BIOTRANSFORMATION OF INOPHENYL)17-ALPHA-1-PROPYNYL-ESTRA-4,9-DIEN-3-ONE (RU486) IN RAT HEPATOMA VARIANTS

Authors
CHASSEROTGOLAZ S BECK G VENETIANER A
Citation
S. Chasserotgolaz et al., BIOTRANSFORMATION OF INOPHENYL)17-ALPHA-1-PROPYNYL-ESTRA-4,9-DIEN-3-ONE (RU486) IN RAT HEPATOMA VARIANTS, Biochemical pharmacology, 46(11), 1993, pp. 2100-2103
Citations number
23
Categorie Soggetti
Pharmacology & Pharmacy",Biology
Journal title
Biochemical pharmacology → ACNP
ISSN journal
00062952
Volume
46
Issue
11
Year of publication
1993
Pages
2100 - 2103
Database
ISI
SICI code
0006-2952(1993)46:11<2100:BOI>2.0.ZU;2-I
Abstract
Metabolism of the synthetic steroid 17 beta-hydroxy-11 beta(4-dimethyl aminophenyl)17 alpha-1-propynyl-estra-4,9-dien-3-one (RU486) occurs in the dedifferentiated S-H56-125 variant of Reuber hepatoma. Considerin g that rat liver cytochrome P450 (P450) monooxygenases are engaged in different oxidative steps of the metabolism of RU486, the influence of several prototype P450 inducers was investigated. The data obtained b y treating H56 and S-H56-125 hepatoma cells with different P450 induce rs (dexamethasone (DEX), benzanthracene, phenobarbital) or with a spec ific P450 inhibitor, troleandomycin, led us to conclude that CYP3A is involved in the hydroxylation of RU486. This form is induced by DEX in dependently of the availability of the canonical glucocorticoid recept or.