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一种新型抗肿瘤钯(II)配合物与小牛胸腺DNA的结合研究。

Binding studies of a novel antitumor palladium(II) complex to calf thymus DNA.

作者信息

Mansouri-Torshizi H, Saeidifar M, Divsalar A, Saboury A A

机构信息

Department of Chemistry, University of Sistan and Baluchestan, Zahedan, Iran.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2011 Jun;30(6):405-22. doi: 10.1080/15257770.2011.586008.

DOI:10.1080/15257770.2011.586008
PMID:21780907
Abstract

The interaction of new 1, 10-phenanthrolineoctyldithiocarbamatopalladium (II) nitrate with DNA from calf thymus was investigated at 300 and 310 K in a Tris-HCl buffer of pH 7.0 medium containing 20 mM sodium chloride. This water soluble, square planar Pd(II) complex has been synthesized and spectroscopic (electronic, infrared, and nuclear magnetic resonance) and elemental analysis of the complex are discussed. This complex shows greater growth inhibitory activity against human tumor cell line K562 than cisplatin. Results of UV-visible studies show that the complex exhibits cooperative binding with DNA and denatures the DNA at an extremely low concentration (∼11.98 μM). Fluorescence studies reveal that the mode of binding of this complex with DNA seems to be intercalation. The results of sephadex G-25 column show that the binding of metal complex with DNA is so strong that it does not readily break. Several binding and thermodynamic parameters are also described. They may shed light on the mechanisms of interaction of this agent with DNA, which should be quite different from that of cisplatin.

摘要

在300K和310K温度下,于pH 7.0、含有20 mM氯化钠的Tris-HCl缓冲介质中,研究了新型1,10-菲咯啉辛基二硫代氨基甲酸钯(II)硝酸盐与小牛胸腺DNA的相互作用。已合成了这种水溶性的平面正方形钯(II)配合物,并对该配合物进行了光谱分析(电子、红外和核磁共振)以及元素分析。该配合物对人肿瘤细胞系K562显示出比顺铂更强的生长抑制活性。紫外可见光谱研究结果表明,该配合物与DNA表现出协同结合,并在极低浓度(约11.98 μM)下使DNA变性。荧光研究表明,该配合物与DNA的结合模式似乎是嵌入。葡聚糖G-25柱层析结果表明,金属配合物与DNA的结合非常牢固,不易断裂。还描述了几个结合和热力学参数。它们可能有助于阐明该试剂与DNA相互作用的机制,这应该与顺铂的机制有很大不同。

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