Quantitative studies of the metabolism of furazolidone by rat liver microsomes

Toxicology in Vitro : an International Journal Published in Association with BIBRA
L H VroomenP J van Bladeren

Abstract

The nitrofuran, furazolidone, is metabolized by rat liver microsomes under both aerobic and anaerobic conditions, the rates for microsomes from 3-methylcholanthrene-induced male rats being 3.52 and 4.26 nmol/mg protein/min, respectively. The two major metabolites formed are the well-known 3-(4-cyano-2-oxobutylideneamino)-2-oxazolidone, and 2,3-dihydro-3-cyanomethyl-2-hydroxy-5-nitro-1alpha,2-di-(2-oxo-oxazolidin-3-yl)iminomethylfuro[2,3-b]furan (accounting for 16.6 and 16.4% of total extractable radioactivity, respectively). Cytochrome P-450 is not involved in the conversion of furazolidone, which was converted by rat liver microsomes to products identical to those obtained upon incubation with purified NADPH-cytochrome P-450 reductase, which is a microsomal reductase. During metabolism, a considerable amount of material (2-3% of total metabolites) became covalently bound to microsomal protein. This covalent binding could be inhibited by addition of glutathione, which also resulted in an almost complete shift from non-polar to water-soluble metabolites. No interaction of furazolidone with added calf thymus DNA was detected.

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Citations

Oct 15, 1991·The Science of the Total Environment·O B SamuelsenB T Lunestad
May 1, 1992·Toxicology in Vitro : an International Journal Published in Association with BIBRA·L A HoogenboomH A Kuiper
Jul 1, 2002·Environmental Toxicology and Pharmacology·Laurentius A P HoogenboomHarry A Kuiper
Jan 1, 1990·The Veterinary Quarterly·J F Nouws, J Laurensen
Dec 1, 1987·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·L H VroomenH A Kuiper
Jan 1, 1987·Chemico-biological Interactions·L H VroomenP J van Bladeren
Aug 1, 1988·Toxicology and Applied Pharmacology·L H VroomenP J van Bladeren
Jan 1, 1990·Drug Metabolism Reviews·L H VroomenH A Kuiper
Oct 17, 1998·Toxicology and Applied Pharmacology·I De AngelisF Zucco
May 12, 2017·Journal of Agricultural and Food Chemistry·Yinan WangWan Chan
Nov 1, 1989·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·L A HoogenboomH A Kuiper

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