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?±-Glucosidase and pancreatic lipase inhibitory activities and glucose uptake stimulatory effect of phenolic compounds from Dendrobium formosum

机译:铁皮石end中酚类化合物对α-葡萄糖苷酶和胰脂肪酶的抑制活性及葡萄糖摄取的刺激作用

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A methanol extract from the whole plant of Dendrobium formosum Roxb. ex Lindl., Orchidaceae, showed inhibitory potential against ?±-glucosidase and pancreatic lipase enzymes. Chromatographic separation of the extract resulted in the isolation of twelve phenolic compounds. The structures of these compounds were determined through analysis of NMR and HR-ESI-MS data. All of the isolates were evaluated for their ?±-glucosidase and pancreatic lipase inhibitory activities, as well as glucose uptake stimulatory effect. Among the isolates, 5-methoxy-7-hydroxy-9,10-dihydro-1,4-phenanthrenequinone ( 12 ) showed the highest ?±-glucosidase and pancreatic lipase inhibitory effects with an IC 50 values of 126.88 ?± 0.66 ?μM and 69.45 ?± 10.14 ?μM, respectively. An enzyme kinetics study was conducted by the Lineweaver-Burk plot method. The kinetics studies revealed that compound 12 was a non-competitive inhibitor of ?±-glucosidase and pancreatic lipase enzymes. Moreover, lusianthridin at 1 and 10 ?μg/ml and moscatilin at 100 ?μg/ml showed glucose uptake stimulatory effect without toxicity on L6 myotubes. This study is the first report on the phytochemical constituents and anti-diabetic and anti-obesity activities of D. formosum .
机译:从石for石the整个植物中提取甲醇。兰科的前林德公司显示出对β±葡糖苷酶和胰脂肪酶的抑制潜能。萃取物进行色谱分离,分离出十二种酚类化合物。这些化合物的结构是通过NMR和HR-ESI-MS数据分析确定的。评价所有分离物的α±葡萄糖苷酶和胰脂肪酶抑制活性,以及​​葡萄糖摄取刺激作用。在分离物中,5-甲氧基-7-羟基-9,10-二氢-1,4-菲醌(12)表现出最高的α±-葡萄糖苷酶和胰脂肪酶抑制作用,IC 50值为126.88±±0.66μM。和69.45Ω±10.14μM。酶动力学研究通过Lineweaver-Burk图法进行。动力学研究表明,化合物12是β-葡糖苷酶和胰脂肪酶的非竞争性抑制剂。此外,1和10?μg/ ml的卢甜菊酯和100?μg/ ml的莫卡替林显示出对L6肌管无毒性的葡萄糖摄取刺激作用。这项研究是有关福寿螺的植物化学成分以及抗糖尿病和抗肥胖活性的首次报道。

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