Clotrimazole, but not dexamethasone, is a potent in vitro inhibitor of cytochrome P450 isoforms CYP1A and CYP3A in rainbow trout

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60076658%3A12520%2F13%3A43885194" target="_blank" >RIV/60076658:12520/13:43885194 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0045653513001665" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0045653513001665</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.chemosphere.2013.01.050" target="_blank" >10.1016/j.chemosphere.2013.01.050</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Clotrimazole, but not dexamethasone, is a potent in vitro inhibitor of cytochrome P450 isoforms CYP1A and CYP3A in rainbow trout

Popis výsledku v původním jazyce

The effects of clotrimazole (CLO) and dexamethasone (DEX), both detected in the aquatic environment, were assessed on inhibition of cytochrome P450 (CYP450) in hepatic microsomes of rainbow trout. Activity of three CYP450 isoforms: ethoxyresorufin O-deethylase (EROD; CYP1A), 7-benzyloxy-4-trifluoromethylcoumarin O-debenzylase (BFCOD; CYP3A) and p-nitrophenol hydroxylase (PNPH; CYP2E1-like protein) was investigated in the presence of four concentrations of CLO and DEX. Clotrimazole in a concentration range of 1-100 mu M decreased the activity of EROD and MOD. The inhibition was reversible, as pre-incubation of the microsomes with CLO, before addition of the substrate, had no effect. EROD activity was non-competitively inhibited with a K-i of 0.5 mu M, and BFCOD activity revealed competitive inhibition with a K-i of 0.04 mu M. The relatively low K-i for CLO inhibition of EROD and BFCOD activity may indicate that the ability of CYP1A and CYP3A to metabolize xenobiotics is reduced in the p

Název v anglickém jazyce

Clotrimazole, but not dexamethasone, is a potent in vitro inhibitor of cytochrome P450 isoforms CYP1A and CYP3A in rainbow trout

Popis výsledku anglicky

The effects of clotrimazole (CLO) and dexamethasone (DEX), both detected in the aquatic environment, were assessed on inhibition of cytochrome P450 (CYP450) in hepatic microsomes of rainbow trout. Activity of three CYP450 isoforms: ethoxyresorufin O-deethylase (EROD; CYP1A), 7-benzyloxy-4-trifluoromethylcoumarin O-debenzylase (BFCOD; CYP3A) and p-nitrophenol hydroxylase (PNPH; CYP2E1-like protein) was investigated in the presence of four concentrations of CLO and DEX. Clotrimazole in a concentration range of 1-100 mu M decreased the activity of EROD and MOD. The inhibition was reversible, as pre-incubation of the microsomes with CLO, before addition of the substrate, had no effect. EROD activity was non-competitively inhibited with a K-i of 0.5 mu M, and BFCOD activity revealed competitive inhibition with a K-i of 0.04 mu M. The relatively low K-i for CLO inhibition of EROD and BFCOD activity may indicate that the ability of CYP1A and CYP3A to metabolize xenobiotics is reduced in the p

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

CE - Biochemie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2013

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Chemosphere

ISSN

0045-6535

e-ISSN

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Svazek periodika

92

Číslo periodika v rámci svazku

9

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

6

Strana od-do

1099-1104

Kód UT WoS článku

000322936500005

EID výsledku v databázi Scopus

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