含乙基咔唑基团钌化合物的合成及其抗菌活性研究  

Synthesis and Antibacterial Activity of Ruthenium Compounds Containing Ethylcarbazole Groups

作　　者：宋允 黄紫莹 余光英 林文静 姜桂娟 王金涛 廖向文 SONG Yun;HUANG Zi-ying;YU Guang-ying;LIN Wen-jing;JIANG Gui-juan;WANG Jin-tao;LIAO Xiang-wen(School of Pharmacy,Jiangxi Science and Technology Normal University,Nanchang 330013,China)

机构地区：[1]江西科技师范大学药学院,江西南昌330013

出　　处：《化学试剂》2024年第2期114-120,共7页Chemical Reagents

基　　金：江西省自然科学基金项目(20212BAB203007);江西省教育厅科技计划项目(GJJ211106,GJJ201139)。

摘　　要：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 eradication,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.

关 键 词：金黄色葡萄球菌 钌配合物 乙基咔唑 抗菌 

分 类 号：R916[医药卫生—药学]