异喹啉类生物碱抑菌活性及抑菌机制研究进展

该文综述了异喹啉类生物碱中原小檗碱型、普托品型、苯并菲啶型、阿朴菲型、双苄基异喹啉型的抗菌活性和部分构效关系,并从菌体细胞壁、细胞膜的破坏及膜通透性的改变、相关酶和外排泵的抑制、影响菌体DNA和相关蛋白合成等多个方面详细阐述生物碱抑菌作用的分子机制。此外,该文还对当前异喹啉类生物碱构效关系的研究进行总结,指出应充分发挥靶标数据库筛选和组合化学在天然产物开发中的互补作用,以此提高药物靶标的筛选效率。该文将为以异喹啉类生物碱为先导物的新型抗菌剂研发提供理论参考。

Progress of antibacterial activity and antibacterial mechanism of isoquinoline alkaloids

This paper reviewed the antibacterial activity and structure-activity relationship of isoquinoline alkaloids, such as protoberberine, protopine, benzophenanthridine, aporphine, double benzyl isoquinoline, etc. The antibacterial mechanism of alkaloids were illustrated from cell wall and membrane damage, membrane permeability changes, related enzymes and efflux pump inhibition, influence of bacterial DNA and related protein synthesis and so on. In addition, this paper summarized the structure-activity relationship of isoquinoline alkaloids. In order to improve the screening efficiency of drug targets, the complementary effect of biological information science and combinatorial chemistry should be developed abundantly in the development of natural product. This paper will provide a theoretical reference for the research and development of new antibacterial agent.