The Effect of Epitestosterone on Estrogen Biosynthesis in Vitro

Objective: The concentrations of epitestosterone in human serum correlates negatively with that of estradiol. The possible explanation of this relation was addressed, and the influence of epitestosterone on kinetics of estradiol formation in vitro was evaluated. Methods: The concentration of epitestosterone was measured in serum of 54 men participating in a screening program for prostate disease. Epitestosterone inhibition of aromatase and 17β-hydroxysteroid dehydrogenase activities was tested in vitro in the system consisting of human placental microsomes, NADPH or NAD and NADP respectively, and epitestosterone in increasing concentrations. Testosterone, androstenedione, estrone and 17β-estradiol were utilized as substrates. Results: A significant negative correlation between epitestosterone and estradiol levels in human male serum was found. No inhibition of aromatase activity was observed; however, inhibition of 17β-hydroxysteroid dehydrogenase was found preferentially in the direction leading to oxidation of the C-17 hydroxy group. The inhibitory effect of epitestosterone was more pronounced with androgens as substrates. Conclusion: Epitestosterone could influence the formation of estradiol in vitro rather by inhibition of 17β-hydroxysteroid dehydrogenase than by blocking aromatase activity.

Key words

Inhibition - Aromatase - 17β-Hydroxysteroid Dehydrogenase - Placenta