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    题名: Novel Potent Hypoglycemic Compounds from Euonymus laxiflorus Champ. and Their Effect on Reducing Plasma Glucose in an ICR Mouse Model
    作者: Nguyen, Van Bon;Wang, San-Lang;Nguyen, Thi Hanh;Nguyen, Minh Trung;Doan, Chien Thang;Ngoc, Thi;Lin, Zhi-Hu;Nguyen, Quang Vinh;Kuo, Yao-Haur;Nguyen, Anh Dzung
    关键词: Euonymus laxiflorus Champ.;diabetes;α-glucosidase inhibitors;plasma glucose;condensed tannins;natural products
    日期: 2018-08
    上传时间: 2018-08-15 12:10:13 (UTC+8)
    出版者: MDPI
    摘要: 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.
    關聯: Molecules 23(8), pii: E1928
    DOI: 10.3390/molecules23081928
    显示于类别:[化學學系暨研究所] 期刊論文


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