OBJECTIVE Microsomal epoxide hydrolase is an important enzyme involved in the metabolism of endogenous and exogenous toxicants. Polymorphic variants of the human epoxide hydrolase gene vary in enzyme activity. We determined whether genetic variability in the gene encoding for microsomal epoxide hydrolase contributes to individual differences in susceptibility to the development of pre-eclampsia...

A series of conformationally restricted inhibitors of human soluble epoxide hydrolase (sEH) has been developed. Inhibition potency of the described compounds ranges from 4.2 microM to 1.1 nM against recombinant sEH. N-(1-Acetylpiperidin-4-yl)-N'-(adamant-1-yl) urea (5a) was found to be a potent inhibitor (IC(50) = 7.0 nM) that was also orally bioavailable in canines.

Rat liver chemical hepatocarcinogenesis, induced by interrupted feeding of 2-acetylaminofluorene, results in various cellular preneoplastic stages and finally in a hepatoma in about 70 to 90 percent of the rats. The putative precursors of hepatomas, called hyperplastic nodules, appear after 12 weeks of feeding and, after 16 weeks of feeding carcinogen, most of them are persistent. Epoxide hydro...

Quinoline is a hepatocarcinogen in rats and mice and a well-known mutagen in bacteria after incubation with rat liver microsomes. The specific cytochrome P450 enzymes involved in quinoline metabolism in human and rat liver microsomes were determined using cDNA-expressed cytochrome P450s, correlations with specific cytochrome P450-linked monooxygenase activities in human liver microsomes and inh...

An assay for epoxide hydrolase activity using benzo(a)-pyrene 4,5-oxide as substrate was modified in such a manner that it allowed the estimation of activities in native and in cultivated mitogen-stimulated human lymphocytes. Their specific activities were about 1000-fold lower than those of human or rat liver microsomes. In native lymphocytes of 28 subjects, the specific activities of epoxide ...

The production of aliphatic polyesters (via ROP cyclic esters) and polycarbonates ROCOP CO2/epoxide) is an important synthetic pathway for the biodegradable biocompatible polymers. study focuses on catalytic activity selectivity phenoxy-imine based zinc compounds esters (rac-LA -CL) carbon dioxide CHO/PO. monoligated bisligated have same coordination number (four) but differed from each other ...

The tumorigenicity of chrysene, (+)and (-)-frans-1,2-dihydroxy-1,2-dihydrochrysene (chrysene 1,2-dihydrodiol), and the ( + )and (—)-enantiomers of the diastereomeric bay-region chrysene 1,2-diol-3,4-epoxides was assessed in two tumor models. A single topical application of 0.4 or 1.2 /¿mol of the chrysene derivatives on mouse skin followed by 25 weeks of promotion with 12-O-tetradecanoylphor...