Antioxidant effect of the active metabolites of tibolone

Julia Stark, Szabolcs Varbiro, Miklos Sipos, Zsolt Tulassay, Levente Sara, Ildiko Adler, Elek Dinya, Zoltan Magyar, Bela Szekacs, Istvan Marczell, Helenius J. Kloosterboer, Karoly Racz, Gabor Bekesi

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5 Citations (Scopus)


Certain steroidal compounds have an antioxidant effect in humans. Our aim was to test whether the synthetic steroid tibolone and its metabolites are also able to display such a property. For this, granulocytes from healthy men and women were incubated for two hours with different concentrations (10-7, 10-8, 10-9M) of either estradiol, tibolone, 3α-hydroxytibolone, 3β-hydroxytibolone, Δ4-tibolone, 3α-sulfated-tibolone, 3α-17β-disulfated-tibolone, 3β-sulfated-tibolone or 3β-17β-disulfated-tibolone. Superoxide anion generation of neutrophils was measured by photometry. Results of different steroids were given as percentages of their controls. A more simple superoxide generating system, the xanthine-xanthine oxidase reaction was also tested. We found that granulocyte superoxide production did not differ from the control using 10-9M of steroids. Using 10-8M concentration: estradiol (80.9±2.5%); 3β-sulfated-tibolone (83.3±4.7%); 3β-17β-disulfated-tibolone (81.0±4.2%) caused a significant decrease in superoxide production, compared to the control. In addition at 10-7M, 3β-hydroxytibolone and 3α-sulfated-tibolone also showed antioxidant effects. In the xanthine-xanthine oxidase system estradiol (67.4±1.0%), 3α-sulfated-tibolone (85.8±5.3%), 3α-17β-disulfated-tibolone (71.9±2.5%), 3β-sulfated-tibolone (73.9±5.0%), and 3β-17β-disulfated-tibolone (65.8±3.4%) caused a significant decrease in superoxide production. Conclusively, although tibolone itself did not show significant antioxidant capacity, most of its active metabolites have antioxidant effects.

Original languageEnglish
Pages (from-to)31-35
Number of pages5
JournalGynecological Endocrinology
Issue number1
Publication statusPublished - Jan 1 2015



  • Antioxidant effect
  • Estradiol
  • Superoxide anion inhibition
  • Tibolone
  • Tibolone metabolites

ASJC Scopus subject areas

  • Endocrinology, Diabetes and Metabolism
  • Endocrinology
  • Obstetrics and Gynaecology

Cite this

Stark, J., Varbiro, S., Sipos, M., Tulassay, Z., Sara, L., Adler, I., Dinya, E., Magyar, Z., Szekacs, B., Marczell, I., Kloosterboer, H. J., Racz, K., & Bekesi, G. (2015). Antioxidant effect of the active metabolites of tibolone. Gynecological Endocrinology, 31(1), 31-35.