Effects in vitro of medroxyprogesterone acetate on steroid metabolizing enzymes in the rat: selective inhibition of 3 alpha-hydroxysteroid oxidoreductase activity

J Steroid Biochem. 1982 Aug;17(2):197-203. doi: 10.1016/0022-4731(82)90122-4.

Abstract

The effects of 6 alpha-methyl-17 alpha-acetoxy-4-pregnene 3,20-dione (MPA) on the activity of different steroid metabolizing enzymes in vitro were investigated in several organs in the rat. MPA seems to be a potent inhibitor of 3 alpha-reduction of 17 beta-hydroxy-5 alpha-androstan-3-one (Dht) in homogenates of the testis, ovary, epididymis, prostate, kidney and the adrenal glands. In testicular homogenates MPA acts like a competitive inhibitor of the 3 alpha-reduction of Dht, with Ki of 0.42 [microM]. MPA seems to be a selective inhibitor of 3 alpha-hydroxysteroid oxidoreductase in numerous organs. Steroid metabolizing enzymes like 5 alpha-reductase, 7 alpha-hydroxylase, 3 beta-hydroxysteroid oxidoreductase and 17 beta-hydroxysteroid oxidoreductase were not inhibited by MPA under the conditions of incubation employed in these studies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 17-Hydroxysteroid Dehydrogenases / metabolism
  • 3-Hydroxysteroid Dehydrogenases / antagonists & inhibitors*
  • 3-Hydroxysteroid Dehydrogenases / metabolism
  • 3-alpha-Hydroxysteroid Dehydrogenase (B-Specific)
  • Adrenal Glands / enzymology
  • Animals
  • Contraceptive Agents, Female / pharmacology*
  • Epididymis / enzymology
  • Female
  • Kidney / enzymology
  • Male
  • Medroxyprogesterone / analogs & derivatives*
  • Medroxyprogesterone / pharmacology
  • Medroxyprogesterone Acetate
  • Ovary / enzymology*
  • Prostate / enzymology
  • Rats
  • Rats, Inbred Strains
  • Testis / enzymology*

Substances

  • Contraceptive Agents, Female
  • Medroxyprogesterone Acetate
  • 17-Hydroxysteroid Dehydrogenases
  • 3-Hydroxysteroid Dehydrogenases
  • 3-alpha-Hydroxysteroid Dehydrogenase (B-Specific)
  • Medroxyprogesterone