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Synthesis, characterization and biological activity of trans-platinum(II) and trans-platinum(IV) complexes with 4-hydroxymethylpyridine
被引:21
|作者:
Martínez, A
Lorenzo, J
Prieto, MJ
de Llorens, R
Font-Bardia, M
Solans, X
Avilés, FX
Moreno, V
机构:
[1] Univ Barcelona, Dept Quim Inorgan, E-08028 Barcelona, Spain
[2] Univ Autonoma Barcelona, Inst Biotecnol & Biomed, E-08193 Barcelona, Spain
[3] Univ Barcelona, Dept Microbiol, E-08028 Barcelona, Spain
[4] Univ Girona, Dept Biol, Girona 17071, Spain
[5] Univ Barcelona, Dept Cristallografia Mineral & Diposits Minerals, E-08028 Barcelona, Spain
来源:
关键词:
ab initio calculations;
antitumor agents;
apoptosis;
bioinorganic chemistry;
DNA;
platinum;
D O I:
10.1002/cbic.200500108
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 synthesis and chemical characterisation of two new trans-platnium complexes, trans-[PtCl4NH3(4-hydroxymethylpyridine)] (1) and trans-[PtCl4NH3(4-hydroxymethylpyridine)] (2) are described. Their ability to interact with 5'-GMP by themselves and in the presence of reducing agents in the case of trans-[PTCl4NH3(4-hydroxymethylpyridine)] were tested. Circular dichroism, electrophoretic mobility in agarose gel, and atomic force microscopy studies showed that the interaction of complex 1 with DNA is stronger than that of complex 2. Cytotoxicity tests against HL-60 tumor cells also showed higher activity for trans[PtCl2NH3(4-hydroxymethylpyridine)] than for trans-[PtCl4NH3(4-hydroxymethylpyridine)]. Complex I presents similar behavior to cisplatin, but with a lower IC50 at 24 h. Complex I also showed high apoptosis induction.
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页码:2068 / 2077
页数:10
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