Inhibitory effect of a new androstenedione derivative, 14 alpha-hydroxy-4-androstene-3,6,17-trione (14 alpha-OHAT) on aromatase activity of human uterine tumors

J Steroid Biochem. 1990 Aug 28;36(6):517-21. doi: 10.1016/0022-4731(90)90167-q.


The development of human uterine estrogen-dependent tumors is considered to be closely related to estrogen biosynthesis. This study examined whether or not 14 alpha-hydroxy-4-androstene-3,6,17-trione (14 alpha-OHAT), a new 4-androstene-3, 17-dione derivative synthesized microbiologically, inhibits estrogen biosynthetase (aromatase) activities of human uterine tumors (i.e. uterine endometrial cancer, uterine leiomyoma and uterine adenomyosis tissues). 14 alpha-OHAT inhibited aromatase activity in all uterine tumors, dose-dependently (0.1-10 microM). Moreover, 14 alpha-OHAT did not show the binding affinity to rabbit uterine cytosol-sex steroids, and it was not converted to estrogen in human placental preparations. Thus, 14 alpha-OHAT, an aromatase inhibitor, may be useful clinically as an endocrine chemotherapy for peri- or post-menopausal women with uterine estrogen-dependent tumors.

MeSH terms

  • Adult
  • Androstenols / pharmacology*
  • Animals
  • Aromatase / analysis
  • Aromatase Inhibitors*
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Middle Aged
  • Placenta / enzymology
  • Rabbits
  • Uterine Neoplasms / enzymology*


  • Androstenols
  • Aromatase Inhibitors
  • 14-hydroxyandrost-4-ene-3,6,17-trione
  • Aromatase