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Octahedral ruthenium (II) polypyridyl complexes as antimicrobial agents against mycobacterium

机译:八面体钌(II)聚吡啶基配合物作为抗分枝杆菌的抗菌剂

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摘要

Tuberculosis is one of the world’s deadliest infectious disease with 1.5 millions deaths annually. It is imperative to discover novel compounds with potent activity against M. tuberculosis. In this study, susceptibilities of M. smegmatis to the octahedral ruthenium(II) polypyridyl complexes, >1 {[(bpy)3Ru] (PF6)2 (bpy = 2,2′-bipyridine)}, >2 {[(phen)2Ru(dppz)](PF6)2 (phen = 1,10-phenanthroline, dppz = dipyridophenazine)} and >3 {[(phen)3Ru](PF6)2} were measured by broth microdilution and reported as the MIC values. Toxicities of complex >3 to LO2 and hepG2 cell lines were also measured. Complex >2 inhibited the growth of M. smegmatis with MIC value of 2 µg/mL, while complex >3 was bactericidal with MIC value of 26 µg/mL. Furthermore, the bactericidal activity of complex >3 was dependent on reactive oxygen species production. Complex >3 showed no cytotoxicity against LO2 and hepG2 cell lines at concentration as high as 64 µg/mL, paving the way for further optimization and development as a novel antibacterial agent for the treatment of M. tuberculosis infection.
机译:结核病是世界上最致命的传染病之一,每年有150万人死亡。必须发现对结核分枝杆菌具有有效活性的新型化合物。在这项研究中,耻垢分枝杆菌对八面体钌(II)聚吡啶基络合物> 1 {[(bpy)3Ru](PF6)2(bpy = 2,2'-联吡啶)}的敏感性, > 2 {[((phen)2Ru(dppz)](PF6)2(phen = 1,10-菲咯啉,dppz =二吡咯啉))}和> 3 {[((phen)通过肉汤微量稀释测量[3 Ru](PF 6)2},并记录为MIC值。还测量了复合物> 3 对LO2和hepG2细胞系的毒性。复合物> 2 抑制耻垢分枝杆菌的生长,MIC值为2μg/ mL,而复合物> 3 具有杀菌作用,MIC值为26μg/ mL。此外,复合物> 3 的杀菌活性取决于活性氧的产生。复合物> 3 在浓度高达64μg/ mL时对LO2和hepG2细胞系均无细胞毒性,这为进一步优化和开发作为治疗结核分枝杆菌感染的新型抗菌剂铺平了道路。

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