Simultaneous determination of cytochrome P450 1A, 2A and 3A activities in porcine liver microsomes

The aim of this study was to develop a robust method for the simultaneous determination of the activities of three porcine CYP450 enzymes in hepatic microsomes. A cocktail consisting of three selective CYP450 probe substrates, 7-ethoxyresorufin (CYP1A), coumarin (CYP2A) and 7-benzyloxy-4-trifluorome...

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Detalles Bibliográficos
Autores principales: Johansson, Monika, Tomankova, Jana, Li, Shengjie, Zamaratskaia, Galia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Slovak Toxicology Society SETOX 2012
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3600515/
https://www.ncbi.nlm.nih.gov/pubmed/23554555
http://dx.doi.org/10.2478/v10102-012-0024-3
Descripción
Sumario:The aim of this study was to develop a robust method for the simultaneous determination of the activities of three porcine CYP450 enzymes in hepatic microsomes. A cocktail consisting of three selective CYP450 probe substrates, 7-ethoxyresorufin (CYP1A), coumarin (CYP2A) and 7-benzyloxy-4-trifluoromethylcoumarin (BFC; CYP3A), was incubated with porcine liver microsomes. The presence of 7-ethoxyresorufin appears to significantly influence the kinetics of coumarin hydroxylation and BFC O-debenzylation. These results indicate that the use of 7-ethoxyresorufin in substrate cocktails together with coumarin and BFC should be avoided.

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