In vitro inhibitory effects of 16-methyl-substituted steroids on 5α-reductase in rat and human prostates

Imre Faredin, István Tóth, János Wölfling, Gyula Schneider, Eszter Meskó

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4 Citations (Scopus)

Abstract

The inhibitory effects (IC50) of 16-methyl steroids on 5α-reductase were studied. The in vitro experiments were carried out with homogenates of rat and human prostates. The investigated 16-methyl steroids were found to be weak inhibitors. In comparison with the known 5α-reductase inhibitor 4-MA (17β-N,N-diethylcarbamoyl-4-methyl-4-aza-5α-androstan-3-one), the relative IC50 values of the studied compounds are 4.7 times or more greater than 4-MA in human prostate and 23.5 times or more greater than 4-MA in rat prostate. The IC50 values increase in the sequence 16α-, 16β- and 16,16-dimethyl derivatives. In human prostate homogenates IC50 varies between 0.6 and 120, while in rat it ranges from 1.6 to 1000 μM. This shows that the enzyme of the human prostate is more sensitive than that of the rat prostate to the methyl-substituted compounds.

Original languageEnglish
Pages (from-to)568-571
Number of pages4
JournalSteroids
Volume59
Issue number10
DOIs
Publication statusPublished - Oct 1994

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Keywords

  • 16-methyl steroids
  • 5α-reductase
  • anti-androgens
  • in vitro inhibition

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Endocrinology
  • Pharmacology
  • Clinical Biochemistry
  • Organic Chemistry

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