Stimulation of microsomal spironolactone metabolism by reduced glutathione.

Abstract:

:The first step in the conversion of spironolactone (SP) to its biologically active metabolites is deacetylation to 7 alpha-thiospirolactone (7 alpha-thio-SL). Studies were done to evaluate the effects of reduced glutathione (GSH) on SP deacetylation by adrenal microsomal preparations. In the absence of GSH, adrenal microsomes catalyzed the conversion of SP to 7 alpha-thio-SL at low rates. Addition of GSH to the incubation medium caused a concentration-dependent stimulation of SP deacetylation. At a concentration of 10 mM, GSH caused a 4- to 5-fold increase in the rate of 7 alpha-thio-SL production. The results suggest that GSH may have an important role in the overall disposition of SP, including the formation of active metabolites.

journal_name

Pharmacology

journal_title

Pharmacology

authors

Colby HD,LaCagnin LB,Los LE

doi

10.1159/000139358

subject

Has Abstract

pub_date

1996-01-01 00:00:00

pages

30-4

issue

1

eissn

0031-7012

issn

1423-0313

journal_volume

52

pub_type

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