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原花青素 B 可减轻餐后血糖,其对 α-葡萄糖苷酶的抑制作用:通过动力学、荧光光谱、原子力显微镜和分子对接分析。

Proanthocyanidin B attenuates postprandial blood glucose and its inhibitory effect on alpha-glucosidase: analysis by kinetics, fluorescence spectroscopy, atomic force microscopy and molecular docking.

机构信息

College of Food Science and Engineering, Northwest A&F University, Yangling 712100, P. R. China.

出版信息

Food Funct. 2018 Sep 19;9(9):4673-4682. doi: 10.1039/c8fo00993g.

Abstract

As a dimer of proanthocyanidin, proanthocyanidin B2 (PB2) was found to effectively attenuate postprandial blood glucose in mice after sucrose loading. Further studies showed that PB2 revealed strong inhibitory activity against α-glucosidase with an IC50 value of (0.23 ± 0.01) μg mL-1, and this process was reversible with a mixed-type inhibitory manner. PB2 quenched the intrinsic fluorescence of α-glucosidase through a static quenching mechanism and changed the micro-environments and conformations of α-glucosidase that led to an aggregation phenomenon. A further molecular docking study provided more information about the interactions of PB2 with the amino acid residues of α-glucosidase. Our results suggest that PB2 is useful for protection against hyperglycemia through inhibiting the activity of α-glucosidase.

摘要

作为原花青素的二聚体,原花青素 B2(PB2)被发现可有效降低蔗糖负荷后小鼠的餐后血糖。进一步的研究表明,PB2 对 α-葡萄糖苷酶表现出强烈的抑制活性,IC50 值为(0.23±0.01)μg·mL-1,这是一种具有混合抑制模式的可逆过程。PB2 通过静态猝灭机制猝灭α-葡萄糖苷酶的固有荧光,并改变α-葡萄糖苷酶的微环境和构象,导致聚集现象。进一步的分子对接研究提供了更多关于 PB2 与 α-葡萄糖苷酶氨基酸残基相互作用的信息。我们的研究结果表明,PB2 通过抑制 α-葡萄糖苷酶的活性,对防治高血糖有一定作用。

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