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新型钯(II)配合物的碳链长度对与 DNA 的相互作用和细胞毒性活性的影响。

Impact of the carbon chain length of novel palladium(II) complexes on interaction with DNA and cytotoxic activity.

机构信息

Laboratory of Coordination Chemistry, Shenyang University of Chemical Technology, Shenyang 110142, People's Republic of China.

出版信息

Inorg Chem. 2010 Apr 5;49(7):3261-70. doi: 10.1021/ic902176e.

Abstract

A series of Pd(II) complexes with a benzenealkyl dicarboxlate chain, with the formulas [Pd(L(n))(bipy)].mH(2)O (bipy = 2,2'-bipyridine, complex 1: L(1) = phenylmalonate, m = 2.5; complex 2: L(2) = benzylmalonate, m = 1; complex 3: L(3) = phenethylmalonate, m = 2; complex 4: L(4) = phenylpropylmalonate, m = 5), have been prepared in an attempt to correlate factors about the carbon chain of the compounds with DNA binding and cytotoxic activity. The binding of complexes with fish sperm DNA (FS-DNA) was carried out by UV absorption and fluorescence spectra. A gel electrophoresis assay demonstrated the ability of the complexes to cleave the pBR322 plasmid DNA. The cytotoxic effects of these complexes were examined on four cancer cell lines, HeLa, Hep-G2, KB, and AGZY-83a. The four complexes exhibited cytotoxic specificity and a significant cancer cell inhibitory rate. An apparent dependence of DNA-binding properties and cytotoxicity on the carbon chain length was obtained: the longer the carbon chain length, the higher the efficiency of DNA-binding and the greater the cytotoxicity.

摘要

一系列具有苯烷基二羧酸链的 Pd(II) 配合物,其化学式为[Pd(L(n))(bipy)].mH(2)O(bipy = 2,2'-联吡啶,配合物 1:L(1) = 苯丙二酸,m = 2.5;配合物 2:L(2) = 苄基丙二酸,m = 1;配合物 3:L(3) = 苯乙基丙二酸,m = 2;配合物 4:L(4) = 苯丙基丙二酸,m = 5),已被制备以尝试将化合物的碳链的因素与 DNA 结合和细胞毒性活性相关联。通过紫外吸收和荧光光谱法进行配合物与鱼精 DNA(FS-DNA)的结合。凝胶电泳试验证明了这些配合物切割 pBR322 质粒 DNA 的能力。这些配合物的细胞毒性作用在四种癌细胞系(HeLa、Hep-G2、KB 和 AGZY-83a)上进行了检查。四种配合物表现出细胞毒性特异性和显著的癌细胞抑制率。明显地发现 DNA 结合性质和细胞毒性与碳链长度有关:碳链长度越长,DNA 结合效率越高,细胞毒性越大。

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