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7-Ethoxy-3,4-dimethylcoumarin: a substrate for a cytochrome P450-mediated mono-oxygenase activity that is highly
A M Giurnazi1, M J Garle, K Lal
1Department of Physiology and Pharmacology, University of Nottingham Medical School, Queen's Medical Centre, UK.
Abstract:
The O-dealkylation of 7-ethoxy-3,4-dimethylcoumarin in rat liver microsomes was catalysed in a typical cytochrome P450-mediated reaction as judged by cofactor requirement and inhibition criteria, and displayed monophasic Michaelis-Menten kinetics. When measured at low substrate concentration, this activity was highly inducible by treatment with phenobarbitone or beta-naphthoflavone (44- and 78-fold induction, respectively). These data indicate the potential usefulness of this activity as a probe for P4501A1- and P4502B-mediated activities. The O-dealkylation of 7-methoxy- and 7-propoxy-3,4-dimethylcoumarin were much less inducible.