环肽类化合物抗耐药鲍曼不动杆菌的研究进展  

Recent Progress in the Application of Cyclopeptides Against Drug-Resistant Acinetobacter baumannii

作　　者：刘俊娜 周威 徐志 Liu Jun-na;Zhou Wei;Xu Zhi(School of Pharmacy,Guizhou Medical University,Gui’an 561113;Guizhou Miaoaitang Health Management Co.,Ltd.,Guiyang 550025)

机构地区：[1]贵州医科大学药学院,贵安561113 [2]贵州苗艾堂健康管理有限公司,贵阳550025

出　　处：《国外医药（抗生素分册）》2024年第5期297-303,共7页World Notes on Antibiotics

摘　　要：鲍曼不动杆菌通过表达外排泵、改变抗菌药作用靶点和产生药物灭活酶等机制对几乎所有现有抗菌药产生了不同程度的耐药性。目前,治疗耐药鲍曼不动杆菌尤其是耐碳青霉烯类药物鲍曼不动杆菌和耐多药的药物屈指可数,而新型耐药菌如全耐药鲍曼不动杆菌在世界范围内不断涌现。因此,耐药鲍曼不动杆菌业已成为全球范围内最具挑战的公共卫生问题之一,亟待研发新型抗菌药。环肽类化合物具有良好的稳定性、优异的受体亲和力、良好的细胞膜渗透性和口服生物利用度等优点,且环肽类药物达托霉素已用于治疗耐药菌引起的感染。因此,环肽类化合物在抗耐药菌领域引起了研究人员的普遍关注。本文归纳自2020年以来所发展的具有抗耐药鲍曼不动杆菌活性的环肽类化合物的最新研究进展,以期为今后发现新型药物候选物提供理论支持。Acinetobacter baumanniican is resistant to practically all antibiotics now on the market.It gains resistance by a variety of processes,including the expression of efflux pumps,modification of antimicrobial targets,and production of drug-inactivating enzymes.Currently,only a few drugs available to treat drug-resistant Acinetobacter baumannii,especially carbapenem-resistant Acinetobacter baumannii and multidrug-resistant Acinetobacter baumannii,and new resistant forms such as pan-resistant Acinetobacter baumannii are constantly emerging worldwide.Drug-resistant Acinetobacter baumannii has become one of the most challenging public health issues worldwide,creating an urgent need to develop new antibiotics.Cyclopeptides possess good stability,excellent receptor affinity,favorable cell membrane permeability as well as oral bioavailability,and the cyclopeptide agent datomycin has already been applied in clinics to treat infections caused by drug-resistant bacteria.Therefore,cyclopeptides have attracted widespread attention from scientists.In order to give theoretical support for the future discovery of new therapeutic candidates,this study will present an overview of the most recent research progress on cyclopeptides with antibacterial activity against drug-resistant Acinetobacter baumannii infections developed from 2020.

关 键 词：环肽 抗菌 耐药 鲍曼不动杆菌 作用机制 体内活性 

分 类 号：R978[医药卫生—药品]