盐霉素药理活性及构效关系研究进展  

Recent progress of pharmacology and structure-activity relationship study of salinomycin

作　　者：李波[1] 张文轩[1] 武红娜 吴松[1] 

机构地区：[1]中国医学科学院北京协和医学院药物研究所,活性物质发现与适药化研究北京市重点实验室,北京100050

出　　处：《中国药物化学杂志》2016年第3期244-252,共9页Chinese Journal of Medicinal Chemistry

基　　金：北京协和医学院青年基金项目(33320140068);北京市自然科学基金青年基金项目(7164282)

摘　　要：盐霉素一直作为一种抗菌药以及兽药被广泛使用,近年来研究发现盐霉素还具有消除肿瘤干细胞的能力,可选择性诱导肿瘤和肿瘤干细胞的细胞凋亡或者非程序性死亡,但其作用机制目前尚不完全清楚。另外,盐霉素的抗肿瘤活性还需要进一步提高,而且因其具有一定的毒性,影响了其成药性。针对这些问题,目前国内外已经开展了对盐霉素的药物化学研究,并总结了一定的构效关系。本文对盐霉素的抗肿瘤作用机制、毒性以及构效关系方面的研究进行综述。Salinomycin has been widely used as antibacterial and veterinary drug.In recent years,it has been found that salinomycin is capable of killing breast cancer stem cells,selective induction of cancer cells and cancer stem cells apoptosis or non-programmed death.However,the exact mechanism of salinomycin was not fully illuminated.In addition pne important caveat for the potential clinical application of salinomycin is its considerable neural toxicity.Recently,several researches on medicinal chemistry of salinomycin have been reported.This review is focused on the mechanism and toxicity of salinomycin and gives an overview of its structure-activity relationship study.

关 键 词：盐霉素 抗肿瘤药物 机制:结构修饰 

分 类 号：R96[医药卫生—药理学]