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Epitestosterone--an endogenous antiandrogen?

L Stárka1, M Bicíková, R Hampl

  • 1Research Institute of Endocrinology, Praha, Czechoslovakia.

Journal of Steroid Biochemistry
|November 1, 1989
PubMed
Summary

Epitestosterone, a natural compound, acts as a weak antiandrogen by competing with other androgens for receptor binding. It also effectively inhibits the enzyme 5 alpha-reductase, impacting androgen metabolism.

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Area of Science:

  • Endocrinology
  • Androgen Metabolism

Background:

  • Epitestosterone (17 alpha-hydroxy-4-androsten-3-one) is a naturally occurring steroid found in human plasma and urine.
  • Androgens play crucial roles in male reproductive system development and maintenance.

Purpose of the Study:

  • To investigate the antiandrogenic properties of epitestosterone.
  • To determine epitestosterone's effect on testosterone-induced physiological changes.
  • To evaluate epitestosterone's inhibitory activity on 5 alpha-reductase.

Main Methods:

  • Administration of epitestosterone to castrated male mice to assess effects on body and organ weights.
  • In vitro competition assays with methyltrienolone for rat prostate cytosol binding.
  • Enzyme inhibition assays using 5 alpha-reductase from rat prostate pellet.

Main Results:

  • Epitestosterone prevented testosterone-induced changes in body weight and seminal vesicle/kidney weights in castrated mice.
  • Epitestosterone demonstrated competitive binding to rat prostate cytosol with a Ki of 29.8 nmol/L.
  • Epitestosterone inhibited rat prostate 5 alpha-reductase activity with a Ki of 1.2 µmol/L.

Conclusions:

  • Epitestosterone exhibits weak antiandrogen activity through receptor binding displacement.
  • Epitestosterone functions as an effective inhibitor of 5 alpha-reductase, suggesting a role in modulating androgen activity.

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