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结构不同的黄酮类化合物对α-葡萄糖苷酶抑制机制的比较研究及与阿卡波糖的协同作用。

Comparative study of inhibition mechanisms of structurally different flavonoid compounds on α-glucosidase and synergistic effect with acarbose.

机构信息

School of Life Sciences, Tianjin University, Tianjin 300072, PR China.

Shaanxi Zhuyuanbang Medical Technology Co., Ltd, Xi'an 710048, PR China.

出版信息

Food Chem. 2021 Jun 15;347:129056. doi: 10.1016/j.foodchem.2021.129056. Epub 2021 Jan 9.

Abstract

Flavonoid compounds have anti-diabetic activity, which can control blood glucose levels by inhibiting α-glucosidase activity. In this paper, the inhibition mechanisms between four flavonoid compounds and α-glucosidase were studied by multispectroscopic methods and molecular docking. The results showed that the inhibitory activities of flavonoid compounds were higher than that of acarbose, and the sequence of inhibition effect was scutellarein > nepetin > apigenin > hispidulin > acarbose. Also, the synergistic effects of flavonoid compounds combined with acarbose on inhibiting α-glucosidase activity were observed. The fluorescence results showed that flavonoid compounds combined with α-glucosidase to form a stable complex. And the spectral analysis indicated that the microenvironmental and secondary structure of α-glucosidase were changed. The present study demonstrated that the molecular structure of flavonoid compounds played an important role in the inhibition process, namely, scutellarein with more hydroxyl groups on the A-ring might serve as the most effective α-glucosidase inhibitor.

摘要

类黄酮化合物具有降血糖活性,可通过抑制α-葡萄糖苷酶活性来控制血糖水平。本文采用多种光谱方法和分子对接研究了 4 种类黄酮化合物与α-葡萄糖苷酶的相互作用机制。结果表明,类黄酮化合物的抑制活性高于阿卡波糖,抑制效果的顺序为:圣草酚>川陈皮素>芹菜素>哈帕苷>阿卡波糖。此外,还观察到类黄酮化合物与阿卡波糖联合使用对抑制α-葡萄糖苷酶活性具有协同作用。荧光结果表明,类黄酮化合物与α-葡萄糖苷酶形成稳定的复合物。光谱分析表明,α-葡萄糖苷酶的微环境和二级结构发生了变化。本研究表明,类黄酮化合物的分子结构在抑制过程中起着重要作用,即在 A 环上具有更多羟基的圣草酚可能是最有效的α-葡萄糖苷酶抑制剂。

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