以乙基咔唑取代的邻菲啰啉衍生物为主配体(ECYMP)合成了 4个新型抗菌钌化合物,通过最低抑菌浓度、最低杀菌浓度、溶血实验、生物膜清除试验、DNA泄露试验、大蜡螟幼虫以及小鼠感染模型对化合物的抗菌活性、安全性、耐药性和抗菌机制进行了评价.研究结果显示,4个钌配合物均具有显著的抗菌活性,化合物Ru-2能通过破坏细菌细胞膜的完整性杀死细菌.此外,Ru-2不仅能有效抑制细菌毒素的分泌,而且具有较高的安全性.在动物感染模型中,Ru-2也展现出显著的抗感染活性.综合而言,具有乙基咔唑功能化配体的钌化合物具有显著的体内外抗菌活性.
Four new antibacterial ruthenium complexes were synthesized with ethylcarbazole-substituted phenanthroline derivative(ECYMP)as the main ligand.The antibacterial activity,safety,resistance frequencies and mode of action were evaluated through various assays,including minimum inhibitory concentration,minimum bactericidal concentration,hemolytic toxin test,biofilm erad-ication,DNA leakage assay,G.melonella larvae and mouse infection model.The results revealed that all four ruthenium complexes exhibited significant antibacterial activity,with compound Ru-2 demonstrating the ability to kill bacteria by disrupting the integrity of bacterial cell membranes.In addition,Ru-2 not only effectively inhibited the secretion of bacterial toxins,but also exhibited high safety level.In the animal infection model,Ru-2 demonstrated significant anti-infective activity.In summary,ruthenium complexes with ethylcarbazole-functionalized ligands exhibit significant in vitro and in vivo antimicrobial activity.