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合成脂肽作为抗菌剂的最新进展:设计与合成方法

Recent advances in synthetic lipopeptides as anti-microbial agents: designs and synthetic approaches.

作者信息

Koh Jun-Jie, Lin Shuimu, Beuerman Roger W, Liu Shouping

机构信息

Singapore Eye Research Institute, The Academia, 20 College Road, Discovery Tower Level 6, Singapore, 169856, Singapore.

School of Materials Science and Engineering, South China University of Technology, Guangzhou, 510641, China.

出版信息

Amino Acids. 2017 Oct;49(10):1653-1677. doi: 10.1007/s00726-017-2476-4. Epub 2017 Aug 19.

Abstract

Infectious diseases impose serious public health burdens and continue to be a global public health crisis. The treatment of infections caused by multidrug-resistant pathogens is challenging because only a few viable therapeutic options are clinically available. The emergence and risk of drug-resistant superbugs and the dearth of new classes of antibiotics have drawn increasing awareness that we may return to the pre-antibiotic era. To date, lipopeptides have been received considerable attention because of the following properties: They exhibit potent antimicrobial activities against a broad spectrum of pathogens, rapid bactericidal activity and have a different antimicrobial action compared with most of the conventional antibiotics used today and very slow development of drug resistance tendency. In general, lipopeptides can be structurally classified into two parts: a hydrophilic peptide moiety and a hydrophobic fatty acyl chain. To date, a significant amount of design and synthesis of lipopeptides have been done to improve the therapeutic potential of lipopeptides. This review will present the current knowledge and the recent research in design and synthesis of new lipopeptides and their derivatives in the last 5 years.

摘要

传染病给公共卫生带来了沉重负担,并且仍然是一场全球公共卫生危机。由多重耐药病原体引起的感染治疗具有挑战性,因为临床上可用的有效治疗选择很少。耐药超级细菌的出现和风险以及新型抗生素的匮乏,让人们越来越意识到我们可能会回到抗生素出现之前的时代。迄今为止,脂肽因其以下特性而受到了相当多的关注:它们对广泛的病原体表现出强大的抗菌活性、具有快速杀菌活性,与当今使用的大多数传统抗生素相比具有不同的抗菌作用,并且耐药趋势发展非常缓慢。一般来说,脂肽在结构上可分为两部分:亲水性肽部分和疏水性脂肪酰链。迄今为止,已经进行了大量的脂肽设计和合成工作,以提高脂肽的治疗潜力。本综述将介绍过去5年中有关新型脂肽及其衍生物的设计与合成的现有知识和最新研究情况。

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