Dimeric styrylpyrones with stimulating GLP-1 secretion activities from Alpinia kwangsiensis

文献类型： 外文期刊

第一作者： Wu, Meng-Zhen

作者： Wu, Meng-Zhen;Li, Jia;GongPan, Pian-Chou;Sun, Peng;Xiao, Chun-Fen;Ji, Kai-Long;Wu, Meng-Zhen;Li, Jia;Sun, Yi-Li;Dai, Meng -Yuan;Li, Jia;Sun, Yi-Li

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关键词： Glucagon-like peptide-1; Type 2 diabetes; Alpinia kwangsiensis; Dimeric styrylpyrones

期刊名称：TETRAHEDRON （ 影响因子：2.388； 五年影响因子：2.134 ）

ISSN： 0040-4020

年卷期： 2022 年 120 卷

页码：

收录情况： SCI

摘要： Stimulating glucagon-like peptide-1 (GLP-1) secretion is an important approach for the treatment of type 2 diabetes. Chemical investigation of Alpinia kwangsiensis rhizomes produced six dimeric styrylpyrones (1-6), including two new degraded ones (1 and 2). Compounds 1-4 were identified as four pairs of enantiomers and successfully prepared by chiral HPLC separation. These compounds incorporate the distinctive cyclobutane moiety via [2 + 2] cycloaddition, a key step in the biosynthetic pathway. The bioactivities of isolates in stimulating GLP-1 secretion in STC-1 cells were evaluated. Results showed that compounds (+)-1, (+)-2, (-)-2, (-)-4, 5 and 6 significantly increased GLP-1 secretion, and compound (+)-1 exhibited the strongest activity with EC50 value of 6.51 mM. In addition, compounds (+)-2, (-)-4 and 5 promoted GLP-1 secretion by increasing intracellular calcium concentration dependent on the PKA pathway, which could provide a chemical basis for the development of diabetes drugs especially that directly promote GLP-1 secretion.

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