Covalent binding of chlorotrianisene (TACE) metabolite(s) to rat hepatic microsomal components
TACE, an estrogen, is a member of the triarylethylene series of compounds which includes the antiestrogens clomiphene and tamoxifen. TACE has been used as a therapeutic estrogen and has been identified as a contaminant in the pesticide methoxychlor (M) and is presumably one of the factors responsible for the estrogenic properties of technical M. The possibility that like M, TACE is activated to covalently bind to microsomal proteins, was examined. (/sup 3/H)TACE was incubated with liver microsomes from phenobarbital (Pb)-treated male rats and NADPH. Microsomes were precipitated with ethanol and trapped on glass-fiber filter. The filter was washed with ethanol, hexane, and methanol:ether mixtures. The residue was solubilized from the filter by incubating (1hr, 37/sup 0/) With 2% SDS and the radioactivity and protein contents were determined. The solubilized samples were also subjected to SDS-polyacrylamide gel electrophoresis (PAGE). Binding of TACE metabolites to microsomal components in the presence of NADPH was 350 pmol/30 min/mg protein. PAGE analysis revealed radioactivity in a region of 50-55K daltons, suggesting covalent binding to protein(s). When compared to incubations with control microsomes, binding was markedly enhanced by microsomes Pb treated rats.
- Research Organization:
- Worcester Foundation for Experimental Biology, Shrewsbury, MA
- OSTI ID:
- 5463158
- Report Number(s):
- CONF-8604222-
- Journal Information:
- Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States), Journal Name: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States) Vol. 45:3; ISSN FEPRA
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
ANESTHETICS
ANIMALS
ANTICONVULSANTS
AZINES
BARBITURATES
BIOCHEMICAL REACTION KINETICS
BODY
CELL CONSTITUENTS
CENTRAL NERVOUS SYSTEM DEPRESSANTS
COENZYMES
COVALENCE
DIGESTIVE SYSTEM
DRUGS
ELECTROPHORESIS
ESTROGENS
GLANDS
HETEROCYCLIC COMPOUNDS
HORMONES
HYPNOTICS AND SEDATIVES
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
LIVER
MAMMALS
METABOLITES
MICROSOMES
NADP
NUCLEOTIDES
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC OXYGEN COMPOUNDS
ORGANOIDS
ORGANS
PHENOBARBITAL
PYRIMIDINES
RATS
REACTION KINETICS
RODENTS
STEROID HORMONES
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES