CYP-mediated biotransformation of some drugs can lead to the formation of reactive metabolites, the binding of which to intracellular and/or extracellular macromolecules may be associated with idiosyncratic toxicity. Troglitazone (TGZ) is one such drug and is frequently used as a model compound in studies of reactive metabolites, most of which have been conducted with subcellular fractions such...

The role of P-glycoprotein in secretion of indinavir metabolites produced by CYP3A4 was evaluated in Caco-2 cells expressing CYP3A4. Metabolism of indinavir by CYP3A4 expressing Caco-2 cells grown on filters resulted in the formation of N-dealkylation products (M5 and M6) and hydroxylation of indinavir, which were preferentially secreted into the apical compartment. Apical secretion of the meta...

This report describes the biochemistry of fatty acid ethyl esters (FAEE), non-oxidative metabolites of ethanol, and their clinical significance. We review information regarding the enzymes responsible for FAEE synthesis and degradation, and the mechanisms involved with the intracellular and extracellular transport of FAEE and FAEE-mediated cytotoxicity. Also a summary of reports on the emerging...

extracellular ca 2+ concentration ([ca2+]o) may be one of the factors affecting atrial natriuretic factor (anf) release. in the previous studies, there are opposite reports about the effect of [ca2+]o on anf secretion. therefore, the effect of [ca2+]o depletion on anf secretion and gene expression was studied in the present research. isolated right atria from rats were perfused for 6 and 2 hour...

previous studies had shown that sub-inhibitory concentrations of silver sulphadiazine (agsd) stimulated the production of toxic shock syndrome toxin-1 in certain strains (responder strains) of staphylococcus aureus and that protease production was also affected. no changes were detected in other strains (non-responders). extracellular proteins from eleven responder and non-responder strains gro...