Department of General and Inorganic Chemistry, Faculty of Chemistry, Aristotle University of Thessaloniki, P.O. Box 135, GR-54124 Thessaloniki, Greece.
J Inorg Biochem. 2011 Jan;105(1):63-74. doi: 10.1016/j.jinorgbio.2010.09.007. Epub 2010 Oct 1.
The nickel(II) complexes with the second-generation quinolone antibacterial agent enrofloxacin in the presence or absence of the nitrogen-donor heterocyclic ligands 1,10-phenanthroline, 2,2'-bipyridine or pyridine have been synthesized and characterized. Enrofloxacin acts as bidentate ligand coordinated to Ni(II) ion through the ketone oxygen and a carboxylato oxygen. The crystal structure of (1,10-phenanthroline)bis(enrofloxacinato)nickel(II) has been determined by X-ray crystallography. UV study of the interaction of the complexes with calf-thymus DNA (CT DNA) has shown that they bind to CT DNA and bis(pyridine)bis(enrofloxacinato)nickel(II) exhibits the highest binding constant to CT DNA. The cyclic voltammograms of the complexes have shown that in the presence of CT DNA the complexes can bind to CT DNA by the intercalative binding mode which has also been verified by DNA solution viscosity measurements. Competitive study with ethidium bromide (EB) has shown that the complexes can displace the DNA-bound EB indicating that they bind to DNA in strong competition with EB. The complexes exhibit good binding propensity to human or bovine serum albumin protein having relatively high binding constant values. The biological properties of the complexes have been evaluated in comparison to the corresponding Zn(II) enrofloxacinato complexes as well as Ni(II) complexes with the first-generation quinolone oxolinic acid.
在存在或不存在氮供杂环配体 1,10-菲啰啉、2,2'-联吡啶或吡啶的情况下，合成并表征了与第二代喹诺酮类抗菌剂恩诺沙星的镍（II）配合物。恩诺沙星作为双齿配体通过酮氧和羧基氧与 Ni(II)离子配位。通过 X 射线晶体学确定了（1,10-菲啰啉）双（恩诺沙星）镍（II）的晶体结构。配合物与小牛胸腺 DNA（CT DNA）相互作用的 UV 研究表明，它们与 CT DNA 结合，并且双（吡啶）双（恩诺沙星）镍（II）对 CT DNA 具有最高的结合常数。配合物的循环伏安法表明，在 CT DNA 的存在下，配合物可以通过嵌入结合模式与 CT DNA 结合，这也通过 DNA 溶液粘度测量得到了验证。与溴化乙锭（EB）的竞争研究表明，配合物可以取代 DNA 结合的 EB，表明它们与 DNA 结合具有很强的与 EB 的竞争能力。配合物与人或牛血清白蛋白蛋白具有良好的结合倾向，具有相对较高的结合常数值。将配合物的生物性质与相应的 Zn(II)恩诺沙星配合物以及与第一代喹诺酮类药物氧氟沙星的 Ni(II)配合物进行了比较评估。
