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Description
| - 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.
- 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. (en)
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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
- 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 (en)
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skos:prefLabel
| - 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
- 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 (en)
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skos:notation
| - RIV/00216208:11310/13:10134474!RIV14-GA0-11310___
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http://linked.open...avai/predkladatel
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http://linked.open...avai/riv/aktivita
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http://linked.open...avai/riv/aktivity
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http://linked.open...iv/cisloPeriodika
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http://linked.open...vai/riv/dodaniDat
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http://linked.open...aciTvurceVysledku
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http://linked.open.../riv/druhVysledku
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http://linked.open...iv/duvernostUdaju
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http://linked.open...titaPredkladatele
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http://linked.open...dnocenehoVysledku
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http://linked.open...ai/riv/idVysledku
| - RIV/00216208:11310/13:10134474
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - Metabolism; Western Blotting; Protein Expression; Cytochromes P450; Ellipticine (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
| - International Journal of Electrochemical Science
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http://linked.open...in/vavai/riv/obor
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http://linked.open...ichTvurcuVysledku
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http://linked.open...cetTvurcuVysledku
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http://linked.open...vavai/riv/projekt
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http://linked.open...UplatneniVysledku
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http://linked.open...v/svazekPeriodika
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http://linked.open...iv/tvurceVysledku
| - Frei, Eva
- Hodek, Petr
- Kizek, René
- Stiborová, Marie
- Moserová, Michaela
- Vranová, Iveta
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http://linked.open...ain/vavai/riv/wos
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issn
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number of pages
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http://localhost/t...ganizacniJednotka
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