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Medicinal Chemistry 2020-Nov

Potential α-glucosidase inhibitor from Hylotelephium erythrostictum

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Yin-Sheng Quan
Xiao-Yong Zhang
Xiu-Mei Yin
Si-Hong Wang
Li-Li Jin

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抽象

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(IC50 = 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.

Keywords: 2-(methoxy)-3-benzofuranone; Hylotelephium erythrostictum; In silico molecular docking; antidiabetic candidate; α-glucosidase inhibitor.

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