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[异喹啉生物碱的抗菌活性及抗菌机制研究进展]

[Progress of antibacterial activity and antibacterial mechanism of isoquinoline alkaloids].

作者信息

Cao Peng, Zhang Zi-Wei, Leng Dong-Jin, Li Xiao-Yan, Li Ying

机构信息

College of Life Science, Northeast Forest University, Harbin 150040, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2016 Jul;41(14):2600-2606. doi: 10.4268/cjcmm20161406.

Abstract

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.

摘要

本文综述了原小檗碱、原托品碱、苯并菲啶、阿朴啡、双苄基异喹啉等异喹啉生物碱的抗菌活性及构效关系。从细胞壁和细胞膜损伤、膜通透性改变、相关酶及外排泵抑制、对细菌DNA及相关蛋白质合成的影响等方面阐述了生物碱的抗菌机制。此外,本文总结了异喹啉生物碱的构效关系。为提高药物靶点的筛选效率,在天然产物开发中应充分发挥生物信息科学与组合化学的互补作用。本文将为新型抗菌剂的研发提供理论参考。

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