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Description
| - The antineoplastic alkaloid ellipticine is a prodrug, whose pharmacological efficiency is dependent on its cytochrome P450 (CYP)- and/or peroxidase-mediated activation in target tissues. This compound was found to induce expression of cytochrome b5, CYP1A1, 1A2 and 3A proteins determined electrochemically (Western blotting) and their enzymatic activities in livers, lungs and kidneys of rats treated (i.p.) with ellipticine. In addition, induction of these proteins resulted in an increase in ellipticine oxidation to 7-hydroxy-, 9-hydroxy-, 13-hydroxy- and 12-hydroxyellipticine, the metabolites that are both detoxication products (7-hydroxy-, 9-hydroxyellipticine) and metabolites responsible for generation elliptiicne-derived DNA adducts (12-hydroxy- and 13-hydroxyellipticine). The results demonstrate that by inducing CYP1A1/2, 3A and cytochrome b5, ellipticine increases its own metabolism leading both to an activation of this drug to reactive species forming DNA adducts and to detoxication metabolites, thereby modulating its own pharmacological and/or genotoxic potential
- The antineoplastic alkaloid ellipticine is a prodrug, whose pharmacological efficiency is dependent on its cytochrome P450 (CYP)- and/or peroxidase-mediated activation in target tissues. This compound was found to induce expression of cytochrome b5, CYP1A1, 1A2 and 3A proteins determined electrochemically (Western blotting) and their enzymatic activities in livers, lungs and kidneys of rats treated (i.p.) with ellipticine. In addition, induction of these proteins resulted in an increase in ellipticine oxidation to 7-hydroxy-, 9-hydroxy-, 13-hydroxy- and 12-hydroxyellipticine, the metabolites that are both detoxication products (7-hydroxy-, 9-hydroxyellipticine) and metabolites responsible for generation elliptiicne-derived DNA adducts (12-hydroxy- and 13-hydroxyellipticine). The results demonstrate that by inducing CYP1A1/2, 3A and cytochrome b5, ellipticine increases its own metabolism leading both to an activation of this drug to reactive species forming DNA adducts and to detoxication metabolites, thereby modulating its own pharmacological and/or genotoxic potential (en)
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Title
| - The anticancer drug ellipticine induces cytochrome b5 and cytochromes p450 1a1, 1a2 and 3a in rat liver, kidney and lung
- The anticancer drug ellipticine induces cytochrome b5 and cytochromes p450 1a1, 1a2 and 3a in rat liver, kidney and lung (en)
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skos:prefLabel
| - The anticancer drug ellipticine induces cytochrome b5 and cytochromes p450 1a1, 1a2 and 3a in rat liver, kidney and lung
- The anticancer drug ellipticine induces cytochrome b5 and cytochromes p450 1a1, 1a2 and 3a in rat liver, kidney and lung (en)
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skos:notation
| - RIV/62156489:43210/12:00190285!RIV13-GA0-43210___
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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...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/62156489:43210/12:00190285
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - cytochrome; prodrug; ellipticine (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...ontrolniKodProRIV
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http://linked.open...v/mistoKonaniAkce
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http://linked.open...i/riv/mistoVydani
| - Mendelova univerzita v Brně
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http://linked.open...i/riv/nazevZdroje
| - XII. Pracovní setkání fyzikálních chemiků a elektrochemiků
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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...iv/tvurceVysledku
| - Frei, Eva
- Hodek, Petr
- Kizek, René
- Moserova, M.
- Stiborová, Marie
- Vránová, Iveta
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http://linked.open...vavai/riv/typAkce
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http://linked.open.../riv/zahajeniAkce
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number of pages
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http://purl.org/ne...btex#hasPublisher
| - Mendelova zemědělská a lesnická univerzita v Brně
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https://schema.org/isbn
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http://localhost/t...ganizacniJednotka
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