International Urology and Nephrology

, Volume 24, Issue 2, pp 145–154

In vitro study of rat prostate 5α-reductase activity and its inhibition

  • I. Faredin
  • I. Tóth
  • J. Oszlánczy
  • S. Scultéty
Article

DOI: 10.1007/BF02549642

Cite this article as:
Faredin, I., Tóth, I., Oszlánczy, J. et al. International Urology and Nephrology (1992) 24: 145. doi:10.1007/BF02549642

Abstract

A simple and rapid method of measuring 5α-reductase (5α-R) activity and of determining the kinetic parameters (KM and Vmax) of the enzyme is described. The 5α-R activity in the homogenate of the prostate of Wistar rats aged 8–12 weeks was established, and the effects of natural and synthetic steroids and of non-steroidal antiandrogens (IC50) upon the 5α-R activity were studied. Of the natural steroids, 17-0H-progesterone was found to have the highest inhibitory effect (IC50=1.35 μM), followed in decreasing order by progesterone (IC50=5.0 μM) and 4-androstene-3,17-dione (IC50=21.6 μM). Oestradiol-17β had practically no inhibitory effect. Of the synthetic steroids, 4-MA had the highest inhibitory effect (IC50=0.068 μM), followed by nortestosterone (IC50=7.4 μM) and RU-486 (Mifepristone) (IC50=115 μM). Even at 1000 μM, cyproterone acetate exerted no inhibitory effect. Of the nonsteroidal compounds, ketoconazole proved a weak inhibitor (IC50=115 μM), while flutamide was practically ineffective.

Copyright information

© Akadémiai Kiadó 1992

Authors and Affiliations

  • I. Faredin
    • 1
  • I. Tóth
    • 1
  • J. Oszlánczy
    • 2
  • S. Scultéty
    • 2
  1. 1.Endocrine Unit, First Department of MedicineSzent-Györgyi Albert Medical UniversitySzegedHungary
  2. 2.Department of UrologySzent-Györgyi Albert Medical UniversitySzegedHungary

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