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新型双核钴(III)配合物的合成、表征、细胞毒性活性及与 2-乙酰吡啶和丙二酰二肼缩合产物的 DNA 结合性质。

Synthesis, characterization, cytotoxic activity and DNA binding properties of the novel dinuclear cobalt(III) complex with the condensation product of 2-acetylpyridine and malonic acid dihydrazide.

机构信息

Faculty of Chemistry, University of Belgrade, Studentski trg 12-16, 11000 Belgrade, Serbia.

出版信息

J Inorg Biochem. 2011 Sep;105(9):1196-203. doi: 10.1016/j.jinorgbio.2011.05.024. Epub 2011 Jun 13.

Abstract

A novel dinuclear cobalt(III) complex with the condensation product of 2-acetylpyridine and malonic acid dihydrazide, N',N'(2)-bis[(1E)-1-(2-pyridyl)ethylidene]propanedihydrazide was synthesized and characterized by elemental analysis, spectroscopy (NMR and infrared), and X-ray crystal analysis. The complex showed a moderate activity towards Artemia salina. The highest cytotoxic potential of the complex was observed on the epithelial breast cancer (MDA-361) cell line. The investigated complex induced apoptosis, the early apoptotic cells comprising 28.18%, compared to 5.64% of control cells in the same phase. The interaction of the complex with calf thymus DNA (CT-DNA) was monitored by blue shift and hyperchromism in the UV-vis spectra. The observed intrinsic binding constant (K(b)=4.2×10(5)M(-1)) together with structural analysis of the complex indicate the groove binding.

摘要

一种新型双核钴(III)配合物,其配体是 2-乙酰吡啶和丙二酰二酰肼的缩合产物,N',N'-(2)-双[(1E)-1-(2-吡啶基)亚乙基]丙二酰二酰肼,通过元素分析、光谱学(NMR 和红外)和 X 射线晶体分析进行了合成和表征。该配合物对卤虫表现出中等的活性。该配合物的最高细胞毒性潜力出现在上皮性乳腺癌(MDA-361)细胞系上。所研究的配合物诱导了细胞凋亡,与同阶段的 5.64%的对照细胞相比,早期凋亡细胞占 28.18%。配合物与小牛胸腺 DNA(CT-DNA)的相互作用通过紫外可见光谱中的蓝移和增色来监测。观察到的固有结合常数(K(b)=4.2×10(5)M(-1))以及对配合物结构的分析表明其为沟结合。

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