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2003 JUL 3 - (NewsRx.com & NewsRx.net) -- Tibolone exerts progestagenic effects on human endometrial cancer cells.
"Tibolone, a synthetic steroid acting in a tissue-specific manner and used in hormone replacement therapy, is converted into three active metabolites: a Delta(4) isomer (exerting progestagenic and androgenic effects) and two hydroxy metabolites, 3alpha-hydroxytibolone (3alpha-OH-tibolone) and 3beta-OH-tibolone (exerting estrogenic effects)," scientists writing in the Journal of Clinical Endocrinology and Metabolism report.
"In the present study an endometrial carcinoma cell line (Ishikawa PRAB-36) was used to investigate the progestagenic properties of tibolone and its metabolites. This cell line contains progesterone receptors A and B, but lacks estrogen and androgen receptors," wrote L.J. Blok and colleagues, Erasmus Medical Center.
"When tibolone was added to the cells, complete conversion into the progestagenic/androgenic Delta(4) isomer was observed within 6 d. Furthermore, when cells were cultured with tibolone or when the Delta(4) isomer or the established progestagen medroxyprogesterone acetate was added to the medium, marked inhibition of growth was observed," the researchers wrote.
"Interestingly, 3beta-OH-tibolone also induces some inhibition of growth. These growth inhibitions were not observed in progesterone receptor-negative parental Ishikawa cells, ...
Source: HighBeam Research, Tibolone exerts progestagenic effects on human endometrial cancer...