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.
作者
彭希希
王赛赛
付琛
胡昌华
廖国建
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)
出处
《药学学报》
CAS
CSCD
北大核心
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)
关键词
脂肽
达托霉素
抗菌谱
作用机制
耐药机制
构效关系
lipopeptide
daptomycin
spectrum of antimicrobial activity
mode of action
mechanism of drug resistance
structure-activity relationship