斑蝥素及其衍生物构效修饰的研究进展

Research progress on structure-activity modification of cantharidin and its derivatives

关键词:  斑蝥素  斑蝥素衍生物  抗肿瘤  构效关系  结构改造

Key words:  cantharidin  cantharidin derivatives  antitumor  structure-activity relationship  structural modification

摘要:

斑蝥素为存在于中药斑蝥等干燥虫体中的单萜类化合物，具有良好的抗癌活性，但由于黏膜刺激等毒副作用而限制了其临床应用，因此研究人员对其结构进行修饰，以达到减毒增效的目的。本文对斑蝥素及其结构中（ 1）1-、4-位，（ 2）2-、3-位，（ 3）5-、6-位，（ 4）7-O位，（ 5）酸酐等不同位点修饰的衍生物的构效关系进行综述，以期为新型斑蝥素衍生物的药物研发提供理论参考。

Abstract:

Cantharidin is a monoterpene compound existing in dried insects such as Mylabris, a traditional Chinese medicine. Cantharidin has good anticancer activities, however, its clinical application is limited because of mucosal irritation and other toxic side effects. Therefore, researchers have modified the structure of cantharidin to reduce toxicity and increase efficiency. In this paper, the structure-activity relationships of cantharidin and its derivatives modified at (1) 1- and 4- positions, (2) 2- and 3- positions, (3) 5- and 6- positions, (4) 7-O position and (5) anhydride position are discussed, in order to provide theoretical reference for drug research and development of new cantharidin derivatives.