食品科学

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表没食子儿茶素没食子酸酯分子修饰及抗癌研究进展

刘 飞1,熊政委2,李春华1,张 娟1,王小萍1,唐晓波1,王 云1,*   

  1. 1.四川省农业科学院茶叶研究所,四川 成都 610066;2.重庆第二师范学院生物与化学工程系,重庆 400067
  • 出版日期:2015-12-15 发布日期:2015-12-24

Progress in Molecular Modification and Anticancer Activity of (–)-Epigallocatechin-3-gallate (EGCG)

LIU Fei1, XIONG Zhengwei2, LI Chunhua1, ZHANG Juan1, WANG Xiaoping1, TANG Xiaobo1, WANG Yun1,*   

  1. 1. Tea Research Institute, Sichuan Academy of Agricultural Sciences, Chengdu 610066, China;
    2. School of Biological and Chemical Engineering, Chongqing University of Education, Chongqing 400067, China
  • Online:2015-12-15 Published:2015-12-24

摘要:

表没食子儿茶素没食子酸酯((–)-epigallocatechin-3-gallate,EGCG)是茶叶中的一类重要儿茶素,在体内外实验中被证实具有广泛的抗癌活性。研究发现,其抗癌机理包含诱导细胞凋亡、抗血管生成、调控细胞周期、阻滞细胞转移、协同抗癌等,但由于多羟基的化学结构使其在中性或碱性介质中极不稳定,最终导致其生物活性利用率降低,限制了临床应用范围。已有研究表明,分子修饰能显著改善EGCG分子活性,增强其稳定性,并使其表现出较强的抗癌活性。本文首先概述EGCG分子修饰的方法,然后对EGCG及其衍生物的抗癌实例和作用机理进行归纳总结。

关键词: 表没食子儿茶素没食子酸酯, 分子修饰, 衍生物, 抗癌机理, 纳米材料

Abstract:

(–)-Epigallocatechin-3-gallate (EGCG), one of the important catechins in tea, has been demonstrated to have
anticancer activity both in vitro and in vivo. The anticancer mechanism has been confirmed to be associated with cell
apoptosis, resistance to angiogenesis, regulation of cell cycles, retardation of cell transfer, and collaborative anticancer
effects. Unfortunately, EGCG has limited clinical applications due to its unstable characteristics in neutral or alkaline
environment, which stems from its “polyhydroxyl” structure. Previous studies have demonstrated that the anticancer activity
and stability of EGCG can be remarkably improved by molecular modification. The review summarizes the methods used for
molecular modification of EGCG and the anticancer effects and mechanisms of EGCG and its derivatives.

Key words: (–)-epigallocatechin-3-gallate, molecular modification, derivatives, anticancer mechanism, nanometer materials

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