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    Title: Novel Potent Hypoglycemic Compounds from Euonymus laxiflorus Champ. and Their Effect on Reducing Plasma Glucose in an ICR Mouse Model
    Authors: Van Bon Nguyen;San-Lang Wang;Thi Hanh Nguyen;Minh Trung Nguyen;Chien Thang Doan;Thi Ngoc;Zhi-Hu Lin;Quang Vinh Nguyen;Yao-Haur Kuo;Anh Dzung Nguyen
    Keywords: Euonymus laxiflorus Champ.;diabetes;α-glucosidase inhibitors;plasma glucose;condensed tannins;natural products
    Date: 2018-08
    Issue Date: 2018-08-15 12:10:13 (UTC+8)
    Publisher: MDPI
    Abstract: α-Glucosidase inhibitors (aGIs) have been used as an effective therapy for type-2 diabetes, which remains a global health issue. The aim of this study was to achieve bioactivity-guided isolation, identification and evaluation of hypoglycemic compounds from Euonymus laxiflorus Champ. trunk bark (ELCTB). Eleven active compounds were isolated and identified as walterolactone A/B β-d-pyranoglucoside (1), 1-β-d-glucopyranosyloxy-3,5-dimethoxy-4-hydroxybenzene (9), (−)-gallocatechin (10), schweinfurthinol 9-O-β-d-pyranoglucoside (11), 1-O-(3-methyl)-butenoyl-myo-inositol (12), leonuriside (14), (+)-catechin (19), methyl galloate (20), (−)-catechin (23), and condensed tannins (5 and 18). Of these 11, novel 4 compounds (1, 11, 12, and 14) were found as new α-glucosidase inhibitors. Notably, in vitro results indicated that compounds 1, 5, 10–12, 18, and 19 showed potent activity (IC50 = 0.076−31 µg/mL), and their activities were at a higher level than that of acarbose, a commercial inhibitor (IC50 = 1345 µg/mL). In animal tests, the major inhibitor, condensed tannin (18), demonstrated significant reduction of plasma glucose in mice with no symptoms of diarrhea at the dose of 100 mg/kg bw. The results suggest that Euonymus laxiflorus Champ. is a rich source of bioactive compounds for development as health food or drugs with potent hypoglycemic effect. The results of this study also enriched the current novel biological activities of constituents from Euonymus laxiflorus species.
    Relation: Molecules 23(8), 1928
    DOI: 10.3390/molecules23081928
    Appears in Collections:[Graduate Institute & Department of Chemistry] Journal Article

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