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Synthesis of Platinum Complexes Coordinated by Sulfur Containing Compounds and their Anticancer Mechanism

含硫化合物配位铂配合物的合成及其抗癌机制

基本信息

批准号：
62550555
负责人：
TAKEAKI IIDA
金额：
$ 1.02万
依托单位：
Saitama University
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (C)
财政年份：
1987
资助国家：
日本
起止时间：
1987 至 1988
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-62550555/
关键词：
Platinum Complex Anticancer Activity Sulfur Containing Ligand 担体配位子 DNAとの相互作用

项目摘要

Cis-diamminedichloroplatinum (II) complex (cis-DDP) is widely utilized as an anticancer agent for clinical treatments of various cancers. It has been confirmed by many evidences that cis-DDP binds specifically with DNA in cancer cells to inhibit the replication of the DNA. Therefore, many investigations concerning novel platinum complexes with various carrier ligands have been developed to be used as anticancer agents. However, the study on the platinum complex coordinated with a ligand containing sulfur atoms has not been reported yet. in this paper, a novel platinum complex, dichloro-2-aminoethylsulfonyl-platinum (II), was synthesized. The structure of the platinum complex was analyzed by IR and ^<13>C-NMR spectra, elementary analysis and atomic absorption spectrophotometry. The investigations were also carried out on the interaction between the platinum complex and DNA constituent nucleosides by analyzing the UV difference spectra and the liberation rate of the chloride ions from the platinum complex. The isosbestic points were observed in the UV difference spectra for the platinum complex-nucleoside system. It was also found that two chloride ions were liberated from the platinum complex in the interaction with the nucleosides. The platinum complex was found to exhibit a specific anticancer activity against adriamycin resistant cancer cells.

顺式二胺二氯铂（II）配合物（cis-DDP）作为抗癌药物被广泛应用于各种癌症的临床治疗。许多证据证实，顺式ddp与癌细胞中的DNA特异性结合，抑制DNA的复制。因此，各种载体配体的新型铂配合物作为抗癌药物得到了广泛的研究。然而，含硫配体配体铂配合物的研究尚未见报道。本文合成了一种新型铂配合物二氯-2-氨基乙基磺酰基铂（II）。采用红外光谱、13>C-NMR谱、元素分析和原子吸收分光光度法对铂配合物的结构进行了分析。通过分析铂配合物的紫外差谱和氯离子的释放速率，对铂配合物与DNA核苷的相互作用进行了研究。在铂配合物-核苷体系的紫外差谱中观察到等吸点。还发现，在与核苷的相互作用中，铂络合物释放出两个氯离子。铂配合物被发现对阿霉素耐药的癌细胞表现出特定的抗癌活性。