Metformin directly inhibits androgen production in human thecal cells

Fertil Steril. 2001 Sep;76(3):517-24. doi: 10.1016/s0015-0282(01)01975-6.

Abstract

Objective: To examine the direct effect of metformin on thecal cell androgen production.

Setting: Basic science research laboratory, University of Texas Southwestern, Dallas, Texas.

Intervention(s): Human ovarian theca-like tumor cells were treated with various concentrations of metformin in the presence and absence of forskolin for 48 hours.

Main outcome measure(s): Media were collected, and radioimmunoassay (RIA) for progesterone, 17 alpha-hydroxyprogesterone (17OHP), androstenedione, and testosterone was performed. The effect of metformin on the expression of various enzymes involved in theca cell steroidogenesis was examined.

Result(s): Metformin (50 microM and 200 microM) significantly inhibited androstenedione production from both forskolin-stimulated and unstimulated theca cells. Testosterone production was also significantly inhibited in forskolin-treated cells in the presence of 200 microM of metformin-treated compared with forskolin-only-treated cells. Western blot analysis revealed that metformin significantly inhibited the expression of steroidogenic acute regulatory (StAR) protein and 17 alpha-hydroxylase (CYP17) expression in cells stimulated with forskolin compared with forskolin treatment alone. There was no significant change in either 3beta-hydroxysteroid dehydrogenase (3 beta HSD) or cholesterol side-chain cleavage (CYP11A1) protein expression. Northern analysis revealed a significant decrease in the expression of CYP17 mRNA in forskolin-stimulated cells treated with metformin (200 microM) compared with forskolin-only-treated cells, however, there was no significant change in steroidogenic acute regulatory protein mRNA expression.

Conclusion(s): Our results suggest that metformin may have a direct effect on thecal cells' androgen production.

Publication types

  • Comparative Study

MeSH terms

  • 17-alpha-Hydroxyprogesterone / metabolism
  • 3-Hydroxysteroid Dehydrogenases / genetics
  • Androgens / biosynthesis*
  • Androstenedione / metabolism
  • Cells, Cultured
  • Cholesterol Side-Chain Cleavage Enzyme / genetics
  • Colforsin / pharmacology
  • Female
  • Gene Expression Regulation, Enzymologic / drug effects*
  • Humans
  • Metformin / pharmacology*
  • Phosphoproteins / genetics
  • Progesterone / metabolism
  • RNA, Messenger / genetics
  • Steroid 17-alpha-Hydroxylase / genetics
  • Steroidogenic Acute Regulatory Protein
  • Testosterone / metabolism
  • Theca Cells / cytology
  • Theca Cells / drug effects
  • Theca Cells / metabolism*
  • Transcription, Genetic / drug effects

Substances

  • Androgens
  • Phosphoproteins
  • RNA, Messenger
  • Steroidogenic Acute Regulatory Protein
  • Colforsin
  • Testosterone
  • Androstenedione
  • Progesterone
  • 17-alpha-Hydroxyprogesterone
  • Metformin
  • 3-Hydroxysteroid Dehydrogenases
  • Steroid 17-alpha-Hydroxylase
  • Cholesterol Side-Chain Cleavage Enzyme