Department of General and Inorganic Chemistry, Faculty of Chemistry, Aristotle University of Thessaloniki, P.O. Box 135, GR-54124 Thessaloniki, Greece.
J Inorg Biochem. 2009 Dec;103(12):1617-25. doi: 10.1016/j.jinorgbio.2009.08.011. Epub 2009 Sep 4.
The mononuclear nickel(II) complexes with the third-generation quinolone antibacterial agent sparfloxacin in the absence or presence of nitrogen donor heterocyclic ligands (1,10-phenanthroline or 2,2'-bipyridine) have been synthesized and characterized. The experimental data suggest that sparfloxacin acts as deprotonated bidentate ligand coordinated to Ni(II) ion through the ketone and carboxylato oxygens. The crystal structure of (1,10-phenanthroline)bis(sparfloxacinato) nickel(II), 2 has been determined by X-ray crystallography. The cyclic voltammograms of the complexes recorded in dmso solution and in 1/2 dmso/buffer (containing 150 mM NaCl and 15 mM trisodium citrate at pH 7.0) solution have shown that in the presence of CT DNA they can bind to CT DNA by the intercalative binding mode. UV study of the interaction of the complexes with calf-thymus DNA (CT DNA) has shown that the complexes can bind to CT DNA and 2 exhibits the highest binding constant to CT DNA. 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 for the intercalative binding site. The antimicrobial activity of the complexes has been tested on three different microorganisms and has revealed that the inhibition provided by the complexes is slightly decreased in comparison to free sparfloxacin. The complexes exhibit good binding propensity to human and bovine serum albumin proteins having relatively high binding constant values.
在没有或存在氮供杂环配体（1,10-菲咯啉或 2,2'-联吡啶）的情况下，合成并表征了单核镍（II）配合物与第三代喹诺酮类抗菌剂司帕沙星。实验数据表明，司帕沙星通过酮和羧基氧原子作为去质子的双齿配体与 Ni(II)离子配位。通过 X 射线晶体学确定了（1,10-菲咯啉）双（司帕沙星）镍（II），2 的晶体结构。在 dmso 溶液中和 1/2 dmso/缓冲液（在 pH 7.0 时含有 150 mM NaCl 和 15 mM 三磷酸钠柠檬酸钠）溶液中记录的配合物的循环伏安法表明，在存在 CT DNA 的情况下，它们可以通过嵌入结合模式与 CT DNA 结合。配合物与小牛胸腺 DNA（CT DNA）相互作用的 UV 研究表明，配合物可以与 CT DNA 结合，并且 2 对 CT DNA 具有最高的结合常数。与溴化乙锭（EB）的竞争研究表明，配合物可以置换 DNA 结合的 EB，表明它们与 DNA 结合是与 EB 竞争嵌入结合位点的强竞争。配合物的抗菌活性已在三种不同的微生物上进行了测试，结果表明与游离司帕沙星相比，配合物提供的抑制作用略有降低。配合物对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。
