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
Pharmacologyjournal_title
Pharmacologyauthors
Colby HD,LaCagnin LB,Los LEdoi
10.1159/000139358subject
Has Abstractpub_date
1996-01-01 00:00:00pages
30-4issue
1eissn
0031-7012issn
1423-0313journal_volume
52pub_type
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