新型环脂肽抗生素达托霉素研究进展  

Current status and future perspectives of daptomycin development

作　　者：彭希希 王赛赛 付琛[1] 胡昌华[1] 廖国建[1] PENG Xi-xi;WANG Sai-sai;FU Chen;HU Chang-hua;LIAO Guo-jian(Institute of Modern Biopharmaceuticals, School of Pharmaceutical Sciences, Southwest University, Chongqing 400716, China)

机构地区：[1]西南大学药学院,现代生物医药研究所,重庆400716

出　　处：《药学学报》2018年第6期839-844,共6页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(31670050,31100069); 中央高校基本科研业务费专项资金资助项目(XDJK2017B011)

摘　　要：作为首个进入临床应用的新型环脂肽抗生素,达托霉素抗菌活性强,耐药比例低,已成为治疗耐药革兰阳性菌所致感染的一线用药。本文主要对达托霉素的抗菌谱、生物合成途径、作用机制、耐药机制、构效关系、新型衍生物surotomycin和铁载体-达托霉素偶联物杀灭耐药鲍曼不动杆菌等研究结果进行综述,以期为新型达托霉素衍生物研发有所裨益。Due to the potent bactericidal activity and low incidence of drug resistance, the novel cyclic lipopeptide antibiotic - daptomycin has emerged as one of the first line antimicrobial agents in the treatment of serious infections caused by gram-positive resistant pathogens. This review summarizes the research advances of daptomycin in recent years, mainly including spectrum of antimicrobial activity, biosynthesis, mode of action, mechanism of drug resistance, structure-activity relationships, surotomycin and siderophore-daptomycin conjugate to kill multidrug resistant Acinetobacter baumannii. The findings summarized in this review highlight the directions of next-generation of daptomycin derivatives.

关 键 词：脂肽 达托霉素 抗菌谱 作用机制 耐药机制 构效关系 

分 类 号：R961[医药卫生—药理学]