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八面体钌(II)多吡啶配合物作为抗分枝杆菌的抗菌剂。

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

作者信息

Liao Guojian, Ye Zhengyuan, Liu Yunlu, Fu Bin, Fu Chen

机构信息

College of Pharmaceutical Sciences, Southwest University, Chongqing, China.

出版信息

PeerJ. 2017 Apr 27;5:e3252. doi: 10.7717/peerj.3252. eCollection 2017.

Abstract

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 . In this study, susceptibilities of to the octahedral ruthenium(II) polypyridyl complexes, {[(bpy)Ru] (PF) (bpy = 2,2'-bipyridine)}, {(phen)Ru(dppz) (phen = 1,10-phenanthroline, dppz = dipyridophenazine)} and {(phen)Ru} were measured by broth microdilution and reported as the MIC values. Toxicities of complex to LO2 and hepG2 cell lines were also measured. Complex inhibited the growth of with MIC value of 2 µg/mL, while complex was bactericidal with MIC value of 26 µg/mL. Furthermore, the bactericidal activity of complex was dependent on reactive oxygen species production. Complex  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 infection.

摘要

结核病是世界上最致命的传染病之一,每年导致150万人死亡。发现对其具有强效活性的新型化合物势在必行。在本研究中,通过肉汤微量稀释法测定了结核分枝杆菌对八面体钌(II)多吡啶配合物{(bpy)Ru(bpy = 2,2'-联吡啶)}、{(phen)Ru(dppz)(phen = 1,10-菲咯啉,dppz =二吡啶并吩嗪)}和{(phen)Ru}的敏感性,并将其报告为MIC值。还测定了配合物对LO2和hepG2细胞系的毒性。配合物抑制结核分枝杆菌生长的MIC值为2 µg/mL,而配合物具有杀菌作用,MIC值为26 µg/mL。此外,配合物的杀菌活性取决于活性氧的产生。配合物在高达64 µg/mL的浓度下对LO2和hepG2细胞系均无细胞毒性,为作为治疗结核感染的新型抗菌剂进行进一步优化和开发铺平了道路。

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