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从景天三七中提取潜在的α-葡萄糖苷酶抑制剂。

Potential α-glucosidase inhibitor from Hylotelephium erythrostictum.

机构信息

College of Pharmacy, Yanbian University, Yanji 133002, PR China.

Analysis and Inspection Center, Yanbian University, Yanji 133002, PR China.

出版信息

Bioorg Med Chem Lett. 2020 Dec 15;30(24):127665. doi: 10.1016/j.bmcl.2020.127665. Epub 2020 Nov 2.

Abstract

In light of the adequate sources for Hylotelephium erythrostictum, its active components have aroused research interest. 2-(3',4'-dihydroxyphenyl)-2,3-dihydro-4,6-dihydroxy-2-(methoxy)- 3-benzofuranone(1), apigenin(2), diosmetin(3), kaempferol(4), kaempferide(5), rhamnocitrin(6), quercetin(7), and gallic acid(8) were isolated from H. erythrostictum. Rarely occurring naturally, 1 is 2-methoxybenzofuranone type compound against α-glucosidase and exhibits a potential inhibitory effect on α-glucosidase(IC = 1.8 μM), with a Ki value of 709 nM. In silico molecular docking was performed for the investigation of the inhibition mechanism. H. erythrostictum is a potential source of antidiabetic agent. This information is useful in finding more potent antidiabetic candidates from medicinal plants for the clinical development of therapeutics.

摘要

鉴于红景天有充足的来源,其活性成分引起了研究兴趣。从红景天中分离得到了 2-(3',4'-二羟基苯基)-2,3-二氢-4,6-二羟基-2-(甲氧基)-3-苯并呋喃酮(1)、芹菜素(2)、香叶木素(3)、山柰酚(4)、山柰酚-3-O-葡萄糖苷(5)、鼠李柠檬素(6)、槲皮素(7)和没食子酸(8)。1 是一种罕见的天然存在的 2-甲氧基苯并呋喃酮类化合物,对α-葡萄糖苷酶具有潜在的抑制作用,对α-葡萄糖苷酶的抑制活性(IC=1.8μM),Ki 值为 709nM。通过计算机分子对接研究了抑制机制。红景天是一种有潜力的抗糖尿病药物来源。这一信息有助于从药用植物中寻找更有效的抗糖尿病候选药物,为治疗学的临床发展提供帮助。

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