WAP-8294A类抗生素及其高效合成的研究进展

摘要：WAP-8294A是从Lysobacter sp.发酵液中分离得到的环状脂肽类抗生素。其主要产物WAP-8294A2(lotilibcin)对耐甲氧 西林金黄色葡萄球菌(MRSA)具有强抑制活性，该类化合物通过选择性识别存在于革兰阳性细菌细胞质膜中的甲基萘醌(MK)， 破坏细胞膜来杀死细胞，但其低产量限制了工业化生产。本文综述了近年来WAP-8294A类抗生素的研究进展，重点介绍了该类 化合物的起源及生物合成；活性靶点及其构效关系；产量提高策略。为后续探索WAP-8294A类抗生素大规模生产的最适条件及 设计其高活性衍生物奠定基础。

Research progress of WAP-8294A antibiotics and their efficient synthesis

Abstract WAP-8294A is a cyclic lipopolypeptide antibiotic isolated from the fermentation broth of Lysobacter sp. Its major product, WAP-8294A2 (lotilibcin), has strong inhibitory activity against methicillin-resistant Staphylococcus aureus (MRSA), by selectively identifying menaquinone (MK) present in the cytoplasmic membrane of Gram-positive bacteria and destroying cell membranes to kill cells, but its low yield limits industrial production. In this paper, the research progress of WAP-8294A antibiotics in recent years was reviewed, focusing on the origin and biosynthesis of these compounds, active targets, and their structure-activity relationships, as well as strategies for yieldimprovement. This will lay the foundation for the subsequent exploration of the optimal conditions for large-scale production of WAP-8294A antibiotics and the design of their highly active