Suppr超能文献

年轻苹果多酚作为天然α-葡萄糖苷酶抑制剂:体外和计算研究。

Young apple polyphenols as natural α-glucosidase inhibitors: In vitro and in silico studies.

机构信息

College of Food Engineering and Nutritional Science, Shaanxi Normal University, Xi'an 710062, PR China.

College of Food Science and Engineering, Northwest A & F University, Yangling, PR China.

出版信息

Bioorg Chem. 2020 Mar;96:103625. doi: 10.1016/j.bioorg.2020.103625. Epub 2020 Jan 28.

Abstract

In this study, the inhibitory activity of young apple polyphenols (YAP) on α-glucosidase was investigated. Composition and inhibition analyses suggested that tannic acid (TA), (-)-epicatechin (EC) and phlorizin (PH) were the main active constituents in YAP showing α-glucosidase inhibition. PH was a competitive inhibitor, while YAP, TA and EC were the mixed-type ones. YAP, TA, PH and EC quenched the fluorescence spectrum of α-glucosidase significantly. Interestingly, the constants that indicate binding interaction between α-glucosidase and TA, PH, EC, including reciprocal of competitive inhibition constant (1/K), fluorescence quenching constant (K) and binding energy (E), were shown similar orders as TA > PH > EC, contrary to IC values. This indicates that binding interactions between polyphenols and α-glucosidase caused the enzyme inhibition. Additionally, potential enzyme unfolding by polyphenols interactions indicated by red-shift of maximum emission wavelength is supported by the decrease in α-helix and β-sheet contents of the enzyme. Conclusively, the α-glucosidase inhibition indicates that YAP may have potentials in alleviation of type 2 diabetes symptom.

摘要

本研究考察了青年苹果多酚(YAP)对α-葡萄糖苷酶的抑制活性。组成和抑制分析表明,鞣酸(TA)、(-)-表儿茶素(EC)和根皮苷(PH)是 YAP 中具有α-葡萄糖苷酶抑制作用的主要活性成分。PH 是一种竞争性抑制剂,而 YAP、TA 和 EC 则是混合型抑制剂。YAP、TA、PH 和 EC 均能显著猝灭α-葡萄糖苷酶的荧光光谱。有趣的是,表明α-葡萄糖苷酶与 TA、PH、EC 之间结合相互作用的常数,包括竞争性抑制常数的倒数(1/K)、荧光猝灭常数(K)和结合能(E),与 IC 值相反,呈类似的顺序:TA>PH>EC。这表明多酚与α-葡萄糖苷酶之间的结合相互作用导致了酶抑制。此外,多酚相互作用潜在导致酶展开,由最大发射波长的红移得到证实,这反映了酶的α-螺旋和β-折叠含量降低。综上所述,α-葡萄糖苷酶抑制作用表明 YAP 可能具有缓解 2 型糖尿病症状的潜力。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验