Ni(Ⅱ) Ternary Complex Based on Antimicrobial Drug Enoxacin: Synthesis and Biological Properties  

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作  者:Wanyun Huang Shilin Kong Zhongchang Wang Chengxue Pan Hailiang Zhu 

机构地区:[1]State Key Laboratory of Pharmaceutical Biotechnology,Nanjing University,Nanjing 210093,China [2]Department of Pharmacology,Guilin Medical University,Guilin,Guizhou 541004,China [3]Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources(Guangxi Normal University),Ministry of Education of China,Guilin,Guizhou 541004,China

出  处:《Chinese Journal of Chemistry》2014年第11期1169-1175,共7页中国化学(英文版)

基  金:The authors thank the financial support by Jiangsu National Science Foundation(No.BK2009239);The project was also funded by the Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources(Guangxi Normal University);the Ministry of Education of China(No.CMEMR2013-B02).

摘  要:First Ni(Ⅱ)ternary complex using the quinolone antibacterial agent enoxacin(HEn)as ligand and 1,10-phenanthroline as co-ligand has been synthesized and characterized.It is a mononuclear structure,in which enoxacin acts as a bidentate ligand bound to the metal through the ketone oxygen and a carboxylate oxygen atom.The complex exhibited good binding propensity to human and bovine serum albumin proteins having relatively high binding constants(6.40×10^(4) and 7.12×10^(4),respectively).The investigation of the interaction of the complex with calf-thymus(CT)DNA has been performed with UV and circular dichroism(CD)spectroscopies,indicating that they bind to CT DNA probably by the intercalative binding mode.The binding constant(K_(b))of the complex with CT DNA calculated with UV is 2.03×10^(5),which is higher than that of free enoxacin drug(2.09×10^(4))and even higher than that of typical intercalation indicator(1.23×10^(5))of ethidium bromide(EB).Fluorescence competitive studies with EB have revealed that the complex exhibited the ability to displace the DNA-bound EB using the intercalative binding site.In addition,the antimicrobial activity showed that the complex exhibited a little bit good inhibition(MIC=1.843μg•mL^(-1))against B.subtilis than free HEn.

关 键 词:enoxacin QUINOLONES Ni(Ⅱ)complex biological evaluation 

分 类 号:O62[理学—有机化学]

 

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