PMID: 3758069Sep 1, 1986Paper

The effects of metyrapone, chalcone epoxide, benzil, clotrimazole and related compounds on the activity of microsomal epoxide hydrolase in situ, in purified form and in reconstituted systems towards different substrates

European Journal of Biochemistry
J SeidegårdF Oesch

Abstract

The influence of metyrapone, chalcone epoxide, benzil and clotrimazole on the activity of microsomal epoxide hydrolase towards styrene oxide, benzo[a]pyrene 4,5-oxide, estroxide and androstene oxide was investigated. The studies were performed using liver microsomes from rats, rabbits, mice and humans; epoxide hydrolase purified from rat liver microsomes to apparent homogeneity; and the purified enzyme incorporated into liposomes composed of egg-yolk phosphatidylcholine or total rat liver microsomal lipids. All four effectors were found to activate the hydrolysis of styrene oxide by epoxide hydrolase in situ in rat liver microsomal membranes, in agreement with earlier findings. Epoxide hydrolase activity towards styrene oxide in liver microsomes from mouse, rabbit and man was also increased by all four effectors. The most striking effect was a 680% activation by clotrimazole in rat liver microsomes. However, none of the effectors activated microsomal epoxide hydrolase more than 50% when benzo[a]pyrene 4,5-oxide, estroxide or androstene oxide was used as substrate. Indeed, clotrimazole was found to inhibit microsomal epoxide hydrolase activity towards estroxide 30-50% and towards androstene oxide 60-90%. The effects of these fou...Continue Reading

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Citations

Mar 18, 2000·Toxicology Letters·C J OmiecinskiV Hosagrahara
Oct 1, 1988·European Journal of Biochemistry·L SchladtF Oesch
Aug 1, 1995·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·J Y ChoS G Kim
Mar 14, 1997·Chemico-biological Interactions·H T Le, M R Franklin
Feb 18, 1992·Biochemical Pharmacology·D K RobbinsH Thomas

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