从分子角度看抗菌绿茶儿茶素:作用机制和构效关系。

Antibacterial green tea catechins from a molecular perspective: mechanisms of action and structure-activity relationships.

机构信息

Global Education Institute, University of the Ryukyus, Nishihara, Okinawa 903-0213, Japan.

出版信息

Food Funct. 2020 Nov 18;11(11):9370-9396. doi: 10.1039/d0fo02054k.

Abstract

This review summarizes the mechanisms of antibacterial action of green tea catechins, discussing the structure-activity relationship (SAR) studies for each mechanism. The antibacterial activity of green tea catechins results from a variety of mechanisms that can be broadly classified into the following groups: (1) inhibition of virulence factors (toxins and extracellular matrix); (2) cell wall and cell membrane disruption; (3) inhibition of intracellular enzymes; (4) oxidative stress; (5) DNA damage; and (6) iron chelation. These mechanisms operate simultaneously with relative importance differing among bacterial strains. In all SAR studies, the highest antibacterial activity is observed for galloylated compounds (EGCG, ECG, and theaflavin digallate). This observation, combined with numerous experimental and theoretical evidence, suggests that catechins share a common binding mode, characterized by the formation of hydrogen bonds and hydrophobic interactions with their target.

摘要

本文综述了绿茶儿茶素的抗菌作用机制,并讨论了每种机制的结构-活性关系(SAR)研究。绿茶儿茶素的抗菌活性源于多种机制,这些机制可大致分为以下几类:(1)抑制毒力因子(毒素和细胞外基质);(2)破坏细胞壁和细胞膜;(3)抑制细胞内酶;(4)氧化应激;(5)DNA 损伤;(6)铁螯合。这些机制同时作用,不同的细菌菌株其相对重要性不同。在所有的 SAR 研究中,酯化化合物(EGCG、ECG 和茶黄素双没食子酸酯)表现出最高的抗菌活性。这一观察结果,结合大量的实验和理论证据,表明儿茶素具有共同的结合模式,其特征是与靶标形成氢键和疏水相互作用。

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