苦参碱来源于豆科植物苦豆子、苦参和越南槐等中药,在结构分类上属于喹诺里西啶类生物碱,具有多种生物活性,其抗肿瘤活性是近年研究的热点。苦参碱的抗肿瘤活性确切,但是强度不高,因此对其进行结构改造、提高生物利用度以提高抗肿瘤活性显得尤为重要。综述了目前苦参碱结构改造及其抗肿瘤活性的研究进展,希望有助于了解苦参碱的抗肿瘤构效关系和指导抗肿瘤新药物的研发。

Matrine is an alkaloid belonged to quinolizidine in structure which is from Sophora alopecuroides Linn., S. flavescens Alt. and S. tonkinensis Gagnep. Matrine could exhibit a variety of biological activities, especially antitumor activity in recent years. Its antitumor activity is assured, but probably weak. Thus it is necessary to do some structural modifications of it to improve the bioavailability as well as to improve the antitumor potency. This paper reviews the current progress of matrine analogs and their antitumor activities, in the hope to get insight into antitumor structure-activity relationships of matrine and also give tips to antitumor drug research and development.

天津市科技支撑计划项目(12ZCDZSY11900);北京协和医学院研究生创新基金资助项目(20131007021)