Antioxidant effect of the active metabolites of tibolone
| Autor: | Béla Székács, Istvan Marczell, Ildiko Adler, Levente Sara, Szabolcs Várbíró, Zsolt Tulassay, Julia Stark, Károly Rácz, Miklós Sipos, Gabor Bekesi, Helenius J. Kloosterboer, Zoltan Magyar, Elek Dinya |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
Adult
Male medicine.medical_specialty Antioxidant Norpregnenes Chemistry Endocrinology Diabetes and Metabolism medicine.medical_treatment Obstetrics and Gynecology Estrogens Tibolone Middle Aged Antioxidants Steroid Endocrinology Estrogen Receptor Modulators Superoxides Internal medicine medicine Humans Female Active metabolite Granulocytes medicine.drug |
| Zdroj: | Gynecological Endocrinology. 31:31-35 |
| ISSN: | 1473-0766 0951-3590 |
| DOI: | 10.3109/09513590.2014.943727 |
| Popis: | 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(-9 )M) of either estradiol, tibolone, 3α-hydroxytibolone, 3β-hydroxytibolone, Δ(4)-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(-9 )M of steroids. Using 10(-8 )M 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(-7 )M, 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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