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Statements

Subject Item
n2:RIV%2F62156489%3A43210%2F12%3A00190285%21RIV13-GA0-43210___
rdf:type
n5:Vysledek skos:Concept
dcterms: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
dcterms: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
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
skos:notation
RIV/62156489:43210/12:00190285!RIV13-GA0-43210___
n5:predkladatel
n17:orjk%3A43210
n3:aktivita
n11:P
n3:aktivity
P(GAP301/10/0356)
n3:dodaniDat
n12:2013
n3:domaciTvurceVysledku
n22:4995775
n3:druhVysledku
n6:D
n3:duvernostUdaju
n15:S
n3:entitaPredkladatele
n19:predkladatel
n3:idSjednocenehoVysledku
122912
n3:idVysledku
RIV/62156489:43210/12:00190285
n3:jazykVysledku
n4:eng
n3:klicovaSlova
cytochrome; prodrug; ellipticine
n3:klicoveSlovo
n7:ellipticine n7:cytochrome n7:prodrug
n3:kontrolniKodProRIV
[1E7B498C3A20]
n3:mistoKonaniAkce
Brno, Česká republika
n3:mistoVydani
Mendelova univerzita v Brně
n3:nazevZdroje
XII. Pracovní setkání fyzikálních chemiků a elektrochemiků
n3:obor
n14:CE
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
6
n3:projekt
n18:GAP301%2F10%2F0356
n3:rokUplatneniVysledku
n12:2012
n3:tvurceVysledku
Vránová, Iveta Moserova, M. Stiborová, Marie Frei, Eva Kizek, René Hodek, Petr
n3:typAkce
n13:CST
n3:zahajeniAkce
2012-01-01+01:00
s:numberOfPages
3
n16:hasPublisher
Mendelova zemědělská a lesnická univerzita v Brně
n20:isbn
978-80-7375-618-5
n21:organizacniJednotka
43210