Activity and inhibition of 3-beta-hydroxysteroid dehydrogenase/delta-5-4-isomerase in human skin

I. Toth, M. Szecsi, J. Julesz, I. Faredin

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

Activity and inhibition of 3β-hydroxysteroid dehydrogenase/Δ5-4-isomerase, a key enzyme of biosynthesis of androgenic steroids, in human skin were studied. Whole-width dermal tissue specimens excised from various regions of the male and female body were investigated with an in vitro radioenzyme assay method using dehydroepiandrosterone as substrate. The Michaelis-Menten constant of the enzyme was found to be K(m) = 10 nM and the maximal velocity was V(max) = 0.625 pmol produced 4-androstene-3,17-dione/mg protein/20 min. Activity of 3β-hydroxysteroid dehydrogenase/Δ5-4-isomerase in male inguinal skin (n = 8) was 0.132-0.412, in female abdominal skin (n = 4) 0.140-0.255, in perineal skin (n = 4) 0.138-0.962 pmol/mg protein/20 min. The synthetic steroids cyproterone acetate, 4-MA and epostane proved to be potent inhibitors, IC50 values were 150, 6.2 and 1.45 nM, respectively.

Original languageEnglish
Pages (from-to)160-168
Number of pages9
JournalSkin Pharmacology
Volume10
Issue number3
Publication statusPublished - 1997

Fingerprint

Skin
3-Hydroxysteroid Dehydrogenases
Isomerases
Steroids
Cyproterone Acetate
Dehydroepiandrosterone
Androstenedione
Groin
Enzymes
Inhibitory Concentration 50
Proteins
3 beta-hydroxysteroid oxidoreductase-delta(5) 3-ketosteroid isomerase

Keywords

  • Androgen activity
  • Enzymes
  • Human skin
  • Inhibitors

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Dermatology
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Activity and inhibition of 3-beta-hydroxysteroid dehydrogenase/delta-5-4-isomerase in human skin. / Toth, I.; Szecsi, M.; Julesz, J.; Faredin, I.

In: Skin Pharmacology, Vol. 10, No. 3, 1997, p. 160-168.

Research output: Contribution to journalArticle

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