抗细菌药物默诺霉素的化学生物学研究进展

Advances in chemical and biological research of the antibacterial drug moenomycins

摘要:

默诺霉素（moenomycins）家族类化合物主要是由链霉菌产生，属于磷酸糖脂类抗生素。该类化合物通过与细菌细胞壁肽聚糖糖基转移酶（peptidoglycan transferase，PGT）的活性位点结合，可以抑制众多革兰氏阳性细菌细胞壁的合成，具有很强的生物活性和重要的应用开发潜力。本文针对默诺霉素的化学结构、生物活性机制、抗性机制、生物合成研究途径、外排机制和新结构创制等化学生物学方面进行了系统综述，并对默诺霉素化学生物学研究现状以及可能存在的问题进行了总结，旨在为高活性磷酸糖脂类临床药物的研究与开发提供借鉴。

关键词:默诺霉素;肽聚糖糖基转移酶;生物活性机制;生物合成

Abstract:

Moenomycins produced by Streptomyces are phosphoglycolipid antibiotics, and inhibit the active sites of peptidoglycan glycosyltransferases involved in the biosynthesis of Gram-positive bacterial cell wall. Moenomycins show a strong biological activity, and possess important research value and development potential. This paper systematically reviews the advances in chemical biology of moenomycins, including the chemical structures, bioactive mechanisms, latest development of biosynthesis, efflux mechanisms and new derivatives of moenomycins. Moreover, the research bottleneck in chemical biology of moenomycins is referred aiming to promote the research and development of high-activity phosphoglycolipid drugs for clinic and industry.

Key words:moenomycins;peptidoglycan transferase;bioactive mechanisms;biosynthesis