Department of General and Inorganic Chemistry, Faculty of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece.
Department of General and Inorganic Chemistry, Faculty of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece.
J Inorg Biochem. 2021 Apr;217:111357. doi: 10.1016/j.jinorgbio.2021.111357. Epub 2021 Jan 24.
The interaction of copper(II) with the non-steroidal anti-inflammatory drug sodium meclofenamate (Na-mclf) in the presence or absence of the nitrogen-donor co-ligands pyridine (py) or 2,2'-bipyridylamine (bipyam), yielded the novel Cu(II) complexes [Cu(mclf-O,O')(MeOH)]·2MeOH (1·2MeOH), [Cu(mclf-O)(py)]·HO·0.5MeOH (2·HO·0.5MeOH) and [Cu(mclf-O,O')(bipyam)] (3). The characterization of the complexes was achieved by various techniques, including single-crystal X-ray crystallography. In order to study the binding mode and strength of the complexes to calf-thymus (CT) DNA, various techniques were employed which suggested intercalation between the DNA-bases as the most possible interaction mode. Competitive studies with ethidium bromide (EB) revealed the ability of the complexes to displace the EB from the EB-DNA adduct, verifying the intercalative binding mode. The affinity of the complexes to bovine and human serum albumin proteins (SAs) was investigated by fluorescence emission spectroscopy and the corresponding binding constants bear relatively high values, showing that the complexes bind tightly and possibly reversibly to SAs. The antioxidant activity of the complexes against 1,1-diphenyl-picrylhydrazyl (DPPH), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radicals and the ability to reduce HO proved to be of significant magnitude. The in vitro inhibitory activity against the enzymes acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) was evaluated, in order to assess the anticholinergic ability of the complexes, which appeared promising.
在存在或不存在氮供体辅助配体吡啶（py）或 2,2'-联吡啶胺（bipyam）的情况下，铜（II）与非甾体抗炎药甲氯芬那酸（Na-mclf）的相互作用，生成了新型 Cu(II)配合物 [Cu(mclf-O,O')(MeOH)]·2MeOH (1·2MeOH)、[Cu(mclf-O)(py)]·HO·0.5MeOH (2·HO·0.5MeOH) 和 [Cu(mclf-O,O')(bipyam)] (3)。通过各种技术，包括单晶 X 射线晶体学，对配合物进行了表征。为了研究配合物与小牛胸腺（CT）DNA 的结合模式和强度，采用了各种技术，这些技术表明，碱基之间的嵌入是最可能的相互作用模式。与溴化乙锭（EB）的竞争研究表明，配合物能够从 EB-DNA 加合物中置换 EB，验证了嵌入结合模式。通过荧光发射光谱研究了配合物与牛和人血清白蛋白蛋白（SA）的亲和力，相应的结合常数具有相对较高的值，表明配合物与 SA 紧密且可能可逆地结合。配合物对 1,1-二苯基-2-苦基肼基（DPPH）、2,2'-联氮双（3-乙基苯并噻唑啉-6-磺酸）（ABTS）自由基的抗氧化活性和还原 HO 的能力被证明具有显著的重要性。评估了配合物对乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BuChE）的体外抑制活性，以评估配合物的抗胆碱能能力，结果表明这是有希望的。
