Synthesis and antibacterial activity of 8-ketoberberine derivatives

文献类型： 外文期刊

第一作者： Li, Feifei

作者： Li, Feifei;Wu, Jingjing;Yue, Xiyan;Wu, Fanhong;Yu, Yanyan;Suo, Yujuan;Li, Jinliang

作者机构：

关键词： Berberine; alkyl ketone; C-8 substitution; antibacterial activity; foodborne pathogens

期刊名称：FOOD QUALITY AND SAFETY （ 影响因子：4.4； 五年影响因子：4.8 ）

ISSN： 2399-1399

年卷期： 2024 年 8 卷

页码：

收录情况： SCI

摘要： Natural berberine (BBR) exhibits good antimicrobial efficacy; however, its limited bioavailability greatly hinders its clinical application.The aim of this study is to synthesize a series of novel lipophilic C-8 substituted BBR prodrugs, conduct in vitro antibacterial activity tests on four common clinical pathogens, and further investigate their inhibitory mechanisms through bacterial membrane formation ability, cell permeability, hydrophobicity, and self-cohesion. Compound 14 showed the best activity with minimum inhibitory concentration (MIC) of 15.62 mu g/mL and minimum bactericidal concentration (MBC) of 31.25 mu g/mL against Staphylococcus aureus (ATCC 29213) and Listeria monocytogenes (4b G). In the mechanism study, compound 14 significantly inhibited bacterial biofilm formation by over 60% at a concentration of 0.5 MIC and enhanced cell membrane permeability by 40%. Meanwhile, compound 14 can interact with the cell membrane, exposing its hydrophobic regions and reducing the intercellular self-coagulation index to approximately 20%. The study indicates that the novel compound 14 enhanced the antibacterial efficacy by significantly reducing bacterial surface hydrophobicity and self-cohesion, as well as disrupting bacterial biofilm. In summary, we have created a series of 8-ketoberberine derivatives, which opens new prospects for BBR derivatives in the treatment of bacterial infections.

分类号：

  • 相关文献
作者其他论文 更多>>

微信小程序