DNA interaction and antitumor activity of a Pt(III) derivative of 2-mercaptopyridine

被引:36
作者
Cervantes, G
Marchal, S
Prieto, MJ
Pérez, JM
González, VM
Alonso, C
Moreno, V
机构
[1] Univ Barcelona, Dept Quim Inorgan, E-08028 Barcelona, Spain
[2] Univ Barcelona, Dept Microbiol, E-08028 Barcelona, Spain
[3] Univ Autonoma Madrid, Ctr Biol Mol Severo Ochoa, E-28049 Madrid, Spain
关键词
2-mercaptopyridine; Pt-mercaptopyridine complex; DNA-Pt-mercaptopyridine interaction; Pt(III) complex antitumor activity;
D O I
10.1016/S0162-0134(99)00191-9
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The complex [Pt-2(Spy(-))(4)Cl-2], where Spy(-) is deprotonated 2-mercaptopyridine, was prepared and analyzed spectroscopically. A single signal in the Pt-195 NMR spectrum indicates the equivalence of the two Pt(III) ions. The interaction of this complex with DNA was studied by circular dichroism and the modifications caused by the complex in plasmid pBR322 DNA were imaged by atomic force microscopy. Preliminary results showed higher activity against HeLa and U937 tumor lines for the Pt-2-mercaptopyridine complex in comparison with cisplatin. The values of LC50 were lower than those obtained for cisplatin. Promising perspectives or this compound are expected due to its similarity with the analogous Pt and 2-mercaptopyrimidine antitumor compound. (C)1999 Elsevier Science Inc. All rights reserved.
引用
收藏
页码:197 / 203
页数:7
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