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首页> 外文期刊>Acta Chimica Slovenica >New Bioactive Heteroleptic Copper(II) Carboxylates: Structure, Enzymatic and DNA-Binding Studies
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New Bioactive Heteroleptic Copper(II) Carboxylates: Structure, Enzymatic and DNA-Binding Studies

机译:新的具有生物活性的多杀菌铜羧酸盐:结构,酶和DNA结合研究

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摘要

Two new binuclear O-bridged copper(II) carboxylates with chemical formulas [Cu 2 (3-ClC 6 H 4 CH 2 COO) 4 (phen) 2 ] ( 1 ) and [Cu 2 (3-ClC 6 H 4 CH 2 COO) 4 (bipy) 2 ] ( 2 ) where phen = 1,10-phenanthroline and bipy = 2,2′-bipyridine have been synthesized and characterized by FT-IR, UV-Visible spectroscopy, CHN analysis and single crystal XRD. The results revealed distorted square pyramidal geometry around each copper atom of 1 and 2 . The DNA interaction studies showed strong binding with K b = 5.07×10 3 and 4.62×10 3 M –1 for 1 and 2 , respectively. Both complexes showed strong enzyme inhibition, i.e., 70 % and 90 % for α -glucosidase with IC 50 = 34.6 and 30.1 μM for 1 and 2 , respectively, where acarbose was employed as control. However, both the complexes were found inactive against α -amylase. Using galantamine hydrobromide as control, 1 showed moderate inhibition activity (47 %) with IC 50 = 179.4 μM for acetylcholine esterase whereas 2 showed strong inhibition activity (76 %) with IC 50 = 95.8 μM for butyrylcholine esterase. The data reflects active anti-diabetic and anti-Alzheimer’s nature of the synthesized complexes.
机译:具有化学式[Cu 2(3-ClC 6 H 4 CH 2 COO)4(phen)2](1)和[Cu 2(3-ClC 6 H 4 CH 2)的两种新的双核O桥铜(II)羧酸盐已合成了COO)4(bipy)2](2),其中phen = 1,10-菲咯啉和bipy = 2,2'-联吡啶,并通过FT-IR,紫外可见光谱,CHN分析和单晶XRD进行了表征。结果表明,围绕1和2的每个铜原子扭曲了方形锥体形状。 DNA相互作用研究表明,Kb = 5.07×10 3和4.62×10 3 M –1分别与1和2具有强结合力。两种复合物均显示出强烈的酶抑制作用,即α-葡萄糖苷酶的抑制率为70%和90%,其中1和2的IC 50分别为34.6和30.1μM,其中使用阿卡波糖作为对照。然而,发现两种复合物均对α-淀粉酶无活性。使用加兰他敏氢溴酸盐作为对照,1显示对乙酰胆碱酯酶的中等抑制活性(47%),IC 50 = 179.4μM,而2显示对丁酰胆碱酯酶的强抑制活性(76%),IC 50 = 95.8μM。数据反映了合成复合物的活性抗糖尿病和抗阿尔茨海默氏症性质。

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