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Statements

Subject Item
n2:RIV%2F60076658%3A12520%2F13%3A43885194%21RIV14-GA0-12520___
rdf:type
n8:Vysledek skos:Concept
rdfs:seeAlso
http://www.sciencedirect.com/science/article/pii/S0045653513001665
dcterms: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.
dcterms: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
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
skos:notation
RIV/60076658:12520/13:43885194!RIV14-GA0-12520___
n8:predkladatel
n15:orjk%3A12520
n3:aktivita
n18:S n18:P
n3:aktivity
P(ED2.1.00/01.0024), P(GAP503/11/1130), S
n3:cisloPeriodika
9
n3:dodaniDat
n4:2014
n3:domaciTvurceVysledku
n14:3414329 n14:9855130
n3:druhVysledku
n17:J
n3:duvernostUdaju
n11:S
n3:entitaPredkladatele
n20:predkladatel
n3:idSjednocenehoVysledku
65733
n3:idVysledku
RIV/60076658:12520/13:43885194
n3:jazykVysledku
n16:eng
n3:klicovaSlova
CYP2E1-like protein; CYP3A; CYP1A; Rainbow trout; Dexamethasone; Clotrimazole
n3:klicoveSlovo
n10:CYP3A n10:Rainbow%20trout n10:Dexamethasone n10:Clotrimazole n10:CYP1A n10:CYP2E1-like%20protein
n3:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n3:kontrolniKodProRIV
[634D38B43570]
n3:nazevZdroje
Chemosphere
n3:obor
n9:CE
n3:pocetDomacichTvurcuVysledku
2
n3:pocetTvurcuVysledku
3
n3:projekt
n12:ED2.1.00%2F01.0024 n12:GAP503%2F11%2F1130
n3:rokUplatneniVysledku
n4:2013
n3:svazekPeriodika
92
n3:tvurceVysledku
Zamaiatskaia, Galia Žlábek, Vladimír Burkina, Viktoriia
n3:wos
000322936500005
s:issn
0045-6535
s:numberOfPages
6
n19:doi
10.1016/j.chemosphere.2013.01.050
n21:organizacniJednotka
12520