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VRÁNOVÁ, I. MOSEROVÁ, M. HODEK, P. KIZEK, R. FREI, E. STIBOROVÁ, M.
Originální název
The Anticancer Drug Ellipticine Induces Cytochromes P450 1A1, 1A2 and 3A, Cytochrome b(5) and NADPH:Cytochrome P450 Oxidoreductase in Rat Liver, Kidney and Lung
Typ
článek v časopise ve Web of Science, Jimp
Jazyk
angličtina
Originální abstrakt
The antineoplastic alkaloid ellipticine is a prodrug, the pharmacological efficiency of which is dependent on its cytochrome P450 (CYP)- and/or peroxidase-mediated activation in target tissues. Using the Western blotting, we found that this compound increases protein expression of cytochrome b(5), CYP1A1, 1A2, 3A and NADPH: CYP oxidoreductase (POR) in livers, lungs and kidneys of rats treated (i.p.) with ellipticine. The ellipticine-mediated induction of these enzymes resulted in an increase in their enzymatic activities and ellipticine oxidation to 7-hydroxy-, 9-hydroxy-, 12-hydroxy-and 13-hydroxyellipticine, the metabolites that are both detoxication products (7-hydroxy-, 9-hydroxyellipticine) and metabolites responsible for generation ellipticine-derived DNA adducts (12-hydroxy- and 13-hydroxyellipticine). The results demonstrate that by inducing CYP1A1/2, 3A, POR and cytochrome b(5), ellipticine increases its own metabolism in rats, thereby modulating its own pharmacological and/or genotoxic potential.
Klíčová slova
Ellipticine; Cytochromes P450; Protein Expression; Western Blotting; Metabolism
Autoři
VRÁNOVÁ, I.; MOSEROVÁ, M.; HODEK, P.; KIZEK, R.; FREI, E.; STIBOROVÁ, M.
Vydáno
1. 2. 2013
ISSN
1452-3981
Periodikum
INTERNATIONAL JOURNAL OF ELECTROCHEMICAL SCIENCE
Ročník
8
Číslo
2
Stát
Srbská republika
Strany od
1586
Strany do
1597
Strany počet
12
BibTex
@article{BUT145264, author="VRÁNOVÁ, I. and MOSEROVÁ, M. and HODEK, P. and KIZEK, R. and FREI, E. and STIBOROVÁ, M.", title="The Anticancer Drug Ellipticine Induces Cytochromes P450 1A1, 1A2 and 3A, Cytochrome b(5) and NADPH:Cytochrome P450 Oxidoreductase in Rat Liver, Kidney and Lung", journal="INTERNATIONAL JOURNAL OF ELECTROCHEMICAL SCIENCE", year="2013", volume="8", number="2", pages="1586--1597", issn="1452-3981" }