PMID- 7895695 OWN - NLM STAT- MEDLINE DCOM- 19950425 LR - 20131121 IS - 0013-7227 (Print) IS - 0013-7227 (Linking) VI - 136 IP - 4 DP - 1995 Apr TI - 11 alpha- and 11 beta-hydroxyprogesterone, potent inhibitors of 11 beta-hydroxysteroid dehydrogenase (isoforms 1 and 2), confer marked mineralocorticoid activity on corticosterone in the ADX rat. PG - 1809-12 AB - The effects of 11 alpha- and 11 beta-hydroxyprogesterone (11 alpha-OHP, 11 beta-OHP), on the activity of the glucocorticoid inactivating enzyme 11 beta-hydroxysteroid dehydrogenase (11 beta-HSD) were studied. 11 alpha-OHP and 11 beta-OHP were potent inhibitors of both 11 beta-HSD1 in rat liver microsomes and 11 beta-HSD2 in lysates of JEG-3 cells, a human choriocarcinoma cell line. In addition, both progesterone metabolites were markedly potent in conferring mineralocorticoid activity upon B in the adrenalectomized rat. These results provide insight into the structural properties required of inhibitors of 11 beta-HSD activity and indicate a possible role for endogenous 11 beta-HSD inhibitors in the regulation of glucocorticoid-induced Na+ retention. FAU - Souness, G W AU - Souness GW AD - Department of Pathology and Laboratory Medicine, Miriam Hospital, Providence, RI. FAU - Latif, S A AU - Latif SA FAU - Laurenzo, J L AU - Laurenzo JL FAU - Morris, D J AU - Morris DJ LA - eng GR - DK21404/DK/NIDDK NIH HHS/United States PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Research Support, U.S. Gov't, P.H.S. PL - United States TA - Endocrinology JT - Endocrinology JID - 0375040 RN - 0 (Hydroxyprogesterones) RN - 312-90-3 (11-hydroxyprogesterone) RN - EC 1.1.- (Hydroxysteroid Dehydrogenases) RN - EC 1.1.1.146 (11-beta-Hydroxysteroid Dehydrogenases) RN - RWP5GA015D (Potassium) RN - W980KJ009P (Corticosterone) SB - IM MH - 11-beta-Hydroxysteroid Dehydrogenases MH - *Adrenalectomy MH - Animals MH - Choriocarcinoma/enzymology MH - Corticosterone/*pharmacology MH - Humans MH - Hydroxyprogesterones/*pharmacology MH - Hydroxysteroid Dehydrogenases/*antagonists & inhibitors/metabolism MH - Male MH - Microsomes, Liver/enzymology MH - Natriuresis/drug effects MH - Potassium/urine MH - Rats MH - Rats, Sprague-Dawley MH - Tumor Cells, Cultured EDAT- 1995/04/01 00:00 MHDA- 1995/04/01 00:01 CRDT- 1995/04/01 00:00 PHST- 1995/04/01 00:00 [pubmed] PHST- 1995/04/01 00:01 [medline] PHST- 1995/04/01 00:00 [entrez] AID - 10.1210/endo.136.4.7895695 [doi] PST - ppublish SO - Endocrinology. 1995 Apr;136(4):1809-12. doi: 10.1210/endo.136.4.7895695.