白藜芦醇的结构修饰与生物活性研究进展  

Research advances on structural modifications to resveratrol and their effect on biological activities

作　　者：韩丽 李鸿鹏 李文玲[1] HAN Li;LI Hong-peng;LI Wen-ling(College of Chemical and Biological Engineering,Lanzhou Jiaotong University,Lanzhou 730070,China)

机构地区：[1]兰州交通大学化学与生物工程学院,甘肃七州730070

出　　处：《药学学报》2020年第11期2558-2569,共12页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(21462024)。

摘　　要：天然白藜芦醇具有抗癌、抗氧化、诱导细胞凋亡等广泛的生物活性,但其成药性差、代谢快、靶点的选择性和生物利用度低,使其应用价值受到限制。研究表明,对天然活性先导化合物进行结构修饰以改善其药理作用,是目前开发药物的一种新策略。为了提高白藜芦醇的生物利用度,许多研究者致力于白藜芦醇衍生物和类似物的合成及活性的评价,对白藜芦醇分子结构中的酚羟基、双键和苯环等进行化学修饰,揭示各官能团之间的相互作用和构效关系。本文综述了近10年来白藜芦醇单体衍生物的化学结构、合成方法、生物作用机制和相关治疗应用,尤其是抗癌方面的作用,对此类新药的研发具有一定参考价值。Resveratrol possesses a wide range of biological activities,such as anti-cancer,anti-oxidation,induction of apoptosis,etc.,but its poor drug properties,rapid metabolism,low target selectivity and bioavailability limit its application value.Studies have shown that modification of the structure of natural compounds can improve their pharmacological activities.To improve the bioavailability of resveratrol,many researchers have undertaken the synthesis and activity evaluation of resveratrol derivatives and analogues.They have modified the phenolic hydroxyl groups,double bonds and benzene ring of resveratrol so as to further understand the interactions among functional groups and its structure-activity relationship.In this paper,we review the chemical structures,synthetic methods and mechanisms of biological activity of resveratrol monomer derivatives as well as their related therapeutic applications,especially in the anticancer area over the last decade.This will provide some reference value for the further research and development of resveratrol-related drugs.

关 键 词：白藜芦醇 结构修饰 白藜芦醇衍生物 抗癌 生物活性 

分 类 号：R916[医药卫生—药学]