首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, characterization and in vitro biological activity studies of Cu-M (M = Cu2+, Co2+, Ni2+, Mn2+, Zn2+) bimetallic complexes.
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Synthesis, characterization and in vitro biological activity studies of Cu-M (M = Cu2+, Co2+, Ni2+, Mn2+, Zn2+) bimetallic complexes.

机译:Cu-M(金属= Cu2 +,Co2 +,Ni2 +,Mn2 +,Zn2 +)双金属配合物的合成,表征和体外生物学活性研究。

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摘要

Six new bimetallic complexes of the type CuCu, CuCo, CuNi, CuZn and CuMn were prepared. The structures of these complexes and the ligand have been proposed on the basis of FAB mass, elemental analysis, UV-vis, IR, EPR and CV studies. All the complexes completely cleave pBS (SK-) DNA at a concentration of 10 microM; however, even at lower concentrations of 2 microM and 0.1 microM, the complexes (I and Ia) showed partial cleavage. The results of the fluorescence binding studies of the metal complexes with CT-DNA showed that the presence of aliphatic ligands added additional binding effects including electrostatic, hydrogen binding and vander Waals interactions. Complexes (I, Ia) showed 50% inhibition of COX-1 and COX-2 activities at as low a concentration as 12.5 microM, 13.5 microM, 14 microM and 14.5 microM. Inhibition assay of top I and top II by different complexes in mutant yeast strains (JN394, JN394 t(-1) and JN394 t(2-5)) with all the complexes showed significant inhibition of topoisomerase at 5 microM concentration. Complexes I and Ia exhibited good anti-microbial activities against all human pathogens tested except Klebsiella pneumoniae. The following studies showed that among the synthesized bimetallic complexes, complexes I and Ia seem to be promising candidates possessing DNA cleavage activities besides anti-microbial and anti-inflammatory properties to serve as chemical nucleases and chemotherapeutic agents.
机译:制备了六个新的CuCu,CuCo,CuNi,CuZn和CuMn型双金属配合物。这些配合物和配体的结构是根据FAB质量,元素分析,UV-vis,IR,EPR和CV研究提出的。所有的复合物都以10 microM的浓度完全切割pBS(SK-)DNA。然而,即使在2 microM和0.1 microM的较低浓度下,复合物(I和Ia)也显示出部分裂解。金属络合物与CT-DNA的荧光结合研究结果表明,脂肪族配体的存在增加了额外的结合作用,包括静电,氢结合和范德华相互作用。配合物(Ⅰ,Ⅰa)在低至12.5 microM,13.5 microM,14 microM和14.5 microM的浓度下显示出对COX-1和COX-2活性的50%抑制。突变酵母菌株(JN394,JN394 t(-1)和JN394 t(2-5))中所有复合物的不同复合物对前I和前II的抑制试验表明,在5 microM浓度下拓扑异构酶具有明显的抑制作用。复合物I和Ia对除肺炎克雷伯菌外的所有人类病原体均显示良好的抗微生物活性。以下研究表明,在合成的双金属配合物中,配合物I和Ia似乎有望成为具有DNA裂解活性的候选物,并且具有抗微生物和抗炎特性,可以用作化学核酸酶和化学治疗剂。

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