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

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About: Clotrimazole, but not dexamethasone, is a potent in vitro inhibitor of cytochrome P450 isoforms CYP1A and CYP3A in rainbow trout Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://www.sciencedirect.com/science/article/pii/S0045653513001665
Description	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 presence of CLO. PNPH activity was not affected by CLO. DEX showed no inhibitory potency on any investigated reaction. CLO, but not DEX, inhibited EROD and BFCOD activity by different mechanisms. 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 presence of CLO. PNPH activity was not affected by CLO. DEX showed no inhibitory potency on any investigated reaction. CLO, but not DEX, inhibited EROD and BFCOD activity by different mechanisms. (en)
Title	Clotrimazole, but not dexamethasone, is a potent in vitro inhibitor of cytochrome P450 isoforms CYP1A and CYP3A in rainbow trout Clotrimazole, but not dexamethasone, is a potent in vitro inhibitor of cytochrome P450 isoforms CYP1A and CYP3A in rainbow trout (en)
skos:prefLabel	Clotrimazole, but not dexamethasone, is a potent in vitro inhibitor of cytochrome P450 isoforms CYP1A and CYP3A in rainbow trout Clotrimazole, but not dexamethasone, is a potent in vitro inhibitor of cytochrome P450 isoforms CYP1A and CYP3A in rainbow trout (en)
skos:notation	RIV/60076658:12520/13:43885194!RIV14-GA0-12520___
http://linked.open...avai/predkladatel	Fakulta rybářství a ochrany vod
http://linked.open...avai/riv/aktivita	P S
http://linked.open...avai/riv/aktivity	P(ED2.1.00/01.0024), P(GAP503/11/1130), S
http://linked.open...iv/cisloPeriodika	9
http://linked.open...vai/riv/dodaniDat	2014
http://linked.open...aciTvurceVysledku	Burkina, Viktoriia Žlábek, Vladimír
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	Jihočeská univerzita v Českých Budějovicích / Fakulta rybářství a ochrany vod
http://linked.open...dnocenehoVysledku	65733
http://linked.open...ai/riv/idVysledku	RIV/60076658:12520/13:43885194
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	CYP2E1-like protein; CYP3A; CYP1A; Rainbow trout; Dexamethasone; Clotrimazole (en)
http://linked.open.../riv/klicoveSlovo	Dexamethasone CYP1A CYP2E1-like protein CYP3A Clotrimazole Rainbow trout
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[634D38B43570]
http://linked.open...i/riv/nazevZdroje	Chemosphere
http://linked.open...in/vavai/riv/obor	CE
http://linked.open...ichTvurcuVysledku	2 (xsd:int)
http://linked.open...cetTvurcuVysledku	3 (xsd:int)
http://linked.open...vavai/riv/projekt	Effect of environmental levels of selected pharmaceuticals on rainbow trout (Oncorhynchus mykiss) and fish cell culture models South Bohemian Research Center of Aquaculture and Biodiversity of Hydrocenoses
http://linked.open...UplatneniVysledku	2013
http://linked.open...v/svazekPeriodika	92
http://linked.open...iv/tvurceVysledku	Žlábek, Vladimír Burkina, Viktoriia Zamaiatskaia, Galia
http://linked.open...ain/vavai/riv/wos	000322936500005
issn	0045-6535
number of pages	6 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.chemosphere.2013.01.050
http://localhost/t...ganizacniJednotka	12520

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