诺卡沙星及其结构类似物的研究进展

Research Progress of Nocathiacin and Its Structural Analogues

诺卡沙星及其结构类似物是一类结构特征明显的天然次级代谢产物,对革兰氏阳性菌具有很强的杀灭作用,其独具一格的抗菌机制受到研究者的广泛关注。诺卡沙星大多本身成药性不好,但是其非天然的结构类似物在成药性方面得到改善。诺卡沙星的生产方式已不局限于生物发酵,化学合成技术也有望用于改造和生产的中间环节。综述了诺卡沙星及其结构类似物的生物合成机制、生产策略、抗菌机制,指出了诺卡沙星及其结构类似物在应用方面存在的问题,为其在医药及养殖行业的广泛应用提供了有效策略。

Nocathiacin and its structural analogues are a class of natural secondary metabolites with obvious structural characteristics.They have a strong killing effect on Gram-positive bacteria.Their unique antibacterial mechanism has also attracted wide attention of scholars.Nocathiacin almostly have poor drug-making properties,but the drug-forming properties of their unnatural structural analogues have been improved.At the same time,the production method of Nocathiacin is no longer limited to biological fermentation,and chemical synthesis technology is also applied to the intermediate links of transformation and production.In this paper,we summarize the biosynthesis mechanism,production strategy,and antibacterial mechanism of Nocathiacin and its structural analogues,point out the problems existing in the application of Nocathiacin and its structural analogues,and provide effective strategies for its wide application in medicine and aquaculture industry.