About: 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

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About: 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 Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://www.electrochemsci.org/papers/vol8/80201586.pdf
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)
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)
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)
skos:notation	RIV/00216208:11310/13:10134474!RIV14-GA0-11310___
http://linked.open...avai/riv/aktivita	I P S
http://linked.open...avai/riv/aktivity	I, P(GAP301/10/0356), S
http://linked.open...iv/cisloPeriodika	2
http://linked.open...vai/riv/dodaniDat	2014
http://linked.open...aciTvurceVysledku	Moserová, Michaela Vranová, Iveta Hodek, Petr Stiborová, Marie
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Univerzita Karlova v Praze / Přírodovědecká fakulta
http://linked.open...dnocenehoVysledku	61377
http://linked.open...ai/riv/idVysledku	RIV/00216208:11310/13:10134474
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Metabolism; Western Blotting; Protein Expression; Cytochromes P450; Ellipticine (en)
http://linked.open.../riv/klicoveSlovo	Cytochromes P450 Protein Expression Western Blotting Ellipticine Metabolism
http://linked.open...odStatuVydavatele	RS - Srbská republika
http://linked.open...ontrolniKodProRIV	[A0E7B108595A]
http://linked.open...i/riv/nazevZdroje	International Journal of Electrochemical Science
http://linked.open...in/vavai/riv/obor	CG
http://linked.open...ichTvurcuVysledku	4 (xsd:int)
http://linked.open...cetTvurcuVysledku	6 (xsd:int)
http://linked.open...vavai/riv/projekt	Study of contribution of different DNA-damaging mechanisms to toxicity of cytostatics to human chemosensitive and chemoresistant neuroblastomas
http://linked.open...UplatneniVysledku	2013
http://linked.open...v/svazekPeriodika	8
http://linked.open...iv/tvurceVysledku	Frei, Eva Hodek, Petr Kizek, René Stiborová, Marie Moserová, Michaela Vranová, Iveta
http://linked.open...ain/vavai/riv/wos	000316565800004
issn	1452-3981
number of pages	12 (xsd:int)
http://localhost/t...ganizacniJednotka	11310

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