首页|Synthesis and antibacterial activity of 8-ketoberberine derivatives
Synthesis and antibacterial activity of 8-ketoberberine derivatives
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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,hydropho-bicity,and self-cohesion.Compound 14 showed the best activity with minimum inhibitory concentration(MIC)of 15.62 μg/mL and minimum bactericidal concentration(MBC)of 31.25 μg/mL against Staphylococcus aureus(ATCC 29213)and Listeria monocytogenes(4b G).In the mech-anism study,compound 14 significantly inhibited bacterial biofilm formation by over 60％at a concentration of 0.5 MIC and enhanced cell mem-brane 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.
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