槐定碱及其衍生物的生物构效关系研究进展

Research progress on structural modification and biological activity of sophoridine

槐定碱是从药用植物苦豆子中提取出的一种生物碱,除了具有较高的抗肿瘤活性外,还有良好的抗炎、镇痛、杀虫等活性。槐定碱被广泛用作其他抗癌药物的辅助药物,但现目前关于槐定碱的上市药物仅有在2005年由我国自主研制并且拥有知识产权的盐酸槐定碱注射液。随着科技的发展,人工智能技术在药物研发中发挥出越来越重要的作用,广西大学王立升课题组通过分子对接技术发现Topo酶是槐定碱作为抗肿瘤药物的一个重要作用靶点,并以槐定碱为先导化合物,通过对槐定碱进行结构修饰和构效关系分析,为开发出新型安全低毒的抗肿瘤药物提供参考。因此对槐定碱的药理作用以及槐定碱衍生物的构效关系进行简单的总结,用于评价其对于抗癌活性的影响。

Sophoridine is an alkaloid extracted from the medicinal plant Sophora vulgaris.In addition to its high anti-tumor activity,it also has good anti-inflammatory,analgesic,and insecticidal activities.Sophoridine is widely used as an auxiliary drug for other anti-cancer drugs,but currently the only marketed drug for sophoridine is sophoridine hydrochloride injection,which was independently developed by my country in 2005 and has intellectual property rights.With the development of science and technology,artificial intelligence technology is playing an increasingly important role in drug research and development.Through molecular docking technology,Wang Lisheng’s research group at Guangxi University discovered that Topo enzyme is an important target of sophoridine as an anti-tumor drug.And taking sophoridine as the lead compound,through structural modification and structure-activity relationship analysis of sophoridine,it provides a reference for the development of new,safe and low-toxic anti-tumor drugs.Therefore,a simple summary of the pharmacological effects of sophoridine and the structure-activity relationship of sophoridine derivatives is used to evaluate its effect on anticancer activity.