截短侧耳素类抗生素及其耐药研究进展  

Advances in the Research on the Resistance Mechanism of Pleuromutilins

作　　者：丁超月 徐艳 孙丽 王兴宇 王宗朝 袁欣怡 瞿玮[1] 潘源虎[1] Ding Chao-yue;Xu Yan;Sun Li;Wang Xing-yu;Wang Zong-chao;Yuan Xin-yi;Qu Wei;Pan Yuan-hu(National Reference Laboratory of Veterinary Drug Residue,Wuhan 430070)

机构地区：[1]华中农业大学国家兽药残留基准实验室,武汉430070

出　　处：《国外医药（抗生素分册）》2023年第3期166-172,共7页World Notes on Antibiotics

基　　金：国家重点研发计划(2021YDF1800401)。

摘　　要：截短侧耳素(Pleuromutilins)是从担子菌纲侧耳属Pleurotus mutilus和Pleurotus passeckerianus中分离得到的二萜类抗生素,对革兰阳性菌和支原体具有良好的抗菌活性。截短侧耳素类药物用途广泛,泰妙菌素(Tiamulin)和沃尼妙林(Valnemulin)作为兽用药用于防治由病原微生物引起的猪痢疾、支原体肺炎等疾病;人用批准的瑞他莫林(Retapamulin)和来法莫林(Lefamulin)主要用于治疗球菌感染和获得性细菌性肺炎。近年来,截短侧耳素类药物耐药监测表明,在病原微生物的rplC、rplD、23sRNA、Cfr和vga基因中报道了多种新的突变位点,导致侧耳素类药物敏感性降低。本文对已上市的截短侧耳素类药物进行回顾,并对近十年该类药物的耐药机制研究进行综述,以期为新型截短侧耳素类药物的创制提供参考。Pleuromutilin is a diterpene antibiotic isolated from Pleurotus mutilus and Pleurotus passeckerianu,which has good antibacterial activity against Gram-positive bacteria and mycoplasma.The pleuromutilin drugs are widely used.Tiamulin and Valnemulin are used as veterinary drugs to prevent and treat diseases such as swine dysentery and mycoplasma pneumonia caused by pathogenic microorganisms.Retapamulin and Lefamulin approved by human medicine are mainly used to treat coccus infection and acquired bacterial pneumonia.In recent years,the monitoring of pleuromutilin resistance has shown that a variety of new mutation sites have been reported in the rplC,rplD,23sRNA,Cfr and vga genes of pathogenic microorganisms,resulting in reduced sensitivity to pleuromutilin drugs.In this paper,the listed pleuromutilin drugs were reviewed,and the drug resistance mechanism of pleuromutilin drugs in recent ten years was reviewed,in order to provide reference for the creation of new pleuromutilin drugs.

关 键 词：截短侧耳素 抗菌活性 作用机制 耐药机制 PLSA型耐药 ABC-结合蛋白 

分 类 号：R978.1[医药卫生—药品]