Astragalin Exerted Hypoglycemic Effect by Both Inhibiting α-Glucosidase and Modulating AMPK Signaling Pathway

文献类型： 外文期刊

第一作者： Li, Qian

作者： Li, Qian;Yang, Zhangchang;Liu, Fan;Zhou, Donglai;Zou, Yuxiao;Li, Qian;Zou, Yuxiao;Yang, Zhangchang;Zou, Yuxiao;Lu, Huijie

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关键词： astragalin; alpha-glucosidase; inhibitory mechanism; molecular docking; AMPK pathway

期刊名称：NUTRIENTS （ 影响因子：5.0； 五年影响因子：6.0 ）

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年卷期： 2025 年 17 卷 3 期

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收录情况： SCI

摘要： Background: The hypoglycemic activity of mulberry leaf polyphenols has been widely studied, while its mechanism of action needs further elucidation. Methods: The inhibitory activity mechanism of astragalin on alpha-glucosidase was investigated with a combination of multispectroscopic techniques and molecular docking. The hypoglycemic pathway was further revealed with a high-glucose human hepatocellular carcinomas (HepG2) cell model. Results: The results indicated that astragalin inhibited alpha-glucosidase with IC50 of 154.5 mu M, which was the highest in potency among the main polyphenols from mulberry leaves. Astragalin could bind to alpha-glucosidase with a single inhibition site and quench its endofluorescence with a static quenching mechanism. Astragalin changed the secondary structure of alpha-glucosidase, and the decreased alpha-helix content, representing the un-folding conformation, resulted in the decreased activity. The molecular docking further indicated that two sustainable hydrogen bonds were generated between astragalin and alpha-glucosidase residue Ser-88 and Tyr-133. The main driving forces to form the astragalin-alpha-glucosidase complex were the van der Waals force and hydrogen bond. Astragalin at a concentration of 80 mu g/mL obtained the best hypoglycemic effect by activating the Adenosine 5 '-monophosphate (AMP)-activated protein kinase (AMPK) signaling pathway. Conclusions: This study provides new insights into the potential utilization of astragalin-rich foods in the improvement of diabetes mellitus.

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