Determination of rat 5α-reductase type 1 isozyme activity and its inhibition by novel steroidal oxazolines

M. Szécsi, Dóra Ondré, I. Tóth, S. Magony, J. Wölfling, G. Schneider, J. Julesz

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

The 5α-reductase type 1 isozyme is a key enzyme in the metabolism of the androgen steroid hormones and inhibitors of this enzyme represent a new pharmacological treatment for several androgen dependent diseases. We developed a radiosubstrate in vitro incubation method for the determination of 5α-reductase type 1 activity using rat liver microsomes as an enzyme source. With this method we have studied the inhibiting activity of novel (5′ S )-17β-(4,5-dihydrooxazol-5-yl)androst-5-en-3-one compounds containing various derivatized phenyl substituents coupled to the exo -heterocyclic moiety. Tests revealed moderate inhibitory actions compared to finasteride, nevertheless, results provide interesting structure-activity relationship data.

Original languageEnglish
Pages (from-to)274-281
Number of pages8
JournalActa Biologica Hungarica
Volume61
Issue number3
DOIs
Publication statusPublished - Sep 1 2010

Fingerprint

Androgens
Isoenzymes
Rats
Oxidoreductases
androgen
Steroid hormones
enzyme
Finasteride
Liver Microsomes
Enzyme Inhibitors
Enzymes
Structure-Activity Relationship
Metabolism
Liver
Steroids
Hormones
Pharmacology
steroid
hormone
inhibitor

Keywords

  • 5α-reductase inhibitors
  • exo -heterocyclic steroids
  • finasteride
  • rat liver

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Environmental Science(all)
  • Neurology

Cite this

Determination of rat 5α-reductase type 1 isozyme activity and its inhibition by novel steroidal oxazolines. / Szécsi, M.; Ondré, Dóra; Tóth, I.; Magony, S.; Wölfling, J.; Schneider, G.; Julesz, J.

In: Acta Biologica Hungarica, Vol. 61, No. 3, 01.09.2010, p. 274-281.

Research output: Contribution to journalArticle

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