Self-augmentation effect of male-specific products on sexually differentiated progesterone metabolism in adult male rat liver microsomes

J Biol Chem. 2001 Feb 16;276(7):4604-10. doi: 10.1074/jbc.M003355200. Epub 2000 Sep 19.

Abstract

It is well known that several 3-keto-4-ene steroids such as progesterone and testosterone are metabolized in a gender-specific or -predominant manner by adult rat liver microsomes. In the male, these steroids are primarily metabolized into two oxidized (16alpha-hydroxyl and 6beta-hydroxyl) products mainly by the respective, male-specific cytochrome P450 subforms, CYP2C11 and CYP3A2, while they are primarily metabolized into the 5alpha-reduced products by female-predominant 5alpha-reductase in the female. These sexually differentiated enzyme activities are largely regulated at the transcription level under endocrine control. In the present study, we show that unlabeled 16alpha-hydroxyprogesterone and 6beta-hydroxyprogesterone inhibited the 5alpha-reductive [(3)H]progesterone metabolism by adult male rat liver microsomes without significantly inhibiting the CYP2C11 and CYP3A2 activities producing themselves, whereas 3alpha-hydroxy-5alpha-pregnan-20-one and 5alpha-pregnane-3,20-dione not only stimulated the 5alpha-reductive metabolism producing themselves but also inhibited the male-specific oxidative metabolism. This finding compels us to propose a novel hypothesis that adult male rat liver microsomes may possess a self-augmentation system regulated by the male-specific products on sexually differentiated steroid metabolism, besides regulation by gene expressions of the related enzymes.

MeSH terms

  • 5-alpha-Dihydroprogesterone
  • Animals
  • Antibodies / immunology
  • Cytochrome P-450 Enzyme System / metabolism
  • Dose-Response Relationship, Drug
  • Hydroxyprogesterones / pharmacology
  • Male
  • Microsomes, Liver / metabolism*
  • Models, Biological
  • NADPH-Ferrihemoprotein Reductase / immunology
  • Oxidation-Reduction
  • Pregnanediones / pharmacology
  • Pregnanolone / pharmacology
  • Progesterone / metabolism*
  • Rats
  • Rats, Wistar
  • Sex Characteristics*
  • Steroid Hydroxylases / metabolism

Substances

  • Antibodies
  • Hydroxyprogesterones
  • Pregnanediones
  • 16-hydroxyprogesterone
  • Progesterone
  • 6-hydroxyprogesterone
  • Cytochrome P-450 Enzyme System
  • 5-alpha-Dihydroprogesterone
  • Pregnanolone
  • Steroid Hydroxylases
  • steroid hormone 6-beta-hydroxylase
  • NADPH-Ferrihemoprotein Reductase