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

被引:4
作者
Huang, Wanyun [1 ,2 ]
Kong, Shilin [3 ]
Wang, Zhongchang [1 ]
Pan, Chengxue [3 ]
Zhu, Hailiang [1 ]
机构
[1] Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Jiangsu, Peoples R China
[2] Guilin Med Univ, Dept Pharmacol, Guilin 541004, Guizhou, Peoples R China
[3] Guangxi Normal Univ, Minist Educ China, Key Lab Chem & Mol Engn Med Resources, Guilin 541004, Guizhou, Peoples R China
基金
美国国家科学基金会;
关键词
enoxacin; quinolones; Ni(II) complex; biological evaluation; CRYSTAL-STRUCTURE; COPPER(II) COMPLEX; DNA-BINDING; ANTIBACTERIAL; QUINOLONE; CYTOTOXICITY; NICKEL(II); CIPROFLOXACIN; NORFLOXACIN; COBALT(II);
D O I
10.1002/cjoc.201400420
中图分类号
O6 [化学];
学科分类号
0703 ;
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 (6.40x10(4) and 7.12x10(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 2.03x10(5), which is higher than that of free enoxacin drug (2.09x10(4)) and even higher than that of typical intercalation indicator (1.23x10(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=1.843 (gmL(-1)) against B. subtilis than free HEn.
引用
收藏
页码:1169 / 1175
页数:7
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