多吡啶钌配合物[(Phen)_2Ru(dppz)](PF_6)_2的抗菌活性及机制研究  

Analysis of antibacterial activity and mechanism of polypyridyl ruthenium complex

作　　者：刘汉杰[1] 付彬[1] 付爱玲[1] 付琛[1] LIU Han-jie FU-Bin FU Ai-ling FU Chen(College of Pharmaceutical Sciences, Southwest University, Chongqing 400716, China)

机构地区：[1]西南大学药学院,重庆400716

出　　处：《中国药理学通报》2016年第9期1249-1253,共5页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No 81273416);教育部高校基本科研业务费(No XDJK2013A030);教育部回国人员启动基金(No 2012-940);教育部新世纪优秀人才支持计划资助

摘　　要：目的研究多吡啶钌配合物[(Phen)_2Ru(dppz)](PF_6)_2的抗菌活性,并进一步探讨其作用机制。方法采用最小抑菌浓度(MIC)以及最小杀菌浓度(MBC),测定无机配合物[(Phen)_2Ru(dppz)](PF_6)_2的抗菌活性。为了阐明其抗菌机制,首先利用配合物自身荧光特性和核酸染料对DNA的竞争性结合所导致的荧光强度变化,以确定配合物与DNA的结合能力;然后通过DNA凝胶电泳,检测配合物与细菌基因组DNA结合后产生的效果以检测抗菌活性的机制。结果多吡啶钌配合物[(Phen)_2Ru(dppz)](PF_6)_2对大肠杆菌以及金黄色葡萄球菌具有较强的抗菌活性,最小抑菌浓度达0.2~0.4 g·L^(-1)。荧光检测显示,配合物能够与细菌DNA发生结合,以此为基础,配合物能够干扰细菌的转录过程,抑制细菌生长。结论本研究证明了多吡啶钌配合物[(Phen)_2Ru(dppz)](PF_6)_2的抗菌活性及作用机制,为其进一步开发奠定了基础。Aim To analyze the antibiotic activity and mechanism of a polypyridyl ruthenium complex. Methods The antibacterial activity of [（ Phen）_2Ru（ dppz） ]（ PF_6）_2was determined by MIC and MBC value.Based on a fluorescent activity of this complex,the fluorescent emission spectra was used to analyze the combination of complex to DNA. Then the competition combination was analyzed between complex and Gold View to DNA. Lastly,gel electrophoresis of DNA was applied to detect the combination situation between complex and DNA. Results This kind of polypyridyl ruthenium complex showed a significant antibacterial activity with a minimum antibacterial conentration of0. 2 ~ 0. 4 g ·L^（-1）. That was caused by the combination and distortion of DNA due to the activity of this complex. Conclusion The antibacterial activity and the mechanism of antibacterial activity about[（ Phen）_2Ru（ dppz） ]（ PF_6）_2are confirmed in this research,which provides a good foundation for the development of such class of compound.

关 键 词：多吡啶钌配合物 抑菌活性 荧光检测 代谢活性 DNA结合 DNA降解 

分 类 号：R342.3[医药卫生—基础医学] R378.11