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Synthesis, Characterization of novel Cu(II) complexes of isatin derivatives as potential cytotoxicity, DNA binding, cleavage and antibacterial agents

机译:合成,表征新型的Isatin衍生物Cu(II)配合物作为潜在的细胞毒性,DNA结合,裂解和抗菌剂

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Schiff-base ligands are potential anti-cancer, anti-bacterial and anti-viral agents and this activity tends to increase in metal(II) Schiff-base complexes. Some oxindole-Schiff base copper(II) complexes have shown potential antitumor activity towards deferent cells, inducing apoptosis in a process modulated by the ligand. Here, six novel copper(II) complexes with schiff base ligands were isolated and characterized by IR, 1H-NMR, UV-visible , CV, EPR and ESI-Mass. All the complexes are soluble in DMF and DMSO. Elemental analysis and molar conductance values indicate that the complexes are non-electrolytes. All the complexes adopt octahedral geometry around the metal ions. DNA binding activities of the complexes L1-Cu to L6-Cu a spectroscopy are studied by UV-vis. and also cleavage studies of complexes have been done by agarose gel electrophoresis method. In-vitro biological activities of the free ligands and its Cu(II) complexes are screened against few Gram +ve and Gram –ve bacteria by disc diffusion technique. Cytotoxicity experiments carried out toward human Liver HepG2 cells confirmed its pro apoptosis property. Interestingly, compounds, L4-Cu and L6-Cu were found to be excellent anticancer activity against HepG2: liver cells and L4-Cu was most significant cytotoxicity activity against MAIT cells .
机译:席夫碱配体是潜在的抗癌,抗菌和抗病毒药物,这种活性在席夫碱金属(II)配合物中趋于增加。一些羟吲哚-席夫碱铜(II)配合物已显示出对不同细胞的潜在抗肿瘤活性,在配体调节的过程中诱导凋亡。在这里,分离出六个具有席夫碱配体的新型铜(II)配合物,并通过红外,1 H-NMR,紫外可见,CV,EPR和ESI-Mass进行表征。所有复合物均溶于DMF和DMSO。元素分析和摩尔电导值表明该络合物是非电解质。所有的配合物在金属离子周围都采用八面体几何形状。通过UV-vis研究了配合物L1-Cu与L6-Cu的光谱的DNA结合活性。并且还通过琼脂糖凝胶电泳法进行了复合物的裂解研究。通过圆盘扩散技术,针对少数革兰氏+ ve和革兰氏–ve细菌筛选了游离配体及其Cu(II)配合物的体外生物学活性。对人肝HepG2细胞进行的细胞毒性实验证实了其促凋亡特性。有趣的是,发现化合物L4-Cu和L6-Cu对HepG2具有优异的抗癌活性:肝细胞,而L4-Cu对MAIT细胞具有最显着的细胞毒性。

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