含笑内酯的结构修饰、生物活性及构效关系研究进展  

Research progress on structural modifications,biological activities and structure-activity relationships of micheliolide

作　　者：赵茹 曾炳麟 潘显道[1] ZHAO Ru;ZENG Bing-lin;PAN Xian-dao(Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China)

机构地区：[1]中国医学科学院北京协和医学院药物研究所,北京100050

出　　处：《天然产物研究与开发》2020年第3期532-539,497,共9页Natural Product Research and Development

基　　金：国家十三五重大专项子课题(2018ZX09711-001-005)。

摘　　要：含笑内酯是来自天然植物的愈创木烷型倍半萜内酯,具有多重药理作用。近年来,为了提高含笑内酯的生物活性和血药浓度,对其结构进行了大量修饰与改造,发现了一系列活性优于含笑内酯以及更具成药性研究的含笑内酯衍生物。本文总结了含笑内酯作用机制、结构修饰、生物活性及构效关系的相关研究进展。Micheliolide is a sesquiterpene lactone isolated from various natural plants and has lots of biological activities.In recent years,a wide range of micheliolide derivatives have been synthesized by structural modifications with valuable activities.In this review,we will highlight the advances in mechanism of action,structural modifications,biological activities and structure-activity relationships of micheliolide.

关 键 词：含笑内酯 作用机制 衍生物 生物活性 构效关系 

分 类 号：R914.5[医药卫生—药物化学]