[Effect of platinum derivatives on microsomal NADPH-oxidoreductase activity]

I A Shchepetkin¹, V M Plotnikov, V T Kagiia

¹Institute of Oncology, Tomsk Research Center, Siberian Branch of Russian Academy of Medical Sciences, per. Kooperativnyi 5, Tomsk 634001, Russia.

Voprosy Meditsinskoi Khimii

|November 6, 2001

Abstract:

The influence of platinum derivatives, cisplatin (cis-diamminedichloroplatinum) and imidazolplatin (cis-diimidazoledichloroplatinum) on the activity of rat liver microsomal NADPH-oxidoreductases was investigated in vitro using spectrophotometrical and chemiluminometrical methods. In the range of concentrations from 1 to 12 microM cisplatin inhibited NADPH-cytochrome c-reductase activity and NADPH/lucigenin-dependent chemiluminescence of microsomes. The 3 microM cisplatin decreased the NADPH-dependent reductase activity by 50%. At concentrations less than 2.5 mM sanazole (drug AK-2123) did not prevent the inhibiting influence of cisplatin on microsomal NADPH-dependent reductases. Imidazolplatin insignificantly inhibited NADPH-reductases. It is concluded that negligible inhibiting effect of imidazolplatin on microsomal NADPH-oxidoreductase allows us to consider this platinum derivative as a promising compound for further experimental trials as anticancer drug with low toxic action on the normal tissues of an organism.

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Abstract:

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