelin psychodiagnostic test (UKT) and TK system Tanaka AB style intelligence test that before and after a 4 week. Results There was a significant interaction over 4 weeks in BVRT score and between the ginseng group and the placebo group. Conclusion These results suggest that Panax ginseng containing tea was beneficial in the visual cognitive performance improvement among adolescence.

Language：English   Publishing type：Research paper (scientific journal)  

This article describes the biological activities of heartwood extracts from Yakushima native cedar (Cryptomeria japonica) and identifies their main active compounds. Black heartwood and red heartwood were each divided into two parts from the center (the pith) to outer heartwood (the cambium). The methanol extracts of those parts were screened for antioxidant and anti-lipase activities. The extract from the pith of the red heartwood showed the highest ORAC activity among the samples. Regarding anti-lipase activity, all the extracts showed relatively high activity (the IC
₅₀
value were 9.71–37.24 μg mL
⁻¹
). In addition, four compounds were isolated and identified from the pith of red heartwood by NMR and MS analyses. Agatharesinol (3) and sequirin C (4) were thought to be the main active compounds responsible for the antioxidant and anti-lipase activities.

DOI： 10.1080/02773813.2019.1578806

Language：English   Publishing type：Research paper (scientific journal)  

Lotus root (Nelumbo nucifera) is a popular food in Japan and southeast Asia. It is reported that lotus root includes dietary fiber, vitamin C, and abundant polyphenolic compounds. In Chinese medicine, lotus powder is also utilized in anti-tussive or anti-inflammatory drugs. In this study, we focused on the effects of lotus root powder on allergy symptoms in mice. First, we assessed nasal allergy symptoms in 2,4-diisocyanic acid toluene (TDI)-sensitized nasal allergy model mice. We found that lotus root powder alleviated nasal allergy symptoms in the mice. In addition, we estimated serum inflammatory parameters such as serum total IgE, histamine, and leukotriene B4. Lotus root powder intake significantly decreased serum total IgE and leukotriene B4 compared with standard food intake. We suggest that lotus root powder intake may alleviate allergic symptoms.

DOI： 10.1080/09540105.2019.1651255

Language：English   Publishing type：Research paper (scientific journal)  

A new glucoside, 3-methoxy-4-O-β-D-glucopyranosyl-methyl benzoate, has been isolated from Lycium schweinfurthii along with five known compounds through bioactivity guided fractionation of the total plant methanolic extract towards α-glucosidase inhibitory activity. All the isolated compounds were tested for their inhibitory effect on α-glucosidase enzyme. As a result, four of them showed a potent inhibitory activity and thus constitute a therapeutic approach to decrease postprandial hyperglycemia in diabetic patients.

DOI： 10.1080/14786419.2019.1616730

Language：English   Publishing type：Research paper (scientific journal)  

A new simple and robust HPLC-DAD method was developed for the concurrent analysis of hydroquinone (HQ), hydrocortisone acetate (HCA) and tretinoin (TRN) triple combination for the first time using an Inertsil ODS 3-C18 column (150 mm × 4.6 mm, 5 μm particle size) column with 0.05 M phosphate buffer (pH 5.0) and acetonitrile at a ratio of (10:90, v/v) as a mobile phase, eluted by an isocratic elution mode at a flow rate of 1.0 mL/min and detected at 265 nm. Mefenamic acid was used as an internal standard (I.S.). The method produced linear responses in the concentration range of 10-200, 5-100 and 1-40 μg/mL, with detection limits of 2.01, 1.13 and 0.28 × 10^-3 and quantitation limits of 6.11, 3.41 and 0.87 × 10^-3 μg/mL for HQ, HCA and TRN, respectively, and a correlation coefficient higher than 0.9998. All validation requirements were satisfied by proving its linearity, precision, accuracy, robustness and specificity. The method was extended for application in triple combination cream, HQ/TRN co-formulated cream and HQ and TRN single ingredient cream with a recovery >97%.

DOI： 10.1093/chromsci/bmz020

Language：English   Publishing type：Research paper (scientific journal)  

Two new polyhydroxylated steroids, 3β-acetoxy-gorgost-5α,6β,11α-triol (3) and (23 R) methylergosta-20-ene-3β,5α,6β,17α-tetrol (4), together with three known gorgosteroid compounds, gorgost-3β, 5α,6β,11α- tetrol (1), 11α-acetoxy-gorgost- 3β,5α, 6β- triol (2), and gorgost-5 (E) ene-3-β-ol (5), as well as batyl alcohol (6), were isolated from the Egyptian soft coral Heteroxenia fuscescens. The structures of these compounds were elucidated based on NMR spectroscopic analyses, HR-FAB-MS, and comparisons with published data. The cytotoxic activities of the fractions and compounds were evaluated against MCF-7 cancer cell lines using MTT colorimetric assay. Compounds 2 and 4 showed moderate cytotoxic activity, with IC50 values equal to 33.2 and 25.1 µM, respectively, in comparison with the IC50 of 5-fluorouracil 18.7 µM.

DOI： 10.1080/14786419.2019.1624958.

Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

The genus of Macaranga (Euphorbiacaceae) has 250 species of which 160 species are endemic in Kalimantan and New Guinea. They grow as pioneer trees and are used as traditional medicines in the Asian regions. This experiment concerns cytotoxicity in both cancer and normal cells of their methanol extracts from wood, bark and leaf parts. Some of them have not yet reported its cytotoxic activity in those cell lines. The 21 methanol extracts were prepared from seven Macaranga tree species (Macaranga bancana, Macaranga gigantea, Macaranga hullettii, Macaranga pruinosa, Macaranga tanarius, Macaranga trichocarpa and Macaranga triloba). The MTT assay was used to evaluate cytotoxic activity of extracts in cancer cell lines [human breast cancer (MCF-7), mouse melanoma (B16 melanoma), human colon cancer (HCT116), human cervical adenocarcinoma (HeLa)] and normal cell lines [human normal fibroblast (TIG-1) and normal human dermal fibroblast (NHDF)]. The leaf extracts of M. pruinosa, M. tanarius, M. trichocarpa showed more cytotoxicity than wood and bark in all cancer cell lines. In addition, the 5-fluorouracil was used as a positive control. These findings indicated the extracts from leaves of M. pruinosa, M. tanarius and M. trichocarpa had more potential than wood and bark parts to be developed as anticancer agents.

DOI： 10.1007/s13196-018-0215-4

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

An aliphatic ester of hydroxysalicylic acid (6), reported for the first time from a natural source in addition to five known compounds were isolated from the fermented Carica papaya L. preparation, a commercialized functional food. The known compounds were identified as 5-hydroxymethylfurfuraldehyde (1), trans-caffeic acid (2), butyl 4-hydroxybenzoate (butylparaben) (3), lycopene (4), benzyl isothiocyanate (5). Compounds 1 and 3 were reported for the first time from Papaya fruits through this study. The new compound showed a moderate antioxidant activity and a potent hair growth stimulating activity in vitro.

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Although the various folk medicine uses and the biological activity of Forsskaolea tenacissima L., few chemical constituents of this plant have been reported, this provoked us to make our study. Forsskamide, a new ceramide was isolated from aerial parts of F. tenacissima L. (Urticaceae). The chemical structure was established by different spectroscopic methods (1H, 13C-NMR, HMBC, HSQC, ROESY, FAB-MS and HR-FAB-MS). Forsskamide showed a moderate cytotoxic activity by (MTT) method against human colorectal carcinoma cell line (HCT-116) with IC50 33.25 μM in comparison with 5-fluorouracil IC50 26.42 μM. While, it did not show any activity against human hepatocarcinaoma cell line (HepG-2).

DOI： 10.1080/14786419.2017.1419234

Language：English   Publishing type：Research paper (scientific journal)  

Toxoplasmosis is a worldwide parasitic disease responsible for serious health problems to human. The currently available drugs used for toxoplasmosis treatment showed a limited efficacy and cause serious host toxicity. The in vitro screening for toxoplasmicidal activity of Araucaria heterophylla resin (AHR) extract and its major component 13-epi-cupressic acid (CUP) showed that both AHR (EC50 = 3.90) and CUP (EC50 = 3.69) have high toxoplasmicidal activity in comparison with standard cotrimoxazole (EC50 = 4.28). The antiprotozoal effects of AHR and CUP were investigated against acute and chronic toxoplasmosis using mice models. Two groups of Swiss albino mice were infected by RH Toxoplasma strain intraperitoneally and by Me49 strain orally. Both groups were treated with AHR and CUP in different doses. Their effects were evaluated by survival rate, peritoneal, spleen and liver parasite burdens, brain cyst burden, NO serum level and histopathological lesions. The ultrastructural changes of tachyzoites of acutely infected mice were studied using scanning electron microscopy (SEM). There is an evidence of toxoplasmicidal activity of AHR and CUP in acute and chronic experimental toxoplasmosis. In the acute model, mice treated with AHR and CUP showed prolonged survival rates, a significant decrease in the parasite density in peritoneal lavage and pathological insult in both liver and spleen compared with that of untreated ones. SEM results denote evident morphological alterations of treated tachyzoites. In chronic experimental toxoplasmosis, AHR and CUP treated groups could significantly reduce brain cyst burden by 96.05% and 98.02% respectively. This study indicates that AHR and CUP showed potent toxoplasmicidal activities experimentally and could be used as a potential natural nontoxic agent for treatment of toxoplasmosis.

DOI： 10.1016/j.exppara.2018.10.003. Epub 2018 Oct 16.

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Hydroxyproline (Hyp) is a collagen-specific amino acid formed by post-translational hydroxylation of Pro residues. Various Hyp-containing oligopeptides are transported into the blood at high concentrations after oral ingestion of collagen hydrolysate. Here we investigated the angiotensin-converting enzyme (ACE) inhibitory activity of X-Hyp-Gly-type tripeptides. In an in vitro assay, ginger-degraded collagen hydrolysate enriched with X-Hyp-Gly-type tripeptides dose-dependently inhibited ACE and various synthetic X-Hyp-Gly-type tripeptides showed ACE-inhibitory activity. In particular, strong inhibition was observed for Leu-Hyp-Gly, Ile-Hyp-Gly, and Val-Hyp-Gly with IC₅₀ values of 5.5, 9.4, and 12.8 μM, respectively. Surprisingly, substitution of Hyp with Pro dramatically decreased inhibitory activity of X-Hyp-Gly, indicating that Hyp is important for ACE inhibition. This finding was supported by molecular docking experiments using Leu-Hyp-Gly/Leu-Pro-Gly. We further demonstrated that prolyl hydroxylation significantly enhanced resistance to enzymatic degradation by incubation with mouse plasma. The strong ACE-inhibitory activity and high stability of X-Hyp-Gly-type tripeptides highlight their potential for hypertension control.

DOI： 10.1021/acs.jafc.8b03648

Language：English   Publishing type：Research paper (scientific journal)  

In the present study, we compare the performance of two reversed-phase liquid chromatographic approaches using different eluents either conventional hydro-organic eluent or micellar one for simultaneous estimation of hydrocortisone acetate and pramoxine hydrochloride in presence of their degradants and process-related impurities; hydrocortisone and 4-butoxyphenol, respectively. For conventional reversed-phase liquid chromatography (RPLC), separation of the studied compounds was completed on an Inertsil ODS 3-C18 column (150 mm × 4.6 mm, 5 μm particle size) with a mobile phase consists of 50 mM phosphate buffer (pH 5.0): acetonitrile (50: 50, v/v). For micellar liquid chromatography (MLC), an Eclipse XDB-C8 column (150 mm × 4.6 mm, 5 μm particle size) was chosen for the separation with a green mobile phase consists of 0.15 M sodium dodecyl sulfate, 0.3% triethylamine and 10% n-butanol in 20 mM orthophosphoric acid (pH 5.0). Both methods were extended to analyze hydrocortisone acetate and pramoxine hydrochloride in their co-formulated cream. RPLC was superior to MLC with regard to sensitivity for the estimation of impurities. While, MLC represents an eco-friendly, less hazardous and biodegradable approach. Furthermore, the direct injection of the cream to the system without the need to laborious samples pretreatment, excessive amount of analysis time and/or use of large amount of toxic organic solvents is one of the outstanding advantages of MLC.

DOI： https://doi.org/10.1016/j.jfda.2017.12.008

Language：English   Publishing type：Research paper (scientific journal)  

Mushrooms possess various bioactivities and are used as nutritional supplements and medicinal products. Twenty-nine bioactive components have been extracted recently from mushrooms grown in Nepal. In this study, we evaluated the ability of these mushroom extracts to augment SIRT1, a mammalian SIR2 homologue localized in cytosol and nuclei. We established a system for screening food ingredients that augment the SIRT1 promoter in HaCaT cells, and identified a SIRT1-augmenting mushroom extract (number 28, Trametes versicolor). UVB irradiation induced cellular senescence in HaCaT cells, as evidenced by increased activity and expression of cellular senescence markers including senescence-associated β-galactosidase, p21, p16, phosphorylated p38, and γH2AX. Results clearly showed that the mushroom extract (No. 28) suppressed the ultraviolet B irradiation-induced cellular senescence in HaCaT cells possibly through augmenting SIRT1 expression.

DOI： 10.1007/s10616-018-0229-1

Language：English   Publishing type：Research paper (scientific journal)  

Ganoderma lingzhi is a traditional medicinal mushroom, and its extract contains many bioactive compounds. Triterpenoids and polysaccharides are the primary bioactive components that contribute to its medicinal properties. In this study, we quantified 18 triterpenoids, total triterpenoid content and total polysaccharide content in the ethanol and water extracts of G. lingzhi at different growth stages. Triterpenoids were quantified by liquid chromatograph–tandem mass spectrometry in the multiple-reaction-monitoring mode. Total triterpenoid and total polysaccharide content were determined by colorimetric analysis. The results indicated that the fruit bodies at an early growth stage had a higher content of ganoderic acid A, C2, I and LM2, as well as of ganoderenic acid C and D, than those at a later growth stage. In contrast, ganoderic acid K, TN and T–Q contents were higher in mature fruit bodies (maturation stage). The highest total triterpenoid and total polysaccharide contents were found in fruit bodies before maturity (stipe elongation stage or early stage of pileus formation). Our results provide information which will contribute to the establishment of an efficient cultivation system for G. lingzhi with a higher content of triterpenoids.

Language：English   Publishing type：Research paper (scientific journal)  

Dendrobium crepidatum was one of the sources of Herba Dendrobii, a famous and precious traditional Chinese medicine. Indolizine-type alkaloids are the main characteristic ingredients of D. crepidatum, which possesses a variety of changeable skeletons. In the present study, we found that the total alkaloids of D. crepidatum (TAD) can inhibit the production of nitric oxide (NO) in lipopolysaccharide (LPS)-activated macrophages and showed protective effects against LPS-induced acute lung injury (ALI) in mice through downregulating the TLR4-mediated MyD88/MAPK signaling pathway. Further phytochemical study showed that six previously undescribed indolizine-type compounds, including a racemic mixture (dendrocrepidine A-E) were isolated from TAD. Meanwhile, dendrocrepidine F was separated into a pair of enantiomers by a chiral chromatography, and their absolute configurations were assigned by single-crystal X-ray diffraction analysis. The isomer (−)-dendrocrepidine F showed higher anti-inflammatory effects by inhibiting NO production in LPS-treated macrophages with an IC₅₀ value of 13.3 μM. Taken together, indolizine-type alkaloids are the active components of D. crepidatum through downregulating the TLR4-mediated pathway, indicating some kind of therapy of TAD for ALI treatment.

DOI： 10.1016/j.phytochem.2018.02.006

Language：English   Publishing type：Research paper (scientific journal)  

The labdane diterpene, 13-epi-cupressic acid 1, was isolated from the n-hexane-chloroform extract of Araucaria heterophylla resin. Of the 20 fungi screened for possible transformation, only four showed to produce metabolites including 13, 14, 15-trihydroxy-8(17)-labden-19-oic acid 2, 7α,13-dihydroxy-8(17),14-labdadien-19-oic acid 3,13-epi-cupressic acid β-glucosyl ester 4 and iso-communic acid 5 by Cunninghamilla echiulata NRRL 1382 , Aspergillus restrictus NRRL 2869, Coriolus hirsutus ATCC MYA-828 and Cordyceps sinclairii ATCC 24400, respectively. The identity of the isolated compounds was confirmed using 1D and 2D NMR and MS spectroscopies. Compound 4 is a new metabolite while 5 is first time being produced by biotransformation technique. Compound 3 was proved to be a potent anti-inflammatory agent through selective inhibition of COX-2 enzyme assay.

Language：Japanese   Publishing type：Research paper (scientific journal)  

This study focused on the humidity-control performance of the wooden dwelling spaces, which is related to the habitability. To evaluate the moisture-absorption performance in a condition close to real life, the room temperature and relative humidity were measured in a room using naturally processed sugi （Cryptomeria japonica ） wood boards （Room A） and a room using chemically processed wood materials（Room B）as interior materials while subjects were asleep. The interior materials of Room A were free from chemical processing and those of Room B were comprised of bonded or coated woods.
The results obtained from this study during 2014 and 2015 demonstrated that the Room A showed
higher moisture-absorption performance than the Room B.

Repository Public URL： http://hdl.handle.net/2324/1932323

Language：English   Publishing type：Research paper (scientific journal)  

Based on investigating the relative fluorescence intensity of vancomycin hydrochloride (VCM) in methanol, a simple, highly sensitive, time-saving and specific spectrofluorimetric method was developed and validated. VCM fluorescence was measured at 335 nm when excited at 268 nm. Excellent linearity is obeyed in the concentration range 1–100 ng/mL with a detection limit of 5.94 pg/mL, a quantitation limit of 18.03 pg/mL and a very good correlation coefficient (r = 0.9999). Our method was applied to analyze VCM in pharmaceuticals as well as spiked human plasma. Moreover, VCM stability was studied when exposed to various degradation conditions such as oxidative, alkaline as well as acidic stress. Acidic and alkaline degradation kinetics of VCM was studied for the first time. The degradation follows pseudo-first-order kinetics. The apparent rate constants and half-life times were calculated. The Arrhenius equation was assessed and the activation energies of the degradation were also calculated. The developed method can be easily applied in quality control laboratories due to its sensitivity, specificity, simplicity and low cost.

DOI： 10.1016/j.jfda.2017.06.005

Language：English   Publishing type：Research paper (scientific journal)  

Ganoderma lingzhi is a traditional medicinal mushroom, and its extract contains many bioactive compounds. Triterpenoids and polysaccharides are the primary bioactive components that contribute to its medicinal properties. In this study, we quantified 18 triterpenoids, total triterpenoid content and total polysaccharide content in the ethanol and water extracts of G. lingzhi at different growth stages. Triterpenoids were quantified by liquid chromatograph–tandem mass spectrometry in the multiple-reaction-monitoring mode. Total triterpenoid and total polysaccharide content were determined by colorimetric analysis. The results indicated that the fruit bodies at an early growth stage had a higher content of ganoderic acid A, C2, I and LM2, as well as of ganoderenic acid C and D, than those at a later growth stage. In contrast, ganoderic acid K, TN and T–Q contents were higher in mature fruit bodies (maturation stage). The highest total triterpenoid and total polysaccharide contents were found in fruit bodies before maturity (stipe elongation stage or early stage of pileus formation). Our results provide information which will contribute to the establishment of an efficient cultivation system for G. lingzhi with a higher content of triterpenoids.

DOI： 10.1007/s11418-018-1213-y

Language：English   Publishing type：Research paper (scientific journal)  

Three spectrofluorimetric methods were developed for agomelatine (AGM) determination in commercial tablets. Method A is based on measuring the native fluorescence of AGM aqueous solution at 230/360 nm. Methods B and C are based on the formation of a charge transfer complex between AGM and 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) and 7,7,8,8-tetracyanoquinodimethane (TCNQ) with measurement of the formed fluorophore at 365/475 nm and 250/304 nm, respectively. The relative fluorescence intensity (RFI) of AGM–DDQ complex was greatly enhanced in the presence of methyl-β-cyclodextrin (CD). The methods were linear over the concentration ranges of 0.015–0.5, 0.5–8.0, 0.09–6.0 and 0.05–0.2 μg/ml for AGM-native fluorescence, AGM–DDQ, AGM–DDQ–CD and AGM–TCNQ complexes, respectively with excellent correlation coefficients (r = 0.9999). The methods were validated as per the International Conference on Harmonization (ICH) guidelines and all validation requirements were satisfied. The developed methods were extended to the analysis of AGM in commercial tablets. Furthermore, the stability of AGM was studied under different stress conditions (alkaline, acidic, oxidative and photolytic). The potential alkaline and acidic degradation products were identified by LC–MS/TOF.

DOI： 10.1002/bio.3405

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

DOI： 10.22146/ijc.25467

Language：English   Publishing type：Research paper (scientific journal)  

Liver fibrosis has been emphasized as a serious threat to human health. There is currently no effective clinical drug treatment. Although mogrosides (MGs) have extensive pharmacological effects with minimal toxicity, their effects on liver function, inflammation, matrix metalloproteinases and hepatic stellate cell (HSC) activation remain to be researched. In the current study, we investigated whether mogroside IVE (MGIVE), a main compound isolated from MGs, provided protection against liver fibrosis in mice. MGIVE (25 mg/kg) significantly reduced carbon tetrachloride (CCl₄)-induced inflammatory infiltration, pro-inflammatory cytokine release, and myeloperioxide (MPO) activity, as well as improved liver function in CCl₄-treated mice. Additionally, MGIVE also significantly impaired CCl₄-induced increases in liver fibrotic marker expression, such as collagen type I and hypoxia inducible factor-1α (HIF-1α). Further investigation indicated that the possible molecular target of MGIVE is the toll-like receptor 4 (TLR4)-mediated pathway, and MGIVE treatment significantly prevented CCl₄-induced transforming growth factor-β1 (TGF-β1) overexpression and the phosphorylation of mitogen activated protein kinase (MAPK) in vivo. In vitro tests of HSCs or RAW 264.7 cells challenged with TGF-β1 or lipopolysaccharide (LPS) demonstrated that TLR4 expression partly mediated the anti-fibrotic effects of MGIVE. In conclusion, supplementation with MGIVE may attenuate liver fibrosis through inhibiting the TLR4 signaling pathway, including MyD88 and MAPKs, as well as HIF-1α. MGIVE may act as a therapeutic potential drug for the treatment of liver fibrosis via the TLR4/HIF-1α cohort signaling pathway.

DOI： 10.1016/j.intimp.2017.12.023

Language：English   Publishing type：Research paper (scientific journal)  

A new lanostane-type triterpenoid, lucidumol D (1) was isolated from the fruiting bodies of Ganoderma lingzhi. Its structure was elucidated on the basis of extensive 1D- and 2D-NMR studies as well as mass spectrometry. The cytotoxicity of lucidumol D against proliferation of several cancer cells were assayed by using MTT method and the obtained result suggested selective anti-proliferative and cytotoxic effects against MCF-7, HepG2, HeLa, Caco-2, and HCT-116. In comparison to lucidumol C (2) isolated previously by our group, the structure-activity relationship indicated that carbonyl function at C-11 is necessary to enhance the cytotoxicity.

DOI： 10.1080/14786419.2018.1440229

Language：English   Publishing type：Research paper (scientific journal)  

The plants in the genus Derris have proven to be a rich source of rotenoids, of which cytotoxic effect against cancer cells seem to be pronounced. However, their effect on angiogenesis playing a crucial role in both cancer growth and metastasis has been seldom investigated. This study aimed at investigating the effect of the eight rotenoids ( 1 – 8 ) isolated from Derris trifoliata stems on three cancer cells and angiogenesis. Among them, 12a-hydroxyrotenone ( 2 ) exhibited potent inhibition on both cell growth and migration of HCT116 colon cancer cells. Further, anti-angiogenic assay in an ex vivo model was carried out to determine the effect of the isolated rotenoids on angiogenesis. Results revealed that 12a-hydroxyrotenone ( 2 ) displayed the most potent suppression of microvessel sprouting. The in vitro assay on human umbilical vein endothelial cells was performed to determine whether compound 2 elicits anti-angiogenic effect and its effect was found to occur via suppression of endothelial cells proliferation and tube formation, but not endothelial cells migration. This study provides the first evidence that compound 2 could potently inhibit HCT116 cancer migration and anti-angiogenic activity, demonstrating that 2 might be a potential agent or a lead compound for cancer therapy.

DOI： 10.1055/s-0044-100797

Language：English   Publishing type：Research paper (scientific journal)  

The investigation of the Syzygium polycephalum Miq. (Myrtaceae) aimed to assess the phytochemical contents and antioxidant activity of the chloroform fraction. In this study, the fraction was obtained from methanol extract of S. polycephalum stem bark partitionated by chloroform. An ellagic acid derivative was successively isolated from the chloroform fraction. The molecular structure of isolated compound was elucidated and established as 3,4,3’-tri-O-methylellagic acid through extensive spectroscopic studies including UV-Vis, FTIR, NMR and LC-MS analyses and by comparison with literature data. The finding of the isolated compound is the first time from the plant, although the isolated compound previously have been found in the other Syzygium species such as S. cumini together with ellagic acid and 3,3’-di-O-methylellagic acid. The chloroform fraction, isolated compound, and vitamin C showed antioxidant activity against 2,2’-diphenyl-1-picrylhydrazyl (DPPH) with IC50 value of 163.6, 72.1, and 11.5 μg/mL, respectively.

Language：English   Publishing type：Research paper (scientific journal)  

Background A clinical trial was conducted using 21 healthy adults randomly assigned to a saffron extract group or placebo group in order to confirm the increase of sleep quality by taking saffron extract. Objective To determine the effect of saffron extract on the sleep quality of 21 healthy adults. Trial design A clinical parallel, double-blind, randomized control trial (RCT) was conducted. Subgroups were defined by good sleeper or poor sleeper using a PSQI test for analysis. Method The participants, who gave self-report information, were under a randomized controlled trial (RCT) study designed for all participants receiving the saffron extract (crocin: 0.6mg/day) or placebo. Result There was a significant reduction in score for the Pittsburgh sleep quality index (PSQI) only in the group treated with the saffron extract. In addition, a significant saffron extract effect on daytime dysfunction over 4 weeks was apparent between the extract group and the placebo group in the subjects with poor sleeper at baseline.

Language：English   Publishing type：Research paper (scientific journal)  

We investigated the antioxidant, anti-lipase and anti-dementia activities of peach (Prunus persica (L.) Batsch) fruit and its by-products. The ethanol extracts of branch showed relatively high activity in all biological activities. Then, the extract was fractionated, and eight compounds were isolated from the ethyl acetate fraction. Results showed 4,2',4'-trihydroxy-6'-methoxychalcone 4'-O-β-D-glucopyranoside (5) and quercetin 3-O-β-D-glucopyranoside (7) as newly identified compounds in P. persica. From the biological investigation, it was considered that quercetin 3-O-β-D-glucopyranoside (7) was the main active compound of antioxidant activity. The main active compound of anti-lipase activity in these was oleanolic acid (1). In addition, (+)-4'-O-methylcatechin (4), 4,2',4'- trihydroxy-6'-methoxychalcone 4'-O-β-D-glucopyranoside (5) and ferulic acid (6) were the main active compounds of anti-dementia activity with acetylcholinesterase inhibitory assay. The results obtained suggested that these active compounds from peach branches of P. persica could be exploited as natural antioxidants, anti-lipase and anti-dementia materials in the future.

Language：English   Publishing type：Research paper (scientific journal)  

In the present study, we compare the performance of two reversed-phase liquid chromatographic approaches using different eluents either conventional hydro-organic eluent or micellar one for simultaneous estimation of hydrocortisone acetate and pramoxine hydrochloride in presence of their degradants and process-related impurities; hydrocortisone and 4-butoxyphenol, respectively. For conventional reversed-phase liquid chromatography (RPLC), separation of the studied compounds was completed on an Inertsil ODS 3-C18 column (150 mm × 4.6 mm, 5 μm particle size) with a mobile phase consists of 50 mM phosphate buffer (pH 5.0): acetonitrile (50: 50, v/v). For micellar liquid chromatography (MLC), an Eclipse XDB-C8 column (150 mm × 4.6 mm, 5 μm particle size) was chosen for the separation with a green mobile phase consists of 0.15 M sodium dodecyl sulfate, 0.3% triethylamine and 10% n-butanol in 20 mM orthophosphoric acid (pH 5.0). Both methods were extended to analyze hydrocortisone acetate and pramoxine hydrochloride in their co-formulated cream. RPLC was superior to MLC with regard to sensitivity for the estimation of impurities. While, MLC represents an eco-friendly, less hazardous and biodegradable approach. Furthermore, the direct injection of the cream to the system without the need to laborious samples pretreatment, excessive amount of analysis time and/or use of large amount of toxic organic solvents is one of the outstanding advantages of MLC.

DOI： 10.1016/j.jfda.2017.12.008

Language：English   Publishing type：Research paper (scientific journal)  

Although the various folk medicine uses and the biological activity of Forsskaolea tenacissima L., few chemical constituents of this plant have been reported, this provoked us to make our study. Forsskamide, a new ceramide was isolated from aerial parts of F. tenacissima L. (Urticaceae). The chemical structure was established by different spectroscopic methods (¹H, ¹³C-NMR, HMBC, HSQC, ROESY, FAB-MS and HR-FAB-MS). Forsskamide showed a moderate cytotoxic activity by (MTT) method against human colorectal carcinoma cell line (HCT-116) with IC₅₀ 33.25 μM in comparison with 5-fluorouracil IC₅₀ 26.42 μM. While, it did not show any activity against human hepatocarcinaoma cell line (HepG-2).

DOI： 10.1080/14786419.2017.1419234

Language：English   Publishing type：Research paper (scientific journal)  

An adenine derivative, 9-β-D-glucopyranosyl adenine, reported for the first time from a natural source, in addition to nine known compounds were isolated from the seeds of Coix lacryma-jobi. Their structures were elucidated based on extensive spectroscopic and chemical studies. The isolated compounds and the ethanol extract have been assayed for melanin inhibition using B16-F10 melanoma cell line. The results of our study suggested the potential use of Coix lacryma-jobi seeds as a skin whitening agent and reveal the seeds to be a rich source of important phytochemicals with melanogenesis inhibitory activity. Among the isolated compounds, coixol (2) and 2-O-β-glucopyranosyl-7-methoxy-2H-1,4-benzoxazin-3(4H)-one (8) exhibited potent melanogenesis inhibitory activity with no obvious melanocytotoxicity. The rest of the compounds showed weak to moderate activity.

DOI： 10.1080/14786419.2017.1292270

Language：English   Publishing type：Research paper (scientific journal)  

Due to the highly specific binding between an antibody and its target, superior analytical performances was obtained by immunoassays for phytochemical analysis over conventional chromatographic techniques. Here, we describe a simple method for producing a functional single-chain variable fragment (scFv) antibody against ganoderic acid A (GAA), a pharmacologically active metabolite from Ganoderma lingzhi. The Escherichia coli BL21(DE3) strain produced a large amount of anti-GAA scFv. However, in vitro refolding steps, which partially recovered the reactivity of the scFv, were required. Interestingly, the functional scFv was expressed as a soluble and active form in the cytoplasm of an engineered E. coli SHuffle^® strain. Purified anti-GAA scFv, which yielded 2.56mg from 1L of culture medium, was obtained from simple and inexpensive procedures for expression and purification. The anti-GAA scFv-based indirect competitive enzyme-linked immunosorbent assay (icELISA) exhibited high sensitivity (linearity: 0.078–1.25µg/mL) with precision (CV: ≤6.20%) and reliability (recovery: 100.1–101.8%) for GAA determination. In summary, the approach described here is an inexpensive, simple, and efficient expression system that extends the application of anti-GAA scFv-based immunoassays. In addition, when in vitro refolding steps can be skipped, the cost and complexity of scFv antibody production can be minimized.

Language：English   Publishing type：Research paper (scientific journal)  

Three spectrofluorimetric methods were developed for agomelatine (AGM) determination in commercial tablets. Method A is based on measuring the native fluorescence of AGM aqueous solution at 230/360 nm. Methods B and C are based on the formation of a charge transfer complex between AGM and 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) and 7,7,8,8-tetracyanoquinodimethane (TCNQ) with measurement of the formed fluorophore at 365/475 nm and 250/304 nm, respectively. The relative fluorescence intensity (RFI) of AGM-DDQ complex was greatly enhanced in the presence of methyl-β-cyclodextrin (CD). The methods were linear over the concentration ranges of 0.015-0.5, 0.5-8.0, 0.09-6.0 and 0.05-0.2 μg/ml for AGM-native fluorescence, AGM-DDQ, AGM-DDQ-CD and AGM-TCNQ complexes, respectively with excellent correlation coefficients (r = 0.9999). The methods were validated as per the International Conference on Harmonization (ICH) guidelines and all validation requirements were satisfied. The developed methods were extended to the analysis of AGM in commercial tablets. Furthermore, the stability of AGM was studied under different stress conditions (alkaline, acidic, oxidative and photolytic). The potential alkaline and acidic degradation products were identified by LC-MS/TOF.

Language：English   Publishing type：Research paper (scientific journal)  

The herbs of Polygonum jucundum Lindex. (Polygonaceae) is a traditional Chinese medicine for inflammatory diseases. 2α-Hydroxyl-3β-angeloylcinnamolide (HAC), a drimane-type sesquiterpenoid, was the major active compound of the ethanol extract of P. jucundum which inhibited the production of inflammatory mediators. However, the biological mechanism of HAC for anti-inflammatory activity has not been reported. In the current study, we investigated whether HAC could suppress the production of inflammatory mediators in lipopolysaccharide (LPS)-induced acute lung injury in mice (ALI) through downregulation of Toll-like receptor 4 (TLR4) and activations of mitogen-activated protein kinases (MAPKs) and inducible protein nitric oxide synthase (iNOS). Moreover, our data indicated that HAC inhibits the overexpression of iNOS and TLR4 in LPS-treated RAW264.7, and also inhibits MAPK signal. These findings suggest that HAC shows anti-inflammatory effects in ALI mice through suppressing TLR4-mediated MAPK pathway in activated macrophages. In addition, six derivatives of HAC obtained by structure modification were investigated for their inhibitory effects on the production of nitric oxide (NO) and tumor necrosis factor-α (TNF-α), suggesting that the acetylation could increase the inhibition of HAC on TNF-α release in LPS-treated RAW264.7 cells. In summary, all these results showed that HAC may be a potential anti-inflammatory lead compound for the treatment of acute lung injury.

DOI： 10.1007/s10753-017-0563-z

Language：English   Publishing type：Research paper (scientific journal)  

Two new flavonoid glycosides, kaempferol 3-O-α-L-rhamnopyranosyl (1→6) (3′′-acetyl)-β-D-galactopyranoside 1 and kaempferol 3-O-α-L-arabinopyranosyl-5-O-α-L-rhamnopyranoside 2, along with six known ones 3–8 were isolated from the flowers of Vicia faba L. (Fabaceae). Methanol extract and the isolated compounds were tested against lipase and melanogenesis inhibition activities and resulted in that compound 2 showed 53 and 77% lipase inhibition activity in concentrations of 400 and 800 μg/mL, respectively. For melanogenesis, compounds 2, 3 and 4 exhibited potent melanogenesis inhibition activity where the melanin content in melanoma cells was decreased to be about 57.5, 56 and 61%, respectively, with no obvious melanocytotoxicity. The rest of compounds showed weak to moderate activity. The results of melanogenesis inhibition activity of this study suggested the potential use of Vicia faba flowers as a skin-whitening agent and reveal the flowers to be a rich source of important phytochemicals with antilipase and melanogenesis inhibitory activity.

DOI： 10.1080/14786419.2017.1359169

Language：English   Publishing type：Research paper (scientific journal)  

The present study aims to reveal the antibacterial potential of the wild mushrooms of Nepal. Despite the recognition of the medicinal potential of the natural resources in this country, a systematic study on the bioactivities of the wild mushrooms is still lacking. Therefore, in an attempt to fill this gap, ethanol extracts of 90 Nepalese wild mushroom samples were tested for antibacterial activity against Staphylococcus aureus and Propionibacterium acnes. Staphylococcus aureus was comparatively more susceptible with Inonotus clemensiae exhibiting the least minimum bactericidal concentration (MBC) of 100 μg/mL. The major compound in I. clemensiae was identified to be hispidin using high resolution liquid chromatography–electron spray ionization mass spectrometry (LC–ESI-MS) and nuclear magnetic resonance (NMR) analyses. Furthermore, the minimum inhibitory concentration (MIC) and MBC values of hispidin were determined to be 25 and 100 µg/mL for S. aureus and P. acnes, respectively. These findings show that the Nepalese wild mushrooms have the potential to be a novel addition to the functional ingredients industry due to their strong antibacterial potential.

DOI： 10.1007/s10086-017-1636-1

Language：English   Publishing type：Research paper (scientific journal)  

A new green micellar liquid chromatographic method was developed and validated for the quantitative estimation of nicotinamide (NICO) and clindamycin phosphate (CLD) in bulk and pharmaceutical gel formulation. The analytes are well resolved in less than 6.0 minutes using micellar mobile phase consisting of 0.10M sodium dodecyl sulfate (SDS), 0.3% triethylamine, and 10% 2-propanol in 0.02M orthophosphoric acid at pH 3.0, running through an Eclipse XDB-C₈ column (150 mm × 4.6 mm, 5 μm particle size) with flow rate 1.0 mL/min. The effluent was monitored with diode array detection at 210 nm. The retention times of NICO and CLD were 3.8 minutes and 5.6 minutes, respectively. The method was validated according to the International Conference on Harmonisation (ICH) guidelines in terms of linearity, limit of detection, limit of quantification, accuracy, precision, robustness, and specificity to prove its reliability. Linear correlation was achieved by plotting the peak area of each drug against its concentration. It was found to be rectilinear in the ranges of 1.0–40.0 μg/mL and 0.5–15.0 μg/mL with limits of detection of 0.06 μg/mL and 0.03 μg/mL and limits of quantification of 0.19 μg/mL and 0.09 μg/mL for NICO and CLD, respectively. The method was successfully implemented for the simultaneous determination of the analytes in their bulk powder and combined gel formulation with high % recoveries. The ease of sample treatment facilitates and greatly expedites the treatment with reduced cost and improved accuracy of the procedure.

DOI： 10.1016/j.jfda.2016.09.009

Language：English   Publishing type：Research paper (scientific journal)  

Rho-kinase enzymes are one of the most important targets recently identified in our bodies. Several lines of evidence indicate that these enzymes are involved in many diseases and cellular disorders. ROCK inhibitors may have clinical applications for cancer, hypertension, glaucoma, etc. Our study aims to identify the possible involvement of Rho-kinase inhibition to the multiple biological activities of adlay seeds and provide a rationale for their folkloric medicines. Hence, we evaluated Rho-kinase I and II inhibitory activity of the ethanol extract and 28 compounds derived from the seeds. A molecular docking assay was designed to estimate the binding affinity of the tested compounds with the target enzymes. The results of our study suggest a possible involvement of Rho-kinase inhibition to the multiple biological activities of the seeds. Furthermore, the results obtained with the tested compounds revealed some interesting skeletons as a scaffold for design and development of natural Rho-kinase inhibitors.

DOI： 10.1080/14786419.2017.1354183

Language：English   Publishing type：Research paper (scientific journal)  

Hericium erinaceus (H. erinaceus) improves the symptoms of menopause. In this study, using ovariectomized mice as a model of menopause, we investigated the anti-obesity effect of this mushroom in menopause. Mice fed diets containing H. erinaceus powder showed significant decreases in the amounts of fat tissue, plasma levels of total cholesterol, and leptin. To determine the mechanism, groups of mice were respectively fed a diet containing H. erinaceus powder, a diet containing ethanol extract of H. erinaceus, and a diet containing a residue of the extract. As a result, H. erinaceus powder was found to increase fecal lipid levels in excreted matter. Further in vitro investigation showed that ethanol extract inhibited the activity of lipase, and four lipase-inhibitory compounds were isolated from the extract: hericenone C, hericenone D, hericenone F, and hericenone G. In short, we suggest that H. erinaceus has an anti-obesity effect during menopause because it decreases the ability to absorb lipids.

DOI： 10.1007/s11418-017-1075-8

Language：English   Publishing type：Research paper (scientific journal)  

The consumption of mushroom Ganoderma lingzhi (G. lingzhi) is believed to help people fight influenza. However, few scientific studies, particularly in animals, has addressed that. Here, a hot-water extract of G. lingzhi was orally or intranasally administered to mice infected with influenza A virus, following by a 21-day post-infection observation. An in vitro neuraminidase (NA) assay, with four subtypes of NA, was used to assess inhibition. The total content of triterpenoids and carbohydrates in the extract were determined with colorimetric assays. Results showed that intranasal administration of the extract reduced the severe weight loss in infected mice by 55.1%. Oral administration of the extract did not significantly interfere the virus infection. In addition, the extract strongly inhibited NA from influenza virus H1N1 and H5N1. These findings suggest that short-term oral consumption of hot-water extract of G. lingzhi has limited anti-influenza function, which also inform further research for its activity observed.
霊芝には、古来よりガンを初め、様々な疾病に関する効能が伝承されている。その効能を裏付けようと多くの基礎研究が実施されており、霊芝の薬理活性に関する研究は、近年、劇的に増大している。その薬理活性は、含有されるβ-グルカンに代表される多糖類と、特徴的な構造を有するラノスタン型トリテルペノイド類に由来すると言われている。抗インフルエンザ薬のターゲットして、ノイラミニダーゼ阻害剤が知られている。すでに、我々は、霊芝に含有されるラノスタン型トリテルペノイドのいくつかが、強力にノイラミニダーゼ活性を阻害することを見出している（SciRep2016).
そこで、その効果をin vivoで検証するために、インフルエンザ罹患動物を用いて、その効果を検討したところ、霊芝には、インフルエンザ予防効果を有することが明らかとなった。

DOI： 10.1016/j.jff.2017.04.040

Language：English   Publishing type：Research paper (scientific journal)  

The leaves of loquat (Eriobotrya japonica) possess high medicinal value and have been used as traditional medicines. However, there are no evidence-based studies on the skin-care effects of E. japonica leaves. To explore new biological activities of E. japonica leaves against skin disorder and to gain a better understanding of the chemical components associated with bioactivities, we evaluated 18 triterpenoids from E. japonica leaves on anti-melanogenesis, anti-acne, anti-allergy and anti-aging activities. Our results revealed that eight compounds showed anti-melanogenesis activity, of which ursolic acid (1) and maslinic acid (7) were the most potent with the similar selective index to that of arbutin. Structure–activity relationship and possible mechanism of active compounds were proposed. Twelve compounds exhibited anti-acne effect; ursolic acid (1), maslinic acid (7), corosolic acid (8) and euscaphic acid (12) showed highest activities against P. acnes. Four compounds displayed anti-allergy and anti-inflammatory activity; 3-epicorosolic acid (9) and euscaphic acid (12) showed marked activity against β-hexosaminidase release. Finally, ursolic acid (1), pomolic acid (10), colosolic acid (8) and its methylated derivative (6) exhibited the highest anti-aging activity by stimulating collagen and hyaluronic acid (HA) production. Our findings provide valuable evidence that E. japonica leaves have potential applications as ingredients of function foods or cosmetics for health benefits and a number of triterpenoids may play an important role in these bioactivities.

DOI： 10.3390/ijms18051030

Language：English   Publishing type：Research paper (scientific journal)  

Tubulin polymerization is an important target for anticancer therapies. Even though the potential of Ganoderma triterpenoids against various cancer targets had been well documented, studies on their tubulin polymerization-stimulating activity are scarce. This study was conducted to evaluate the effect of Ganoderma triterpenoids on tubulin polymerization. A total of twenty-four compounds were investigated using an in vitro tubulin polymerization assay. Results showed that most of the studied triterpenoids exhibited microtuble-stabilizing activity to different degrees. Among the investigated compounds, ganoderic acid T-Q, ganoderiol F, ganoderic acid S, ganodermanontriol and ganoderic acid TR were found to have the highest activities. A structure-activity relationship (SAR) analysis was performed. Extensive investigation of the SAR suggests the favorable structural features for the tubulin polymerization-stimulating activity of lanostane triterpenes. These findings would be helpful for further studies on the potential mechanisms of the anticancer activity of Ganoderma triterpenoids and give some indications on the design of tubulin-targeting anticancer agents.

Language：English   Publishing type：Research paper (scientific journal)  

The degranulation of basophils stimulated by antigen is one of the allergic mechanisms of immediate hypersensitivity reactions. In a previous study, the β-hexosaminidase release of rat basophilic leukemia (RBL-2H3) cells stimulated by IgE cross-linking was specifically inhibited by ethanol extract of olive milled waste (OMW). OMW is a potential source of triterpenes, which show several biological activities. However, little is known about the effect of triterpenes in OMW on β-hexosaminidase release. Here we investigated anti-allergic triterpenes from the ethanol extract of OMW, and we discuss the structure–activity relationship. We subjected ethanol extract of OMW to activity-guided fractionation; this led to the isolation of five known triterpenes, i.e., maslinic acid (1), oleanolic acid (2), punicanolic acid (3), 2-O-acetylmaslinic acid (4), and epimaslinic acid (5) as well as one new triterpene, 11-oxo-maslinic acid (6). An anti-allergic assay revealed that 2-O-acetylmaslinic acid (4) and 11-oxo-maslinic acid (6) showed anti-allergic activity. Considering the structure–activity relationship of these triterpenes, it appears that the existence of a ketone group at C-11 or an acetyl group at C-2 would influence the anti-allergic activity.

DOI： 10.1007/s10616-016-0058-z

Language：English   Publishing type：Research paper (scientific journal)  

Tubulin polymerization is an important target for anticancer therapies. Even though the potential of Ganoderma triterpenoids against various cancer targets had been well documented, studies on their tubulin polymerization-stimulating activity are scarce. This study was conducted to evaluate the effect of Ganoderma triterpenoids on tubulin polymerization. A total of twenty-four compounds were investigated using an in vitro tubulin polymerization assay. Results showed that most of the studied triterpenoids exhibited microtuble-stabilizing activity to different degrees. Among the investigated compounds, ganoderic acid T-Q, ganoderiol F, ganoderic acid S, ganodermanontriol and ganoderic acid TR were found to have the highest activities. A structure–activity relationship (SAR) analysis was performed. Extensive investigation of the SAR suggests the favorable structural features for the tubulin polymerization-stimulating activity of lanostane triterpenes. These findings would be helpful for further studies on the potential mechanisms of the anticancer activity of Ganoderma triterpenoids and give some indications on the design of tubulin-targeting anticancer agents.

DOI： 10.1007/s11418-017-1072-y

Language：English   Publishing type：Research paper (scientific journal)  

Recent studies identified Rho-kinase enzymes (ROCK-I and ROCK-II) as important targets that are involved in a variety of diseases. Synthetic Rho-kinase inhibitors have emerged as potential therapeutic agents to treat disorders such as hypertension, stroke, cancer, diabetes, glaucoma, etc. Our study is the first to screen the total ethanol extract of the medicinal mushroom Ganoderma lingzhi with thirty-five compounds for Rho-kinase inhibitory activity. Moreover, a molecular binding experiment was designed to investigate the binding affinity of the compounds at the active sites of Rho-kinase enzymes. The structure–activity relationship analysis was investigated. Our results suggest that the traditional uses of G. lingzhi might be in part due to the ROCK-I and ROCK-II inhibitory potential of this mushroom. Structure–activity relationship studies revealed some interesting features of the lanostane triterpenes that potentiate their Rho-kinase inhibition. These findings would be helpful for further studies on the design of Rho-kinase inhibitors from natural sources and open the door for contributions from other researchers for optimizing the development of natural Rho-kinase inhibitors.

DOI： 10.1007/s11418-016-1069-y

Language：English   Publishing type：Research paper (scientific journal)  

Aldrin and its metabolite dieldrin are persistent organic pollutants that contaminate soil in many parts of the world. Given the potential hazards associated with these pollutants, an efficient degradation method is required. In this study, we investigated the ability of Pleurotus ostreatus to transform aldrin as well as dieldrin in pure liquid cultures. This fungus completely eliminated aldrin in potato dextrose broth (PDB) medium during a 14-day incubation period. Dieldrin was detected as the main metabolite, and 9-hydroxylaldrin and 9-hydroxyldieldrin were less abundant metabolites. The proposed route of aldrin biotransformation is initial metabolism by epoxidation, followed by hydroxylation. The fungus was also capable of degrading dieldrin, a recalcitrant metabolite of aldrin. Approximately 3, 9, and 18% of dieldrin were eliminated by P. ostreatus in low-nitrogen, high-nitrogen, and PDB media, respectively, during a 14-day incubation period. 9-Dihydroxydieldrin was detected as a metabolite in the PDB culture, suggesting that the hydroxylation reaction occurred in the epoxide ring. These results indicate that P. ostreatus has potential applications in the transformation of aldrin as well as dieldrin.

DOI： 10.1007/s00284-016-1184-8

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：English  

Recent studies identified Rho-kinase enzymes (ROCK-I and ROCK-II) as important targets that are involved in a variety of diseases. Synthetic Rho-kinase inhibitors have emerged as potential therapeutic agents to treat disorders such as hypertension, stroke, cancer, diabetes, glaucoma, etc. Our study is the first to screen the total ethanol extract of the medicinal mushroom Ganoderma lingzhi with thirty-five compounds for Rho-kinase inhibitory activity. Moreover, a molecular binding experiment was designed to investigate the binding affinity of the compounds at the active sites of Rho-kinase enzymes. The structure-activity relationship analysis was investigated. Our results suggest that the traditional uses of G. lingzhi might be in part due to the ROCK-I and ROCK-II inhibitory potential of this mushroom. Structure-activity relationship studies revealed some interesting features of the lanostane triterpenes that potentiate their Rho-kinase inhibition. These findings would be helpful for further studies on the design of Rho-kinase inhibitors from natural sources and open the door for contributions from other researchers for optimizing the development of natural Rho-kinase inhibitors.

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：Japanese   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Antioxidant activities of Syzygium polyanthum leaves extracts (methanol, ethyl acetate, dichloromethane and n-hexane) were evaluated by using DPPH (2,2-diphenyl-2-picrylhydrazyl) and ABTS
(2,2’-azinobis (3-ethylbenzothiazole-6-sulfonic acid) methods. The methanol extract showed the highest antioxidant activity of DPPH assay among extract with IC₅₀ value of 44.35 μg/mL. In addition, methanol extract also showed the highest antioxidant activity of ABTS assay among extracts with IC₅₀ value of 17.69 μg/mL. This study indicated that the methanol extract of S. polyanthum leaves is potential as antioxidant.

DOI： 10.22146/ijc.23545

Language：English   Publishing type：Research paper (scientific journal)  

An eco-friendly sensitive, rapid and less hazardous micellar liquid chromatographic method was developed and validated for the simultaneous analysis of ethamsylate (ETM) and mefenamic acid (MFA) in the presence of hydroquinone (HQ) and 2,3-dimethylaniline (DMA) the main impurities of ETM and MFA, respectively. Good chromatographic separation was attained using Eclipse XDBC8 column (150mm × 4.6 mm, 5 μm particle size) adopting UV detection at 300 nm with micellar mobile phase consisting of 0.12M sodium dodecyl sulfate, 0.3% triethylamine and 15% 2- propanol in 0.02M orthophosphoric acid (pH 7.0) at 1.0 mL/min. The analytes were well resolved in <6.0 min, ETM (t_R = 1.55 min), HQ (t_R = 1.95 min), MFA (t_R = 4.55 min) and DMA (t_R = 5.80 min). Different validation parameters were examined as recommended by international conference on harmonization (ICH) guidelines. The method was linear over the concentration ranges of 0.5-18.0, 0.5-20.0, 0.01-0.5 and 0.02-0.2 μg/mL with limits of detection of 0.118, 0.159, 0.005 and 0.005 μg/ mL and limits of quantification of 0.358, 0.482, 0.014 and 0.015 μg/mL for ETM, MFA, HQ and DMA, respectively. The suggested method was successfully applied for the determination of the two drugs in their bulk powder, laboratory-prepared mixtures, single-ingredient and co-formulated tablets. The obtained results were in accordance with those of the comparison method. The method can also detect trace amounts of HQ and DMA as the main impurities of ETM and MFA, respectively, within the BP limit (0.1%) for both impurities. Furthermore, it is a stability-indicating one for the determination of ETM in its pure form, single-component tablet and co-formulated tablets with other drugs.

DOI： 10.1093/chromsci/bmw143

Language：English   Publishing type：Research paper (scientific journal)  

Angelica shikokiana (Apiaceae) is a Japanese traditional herb and widely marketed as a dietary food supplement as a health tea preparation consumed as a daily beverage for its health benefits. Our previous research showed that the methanol extract of the aerial parts of A. shikokiana and its major coumarin, isoepoxypteryxin had a significant cytotoxicity against HepG2 cell line. In this study, we investigated the hepatoprotective activity more deeply by the in vitro inhibition of HepG2 cells invasion assay and in vivo using thioacetamide-induced hepatocellular carcinoma model in rats. The ex vivo levels of nitric oxide production, inducible nitric oxide synthase, vascular endothelial cell growth factor-C and caspase-3 were also estimated to investigate the possible mechanisms of hepatoprotection. The methanol extract of A. shikokiana and isoepoxypteryxin concentration-dependently depressed the invasion of HepG2 cells induced by 12-O-tetradecanoylphorbol 13-acetate. In vivo, they significantly reduced the levels of alanine transaminase, aspartate transaminase, gamma-glutamyl transpeptidase, total bilirubin and nitric oxide production when compared with hepatocellular carcinoma group. Besides, the thioacetamide-injected groups treated with methanol extract of A. shikokiana and isoepoxypteryxin exhibited a significant increase in the level of caspase-3 protein and a significant decrease of inducible nitric oxide synthase and vascular endothelial cell growth factor C levels when compared with hepatocellular carcinoma group. To the best of our knowledge, this is the first report of the hepatoprotective effect of A. shikokiana and isoepoxypteryxin against hepatocellular carcinoma.

DOI： 10.4172/pharmaceutical-sciences.1000265

Language：English   Publishing type：Research paper (scientific journal)  

Angelica shikokiana is a Japanese medicinal plant that is used traditionally in several ailments of cardiovascular diseases. However, there is no report regarding its anticoagulant or antiplatelet activities. So this study was designed to screen for such activities (anticoagulant by prothrombin time [PT], activated partial thromboplastin time, and thrombin time assays and antiplatelet activities against adenosine 5′-diphosphate [ADP] and arachidonic acid-induced platelet aggregations) for the methanol extract of the aerial part (Angelica methanol extract [AME]), its isolated coumarins, flavonoids, and flavonoid metabolites. The AME had potent anticoagulant and antiplatelet activities, and the flavonoid compounds were evidenced to be responsible for such activities. Among coumarins compounds, hyuganin C showed significant prolongation of only PT, while other coumarins were inactive. Similarly, hyuganin C and bergapten were the only active coumarins against ADP-induced platelet aggregation. Compared to the parent compounds, colonic metabolites of the flavonoids had similar anticoagulant and antiplatelet activities, while glucuronides showed sharp decreases in all studied activities. This is the first report showing that the medicinal plant A shikokiana has potent antiplatelet and anticoagulant activities.

DOI： 10.1177/1076029615595879

Language：English  

Leukotriene A4 hydrolase (LTA4H) is a proinflammatory enzyme that generates the inflammatory mediator leukotriene which may play an important role in chronic inflammation associated carcinogenesis. [6]-gingerol, the major bioactive compound of Zingiber officinale, is a potential inhibitor of LTA4H, a highly expressed enzyme in colorectal carcinoma. Eighteen compounds; seven of natural origin (including [4]-, [6]-, [8]-, and [10]-gingerol), five new and six known semi-synthesized [6]-gingerol derivatives were examined using docking, in vitro cytotoxicity against human colon cancer cells (HCT-116) and LTA4H aminopeptidase and epoxide hydrolase inhibitory studies. Methyl shogoal (D8) showed to be the most potent compound against HCT-116 cells (IC50; 1.54μM). Remarkably, D8 proved to be non-cytotoxic to normal cells; (TIG-1) and (HF-19) with high selective index (SI; 52.3). Furthermore [6]-gingerol derivatives showed potent LTA4H inhibitory activities in comparison to the universal positive controls (bestatin and 4BSA). Among the natural gingerols, [10]-gingerol (N3) exhibited the highest LTA4H aminopeptidase and epoxide hydrolase inhibitory activities with IC50; 21.59 and 15.24μM, respectively. Meanwhile, methyl shogoal (D8) and 4'-O-prenyl-[6]-gingerol (D10) retained the highest inhibition with IC50; 4.92 and 3.01μM, for aminopeptidase, and 11.27 and 7.25μM for epoxide hydrolase activities, respectively.

Language：English  

This study describes the chemical investigations of Syzygiumlittorale (S.littorale), a plant
belonging to the family Myrtaceae, and their antioxidant properties. As far, there is no study due to
chemical investigations conducted to the plant either on leaves, fruits, stem bark or the others. The
stem bark of S. littorale was extracted with organic solvent and the extracts were then fractionated
and purified by using standard chromatographic techniques. The molecular structure of pure
isolated pure compound was elucidated and established through extensive spectroscopic studies
and by comparing with literature data and authentic sample. The dried and powdered stem bark of
S. littorale was extracted with methanol and then partitioned by chloroform. Chromatographic
(vacuum liquid chromatography and gravitational column chromatography) fractionation and
purification of the chloroform soluble fraction that is always monitored by TLC yielded a pure
isolated pure compound. The purified compound was then identified and justified as a phenolic
acid i.e. gallic acid. This compound is found for the first time from this plant, although it has
previously been found in other Syzygium species such as S. aromaticum, S. cumini, S. polyanthum,
S. cordatum, etc. The chloroform fraction, isolated compound, and vitamin C showed very strong
antioxidant activity against 2,2‟-diphenyl-1-picrylhydrazyl (DPPH) with the IC50 value of 23.2; 7.5;
and 12.5 ug/mL, respectively.

Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Genus Angelica (Family: Apiaceae) comprises more than 60 species of medicinal plants. Many of these species have long been used in ancient traditional medicine systems, especially in the Eastern countries. For many years, several species of Angelica, e.g., A. archangelica, A. dahurica, A. keiskei, A. gigas, A. pubescens, A. sinensis, A. shikokiana have been used traditionally as anti-inflammatory, diuretic, expectorant, and diaphoretic. Also, these have been used as remedies for hepatitis, arthritis, indigestion, coughs, chronic bronchitis, pleurisy, fever, rheumatism, bacterial and fungal infections, and diseases of the urinary organs. Several classes of compounds such as coumarins, acetylenic compounds, chalcones, sesquiterpenes, and polysaccharides have been reported from these plants. This chapter outlines the results of various scientific studies on Angelica species that were reported to have anticancer and antitumor activities.

Language：English  

BACKGROUND:
Salvia officinalis is a traditionally used herb with a wide range of medicinal applications. Many phytoconstituents have been isolated from S. officinalis, mainly phenolic diterpenes, which possess many biological activities.

PURPOSE:
This study aimed to evaluate the ability of the phenolic diterpenes of S. officinalis to inhibit acetylcholine esterase (AChE) as well as their ability to inhibit melanin biosynthesis in B16 melanoma cells.

METHODS:
The phenolic diterpenes isolated from the aerial parts of S. officinalis were tested for their effect on melanin biosynthesis in B16 melanoma cell lines. They were also tested for their ability to inhibit AChE using Ellman's method. Moreover, a molecular docking experiment was used to investigate the binding affinity of the isolated phenolic diterpenes to the amino acid residues at the active sites of AChE.

RESULTS:
Seven phenolic diterpenes-sageone, 12-methylcarnosol, carnosol, 7b-methoxyrosmanol, 7a-methoxyrosmanol, isorosmanol and epirosmanol-were isolated from the methanolic extract of the aerial parts of S. officinalis. Isorosmanol showed a melanin-inhibiting activity as potent as that of arbutin. Compounds 7a-methoxyrosmanol and isorosmanol inhibited AChE activity by 50% and 65%, respectively, at a concentration of 500 µM.

CONCLUSIONS:
The results suggest that isorosmanol is a promising natural compound for further studies on development of new medications which might be useful in ageing disorders such as the declining of cognitive functions and hyperpigmentation.

Language：English   Publishing type：Research paper (scientific journal)  

Cryptomeria japonica is one of the most important forest tree species in Japan. To increase the demand for domestic timber, broad uses related to the functional attributes of C. japonica must be developed. Several studies have examined the usefulness of C. japonica in terms of its biological activities, but a comprehensive study subjecting all parts of the C. japonica plant to the same solvent for extraction has not been done. Here, methanol extractions from the leaves, branches, bearing branches, male flowers, female flowers, cones, bark, heartwood, sapwood, pith, rhizomes, roots, and pollen were subjected to several in vitro assays of their biological activities such as antioxidant activity, anti-lipase activity, antibacterial activity and melanin-biosynthesis-inhibition activity. Their total phenolic content was also determined. The methanol extracts from each part of C. japonica except for pollen showed strong activities in the bioactivity assays. Furthermore, the methanol extracts were analyzed by GC/MS. The phytochemical profile varied among extracts from various parts of C. japonica. Our results suggest the great potential of C. japonica for use as a functional ingredient in health-related products.

Language：English  

A new green micellar liquid chromatographic method was developed and validated for the quantitative estimation of nicotinamide (NICO) and clindamycin phosphate (CLD) in bulk and pharmaceutical gel formulation. The analytes are well resolved in less than 6.0 minutes using micellar mobile phase consisting of 0.10M sodium dodecyl sulfate (SDS), 0.3% triethylamine, and 10% 2-propanol in 0.02M orthophosphoric acid at pH 3.0, running through an Eclipse XDB-C8 column (150 mm×4.6 mm, 5 μm particle size) with flow rate 1.0 mL/min. The effluent was monitored with diode array detection at 210 nm. The retention times of NICO and CLD were 3.8 minutes and 5.6 minutes, respectively. The method was validated according to the International Conference on Harmonisation (ICH) guidelines in terms of linearity, limit of detection, limit of quantification, accuracy, precision, robustness, and specificity to prove its reliability. Linear correlation was achieved by plotting the peak area of each drug against its concentration. It was found to be rectilinear in the ranges of 1.0-40.0 μg/mL and 0.5-15.0 μg/mL with limits of detection of 0.06 μg/mL and 0.03 μg/mL and limits of quantification of 0.19 μg/mL and 0.09 μg/mL for NICO and CLD, respectively. The method was successfully implemented for the simultaneous determination of the analytes in their bulk powder and combined gel formulation with high % recoveries. The ease of sample treatment facilitates and greatly expedites the treatment with reduced cost and improved accuracy of the procedure.

Language：English  

Further chemical investigation of the metabolites in the fruiting bodies of Ganoderma lingzhi resulted in isolation of eight triterpenes; two of them are new triterpene acid ethyl esters. Their structures were established based on spectroscopic studies and comparison with the known related compounds. The anticancer potential of the isolates were tested with an in vitro cytotoxic assay against five human cancer cell lines (MCF-7, HeLa, HCT-116, Caco-2 and HepG2) and two normal human cell lines (TIG-1 and HF19). Results showed that the new compounds have a strong to moderate selective cytotoxic activity against MCF-7 while they showed moderate to weak activity against HeLa cell line. Potent cytotoxic activities of some of the known isolated compounds are reported for the first time.

Language：English  

Ganoderic acid A (GAA) is one of the major Ganoderma triterpenes produced by medicinal mushroom belonging to the genus Ganoderma (Ganodermataceae). Due to its interesting pharmacological activities, Ganoderma species have been traditionally used in China for the treatment of various diseases. Herein, we developed a colloidal gold-based immunochromatographic strip assay (ICA) for the rapid detection of GAA using highly specific monoclonal antibody against GAA (MAb 12A) conjugated with gold nanoparticles. Using the developed ICA, the detection of GAA can be completed within 15min after dipping the test strip into an analyte solution with the limit of detection (LOD) for GAA of ~500ng/mL. In addition, this system makes it possible to perform a semi-quantitative analysis of GAA in Ganoderma lingzhi, where high reliability was evaluated by enzyme-linked immunosorbent assay (ELISA). The newly developed ICA can potentially be applied to the standardization of Ganoderma using GAA as an index because GAA is major triterpenoid present much in the mushroom.

Language：English   Publishing type：Research paper (scientific journal)  

Moringa oleifera have been evaluated for its antioxidant activity. M. oleifera leaves were extracted with methanol, ethyl acetate, dichloromethane and n-hexane. The antioxidant activity of extracts were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity assay and an improved 2,2’-azino-bis-[3-ethylbenzothiazoline sulphonate] (ABTS) radical cation decolorization assay in vitro. Trolox was used as standard with IC50 5.89 μg/mL in DPPH assay and 3.06 μg/mL in ABTS assay. The methanol extract showed the highest free radical scavenging activity with IC50 value of 49.30 μg/mL in DPPH assay and 11.73 μg/mL in ABTS assay. This study provided that M. oleifera leaves possess antioxidant.

DOI： https://doi.org/10.22146/ijc.21145

Language：English   Publishing type：Research paper (scientific journal)  

Ganoderma lingzhi is one of the most famous medicinal fungi in the world. It has been used in folk medicine, especially in East Asian countries. It is also a white-rot fungus with strong wood degradation ability, especially against lignin. Different classes of bioactive natural products have been reported in Ganoderma, including triterpenes, polysaccharides, sterols, and peptides. The triterpenes and polysaccharides are the primary bioactive compounds of Ganoderma. We report for the first time the presence of 3 methoxyflavones as minor constituents in G. linghzi. The 3 compounds were identified based on different spectroscopic techniques, including 1- and 2-dimensional nuclear magnetic resonance (1H-1H correlation spectroscopy, heteronuclear single quantum coherence, and heteronuclear multiple bond correlation) and mass spectrometry (high-resolution electrospray ionization mass spectrometry). Our report provides an approach to a possible biosynthetic pathway for biosynthetic genes in the mushrooms. Another great possibility is that these compounds may exist or be formed through degradation of the components in the woody substrate, such as lignin, and then subsequently translocate to the fruiting bodies.

Language：English   Publishing type：Research paper (scientific journal)  

A new oxygenated lanostane-type triterpene, named lucidumol C, together with six known compounds, was isolated from the chloroform extract of the fruiting bodies of Ganoderma lingzhi. Structures were established based on extensive spectroscopic and chemical studies. Potential cytotoxic activities of the isolated compounds were evaluated against human colorectal carcinoma (HCT-116, Caco-2), human liver carcinoma (HepG2), and human cervical carcinoma (HeLa) cell lines using WST-1 reagent. Selectivity was evaluated using normal human fibroblast cells (TIG-1 and HF19). Among the compounds, lucidumol C showed potent selective cytotoxicity against HCT-116 cells with an IC50 value of 7.86 ± 4.56 µM and selectivity index (SI) >10 with remarkable cytotoxic activities against Caco-2, HepG2 and HeLa cell lines.

Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Language：English   Publishing type：Research paper (scientific journal)  

Hericium erinaceus (HE), an edible mushroom, has been used as a herbal medicine in several Asian countries since ancient times. HE has potential as a medicine for the treatment and prevention of dementia, a disorder closely linked with circadian rhythm. This study investigated the effects of the intake of HE extracts on behavioral rhythm, photosensitivity of the circadian clock, and clock gene mRNA expression in the suprachiasmatic nucleus (SCN), a central clock, in mice. Although the HE ethanol extract only affected the offset time of activity, the HE water extract advanced the sleep-wake cycle without affecting the free-running period, photosensitivity, or the clock gene mRNA expression in SCN. In addition, both extracts decreased wakefulness around end of active phase. The findings of the present study suggest that HE may serve as a functional food in the prevention and treatment of Alzheimer's disease and delayed sleep phase syndrome.

Language：English   Publishing type：Research paper (scientific journal)  

The isolation and structure elucidation of new phytoceramides from a methanolic extract of the Red Sea sponge Mycale euplectellioides was exclusively studied. Structure elucidation was achieved using spectroscopic techniques, including 1D and 2D NMR and HRMS. The anti-choline esterase activity of the isolated ceramides was evaluated in vitro using a microplate-based Ellman’s assay. Bioassay guided isolation led to the isolation of a MEC-1 phytoceramide molecular species; further purification of MEC-1 afforded three pure phytoceramides: MEC-1-4, MEC-1-7 and MEC-1-8. Molecular modeling studies using glide docking showed tight binding of the ceramides to acetylcholine esterase (AChE). The ceramides showed a better docking score and glide Emodel value when compared to known AChE inhibitors. The ceramides interacted with an aromatic residue of the peripheral anionic site and penetrated deeply into the catalytic triad residues of the active site. Overall, the ceramides obtained using the approaches described here could be considered as promising lead compounds for the discovery and design of potent anti-choline esterase drug candidates, which would be used for Alzheimer’s eradication.

DOI： 10.1039/C5RA26424C

Language：English   Publishing type：Research paper (scientific journal)  

A new, simple isocratic HPLC method was developed and validated for the simultaneous estimation of four vasoactive phytochemicals: ascorbic acid (ASC), rutin (RUT), hesperidin (HSP), and diosmin (DSM) in different pharmaceutical preparations. Separation of the four compounds was achieved in about 8 min on a phenomenex-C18 column (250 mm x 4.6 mm, 5 μm particle size) using a mobile phase consists of 50 mM phosphate buffer (pH 4.0):acetonitrile (75:25, v/v) eluted at 1.0 mL min-1 with diode array detection at 275 nm. Linear correlation was obeyed over the concentration ranges of 2.0-60.0, 1.0-20.0, 2.0-50.0, and 5.0-100.0 μg mL-1 for ASC, RUT, HSP, and DSM, respectively. The developed method is efficient, reproducible and appropriate as a versatile method for quality control of various combinations of these drugs in different pharmaceutical preparations with high values of %recoveries which agreed well with the labeled claim. The method is also a stability-indicating one for DSM in its pure state and single-component tablets. A comparison of the results obtained by the developed method with those of the comparison methods confirmed no significant differences between them with respect to accuracy and precision.

DOI： 10.1039/C5AY03003J

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This article presents multiple potential uses of the Yakushima native cedar (Cryptomeria japonica), known in Japan as the Yaku-sugi tree. The Yaku-sugi was divided into four parts: leaves, branches with leaves, branches, and stems. We obtained the the ess

DOI： DOI:10.1080/02773813.2015.1057648

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DOI： 10.1055/s-0042-104202

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Adipocyte size is closely related to the occurrence of diabetes, metabolic syndrome, and insulin resistance. Thus, researchers are searching for active substances that function to reduce adipocyte size. In the present study, we focused on sugar cane vinegar, Kibizu, and evaluated the function of Kibizu to reduce adipocyte size by using an in vitro model system, because people in Amami Oshima famous for longevity regularly consume Kibizu. Results showed that Kibizu treatment significantly reduced the size and number of lipid droplets in 3T3-L1 cells, relative to treatment with Kurozu, another traditional vinegar. Results of an extraction experiment suggest that the active components in Kibizu are lipophilic and hydrophobic. In addition, an in vivo experiment on rats treated with Kibizu showed that the active components were contained in large vein blood. Results of an additional in vivo experiment suggest that metabolites generated by Kibizu-treated rats are primarily contained or modified specifically in the large vein blood.

DOI： 10.1007/s10616-015-9849-x

Language：Japanese   Publishing type：Research paper (bulletin of university, research institution)  

Language：Japanese   Publishing type：Research paper (bulletin of university, research institution)  

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Angelica shikokiana is a Japanese medicinal plant that is used traditionally in several ailments of cardiovascular diseases. However, there is no report regarding its anticoagulant or antiplatelet activities. So this study was designed to screen for such

DOI： doi: 10.1177/1076029615595879

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DOI： doi:10.1016/j.phytol.2015.04.021

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Abstract Many triterpenoids have shown ability to inhibit hydrolyzing activity of angiotensin-converting enzyme; however, there has been no report about the structure-activity relationship and inhibition patterns of these compounds. In this study, 32 lanostane-type triterpenoids derived from Ganoderma lingzhi were assayed to determine the structural features involved in the observed inhibition effects. In silico and in vitro experiments were also used to determine the kinetics of the reaction. Fifteen compounds showed measurable in vitro IC₅₀ values ranging from 0.194 to 0.941 mM. It was shown that carboxyl groups play an important role in inhibiting the enzyme; further, a hydroxyl group or carbonyl group at either C⁷ or C¹⁵ increases the inhibition rate, and a double bond at C^24,25 decreases the activity. Based on the docking data we speculated that triterpenoids could not fit into the active site of the enzyme; therefore, the inhibition mode could not be competitive. Dixon plotting showed that the inhibition patterns should be uncompetitive and non-competitive instead.

DOI： 10.1016/j.phytol.2015.04.021

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DOI： DOI: 10.1002/ptr.5326

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DOI： e0128358

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Neuraminidase (NA) inhibitors are the dominant antiviral drugs for treating influenza in the clinic. Increasing prevalence of drug resistance makes the discovery of new NA inhibitors a high priority. Thirty-one triterpenoids from the medicinal mushroom Ga

DOI： DOI: 10.1038/srep13194.

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Our previous results elucidated that the leaves of Eriobotrya japonica possessed the potential to suppress ovariectomy-induced bone mineral density deterioration, and ursolic acid, the major bioactive component in these leaves, suppressed the osteoclast differentiation. The aim of this study was to discover more candidates for development of novel antiosteoclastogenesis agents from the leaves of E. japonica. Phytochemical analysis following a cell-based osteoclastic tartrate-resistant acid phosphatase (TRAP) activity assay revealed 11 more compounds with a potent antiosteoclastogenesis effect. The potency of ursane-type triterpenoids from the leaves of E. japonica prompted us to investigate the structure-activity relationships underlying their antiosteoclastogenesis. The results revealed that both the hydroxyl group at C-3 and the carboxylic group at C-17 played indispensable roles in the antiosteoclastogenesis activity of ursane-type triterpenoids. The configuration at C-3 (a beta-form of the hydroxyl group) was found to be important for this activity. While introducing a hydroxyl group at C-19 increased the inhibitory activity of ursane-type triterpenoids carrying an alpha-form hydroxyl group at C-3. The bioactivity analyses of ursolic acid and oleanolic acid demonstrated that the antiosteoclastogenesis effect of ursolic acid may be related to different positions of the C-29 and C-30 methyl groups on the E-ring, since oleanolic acid showed limited activity. The addition of a hydroxyl group at C-2 would dramatically improve the inhibition of oleanane-type triterpenoids. Collectively, these findings could provide important clues for the improvement of multi-targeted antiosteoclastogenesis agents from the leaves of E. japonica.

DOI： 10.1016/j.phymed.2015.03.002

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DOI： 10.3390/molecules20034813

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Bioethanol production through integrated fungal fermentation (IFF), involving a unified process for biological delignification with consolidated biological processing by the white-rot fungus Phlebia sp. MG-60, was applied to sugarcane bagasse. Initial moisture content of the bagasse was found to affect biological delignification by MG-60, and 75% moisture content was suitable for selective lignin degradation and subsequent ethanol production. Additives, such as basal media, organic compounds, or minerals, also affected biological delignification of bagasse by MG-60. Basal medium addition improved both delignification and ethanol production. Some inorganic chemical factors, such as Fe2+, Mn2+, or Cu2+, reduced bagasse carbohydrate degradation by MG-60 during delignifying incubations and resulted in increased ethanol production. The present results indicated that suitable culture conditions could significantly improve IFF efficiency.

DOI： https://doi.org/10.1016/j.biortech.2014.05.064

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DOI： 10.1016/j.bmcl.2014.08.009

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DOI： doi:10.3390/molecules190913473

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DOI： 10.3390/molecules19068238

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DOI： doi: 10.1021/jf402735u

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The loquat, Eriobotrya japonica Lindl. (Rosaceae), is a small tree native to Japan and China that is widely cultivated for its succulent fruit. Its leaves are used as an ingredient of a tasty tea called “Biwa cha” in Japanese. The anti-osteoporosis effects of the leaves of loquat in vitro and in vivo have been investigated. After 15 days of feeding normal diet or diet supplemented with 5% loquat leaves, the body weight, viscera weights, and bone mineral density (BMD) of both groups of eight ovariectomized (OVX) mice were compared. The result showed that the loss of BMD in loquat-fed mice was significantly prevented in three parts of the body, especially in the trabecular bone of the head (P < 0.05), abdomen (P < 0.01), and lumbar (P < 0.05) compared to the control group. No hypertrophy in the uterus by the loquat leaves diet was observed. The effect of the extract (447.25 g) prepared from the dried leaves of loquat (2.36 kg) was further studied on RANKL-induced osteoclast differentiation and cell viability. The extract suppressed the differentiation of osteoclasts under 50, 125, 250, and 500 μg/mL. Through bioactivity-guided fractionation, ursolic acid (1) was isolated and inhibited osteoclast differentiation under 4 and 10 μg/mL. It was concluded that loquat leaves possess the potential to suppress ovariectomy-induced bone mineral density deterioration.

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Twenty-nine mushrooms collected in the mountainous areas of Nepal were analyzed for antioxidant activity by different methods, including Folin-Ciocalteu, ORAC, ABTS, and DPPH assays. Intracellular H2O2-scavenging activity was also performed on HaCaT cells. The results showed that phenolic compounds are the main antioxidant of the mushrooms. Among studied samples, Inonotus andersonii, and Phellinus gilvus exhibited very high antioxidant activity with the phenolic contents up to 310.8 and 258.7 mg GAE/g extracts, respectively. The H2O2-scavenging assay on cells also revealed the potential of these mushrooms in the prevention of oxidative stress. In term of ACE-inhibition, results showed that Phlebia tremellosa would be a novel and promising candidate for antihypertensive studies. This mushroom exhibited even higher in vitro ACE-inhibition activity than Ganoderma lingzhi, with the IC50 values of the two mushrooms being 32 μg/mL and 2 μg/mL, respectively. This is the first time biological activities of mushrooms collected in Nepal were reported. Information from this study should be a valuable reference for future studies on antioxidant and ACE-inhibitory activities of mushrooms.

DOI： http://dx.doi.org/10.1155/2014/195305

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DOI： doi: 10.1016/j.bmc.2013.11.034.

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DOI： 10.1016/j.bmcl.2013.08.084

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DOI： doi:10.3390/molecules181113823

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DOI： Volume 2014 (2014), Article ID 195305, 11 pages http://dx.doi.org/10.1155/2014/195305

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DOI： doi:10.1038/protex.2013.051

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DOI： 10.1007/s10086-012-1310-6

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霊芝には、古来よりガンを初め、様々な疾病に関する効能が伝承されている。その効能を裏付けようと多くの基礎研究が実施されており、霊芝の薬理活性に関する研究は、近年、劇的に増大している。その薬理活性は、含有されるβ-グルカンに代表される多糖類と、特徴的な構造を有するラノスタン型トリテルペノイド類に由来すると言われている。候補者は、霊芝の前立腺肥大症や骨粗鬆症に関する改善効果を見いだし、その活性成分の一つとして、ラノスタン型トリテルペノイド類に属するganoderic acid DMを単離した。本化合物は、5α-リダクターゼ阻害活性、男性ホルモン受容体結合活性、破骨細胞分化抑制効果、ガン細胞増殖抑制効果を示した。本化合物の作用機構の本質に迫るべく、細胞培養系での挙動並びに、構造活性相関を検討し、本知見を元に、ganoderic acid DM結合磁性プローブを用いて標的タンパク質の探索を行ったところ、微小管形成において重要な役割を担うタンパク質であるチューブリンと特異的に相互作用することを見いだした。さらに、同化合物は、チューブリンの重合を促進させ、微小管を不安定化させることにより、細胞の増殖・機能に影響を与えることを明らかにした。以上、霊芝由来トリテルペノイドの生理活性発現に関する新規メカニズムを提案した。

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A large quantity of quercetin was characterized from a local dish, known as maniçoba in Pará, Brazil. The fresh leaf of Manihot esculenta Crantz (Euphorbiaceae), a principal ingredient for maniçoba, was found to contain a large amount of rutin or quercetin 3-O-rutinoside which was completely hydrolyzed to quercetin during cooking processes. Antioxidant activity of quercetin and its microfloral metabolites was examined. Quercetin inhibited the oxidation of linoleic acid catalyzed by soybean lipoxygenase-1 (EC 1.13.11.12, Type 1) with an IC₅₀of 4.5 μM, while rutin did not inhibit this oxidation up to 200 μM. The progress curves for the enzyme reaction indicate that quercetin shows slow binding kinetics. In the pseudoperoxidase activity, hydroperoxides slowly oxidize quercetin to a rather stable intermediate,
2-(3,4-dihydroxybenzoyl)-2,4,6-trihydroxy-3(2H)-benzofuranone. A microfloral metabolite of quercetin and rutin after ingestion, 3,4-dihydroxyphenylacetic acid, also scavenged superoxide anion generated by xanthine oxidase and inhibited uric acid formation. The antioxidant activity observed with the methanol extract of maniçoba is due mainly to multifunctional quercetin's response.

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Artocarpus plants have been a focus of constant attention due to the potential for skin whitening agents. In the in vitro experiment, compounds from the Artocarpus plants, such as artocarpanone, norartocarpetin, artocarpesin, artogomezianol, andalasin, artocarbene, and chlorophorin showed tyrosinase inhibitory activity. Structure-activity investigations revealed that the 4-substituted resorcinol moiety in these compounds was responsible for their potent inhibitory activities on tyrosinase. In the in vitro assay, using B16 melanoma cells, the prenylated polyphenols isolated from Artocarpus plants, such as artocarpin, cudraflavone C, 6-prenylapigenin, kuwanon C, norartocarpin, albanin A, cudraflavone B, and brosimone I showed potent inhibitory activity on melanin formation. Structure-activity investigations revealed that the introduction of an isoprenoid moiety to a non-isoprenoid-substituted polyphenol enhanced the inhibitory activity of melanin production in B16 melanoma cells. In the in vivo investigation, the extract of the wood of Artocarpus incisus and a representative isolated compound from it, artocarpin had a lightening effect on the skin of guinea pigs’ backs. Other in vivo experiments using human volunteers have shown that water extract of Artocarpus lakoocha reduced the melanin formation in the skin of volunteers. These results indicate that the extracts of Artocarpus plants are potential sources for skin whitening agents.

DOI： https://doi.org/10.1177/1934578X1100600943

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月桂樹（Laurus nobilis L.）の葉を乾燥させたものは、香辛料として広く使用されている。また、葉から水蒸気蒸留により得られた精油も、食品の香り付けや薬、化粧品などにも使われる。月桂樹葉は、抗けいれん作用や抗炎症作用、抗菌活性、抗酸化活性など多岐にわたる生理活性を有することが知られている。さらにリウマチや神経痛、疥癬に効くとされ、ゴキブリ忌避作用や鎮静、麻酔作用なども知られている。本研究では、月桂樹葉揮発成分によるビジランス作業効率への影響について検討した。月桂樹葉の供試量を二段階（低濃度群と高濃度群）に設定し、清浄空気を対照とした三条件で、作業効率と生理心理学的な効果について比較した。低濃度の月桂樹葉揮発成分を吸入することによって、正答率の低下抑制に寄与することが分かった。さらに高濃度群では、吸入によりネガティブ感情を引き起こす可能性が示唆された。低濃度と高濃度群ではともに、心血管系循環促進が示唆され、覚醒状態は維持されていたことが分かった。これらの知見から、低濃度の月桂樹葉揮発成分には、感情への負の影響を引き起こすことなく、生理学的な覚醒状態の維持に寄与し、正答率の低下抑制というビジランス維持の機能を持つことが示唆された。

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The aim was to investigate the extent of reduction of ammonia emissions from poultry manure by utilizing cedar bark, which occurs plentifully from timber trimming facilities and has an ability to adsorb ammonia. In a laboratory scale study, cedar bark meal was contacted with an ammonia concentration of 620 ppm in Tedlar bags for 5 minutes. The result showed that the bark reduced ammonia by 99.5%. This study compiled data on ammonia above poultry manure covered with cedar saw dust or cedar bark during a period of 3 weeks. The results indicated that both types of covering agents achieved significant reductions in ammonia concentrations. The adsorption of ammonia was 11 mg-g-1 and 33 mg-g-1 for saw dust and bark respectively. Water-soluble nitrogen, ionic nitrogen, and organic nitrogen accounted for 22%, 23% and 47%, respectively, of increased nitrogen in the bark during composting. It suggested that the increase in ionic nitrogen was due to the higher cation exchange capacity. The increase in organic nitrogen may be attributed to covalent bonds. The results showed that the reduction in the emission of ammonia appears to be caused by the bark cover acting as an inexpensive and simple deodorizer.

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