Department of General and Inorganic Chemistry, Faculty of Chemistry, Aristotle University of Thessaloniki, PO Box 135, GR-54124 Thessaloniki, Greece.
Bioorg Med Chem. 2010 Apr 1;18(7):2678-85. doi: 10.1016/j.bmc.2010.02.021. Epub 2010 Feb 18.
Zinc mononuclear complexes with the second-generation quinolone antibacterial drug enrofloxacin in the absence or presence of a nitrogen donor heterocyclic ligand 1,10-phenanthroline or 2,2'-bipyridine have been synthesized and characterized. Enrofloxacin is on deprotonated mode acting as a bidentate ligand coordinated to zinc ion through the ketone and a carboxylato oxygen atoms. The crystal structure of bis(enrofloxacinato)(1,10-phenanthroline)zinc(II), 2, has been determined by X-ray crystallography. The biological activity of the complexes has been evaluated by examining their ability to bind to calf-thymus DNA (CT DNA) with UV and fluorescence spectroscopies. UV studies of the interaction of the complexes with DNA have shown that they can bind to CT DNA and the DNA binding constants have been calculated. Competitive studies with ethidium bromide (EB) have shown that the complexes exhibit the ability to displace the DNA-bound EB indicating that they bind to DNA in strong competition with EB for the intercalative binding site. The complexes exhibit good binding propensity to human and bovine serum albumin proteins having relatively high binding constant values.
在不存在或存在氮供杂环配体 1,10-菲咯啉或 2,2'-联吡啶的情况下,合成并表征了具有第二代喹诺酮类抗菌药物恩诺沙星的锌单核配合物。恩诺沙星处于去质子化模式,通过酮和羧基氧原子与锌离子配位,作为双齿配体。通过 X 射线晶体学确定了双(恩诺沙星)(1,10-菲咯啉)锌(II),2 的晶体结构。通过紫外和荧光光谱研究了配合物与小牛胸腺 DNA(CT DNA)结合的能力,评估了其生物活性。与 DNA 的相互作用的 UV 研究表明,它们可以与 CT DNA 结合,并且已经计算了 DNA 结合常数。与溴化乙锭(EB)的竞争性研究表明,这些配合物具有取代 DNA 结合的 EB 的能力,表明它们与 DNA 结合具有很强的竞争性,与 EB 竞争插入结合位点。这些配合物与人血清白蛋白和牛血清白蛋白具有良好的结合倾向,具有相对较高的结合常数值。