Tibolone: a compound with tissue specific inhibitory effects on sulfatase.
作者： Marcel E de Gooyer , George T Overklift Vaupel Kleyn , Karin C Smits , Antwan G.H Ederveen , Herman A.M Verheul
DOI: 10.1016/S0303-7207(01)00606-2
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摘要: Abstract The aim was to test whether sulfatase activity is differently regulated by tibolone in human bone, endometrium and breast cells since selective inhibition of sulfatases various tissues may contribute the tissue-specificity tibolone. Tibolone, its 3α- 3β-hydroxy metabolites their 3-sulfated forms, Δ4-isomer strongly (70–90%) inhibited cell lines (two T-47D clones) intermediately (8–43%) endometrial (HEC-1A). In contrast, they did not inhibit two osteoblast-like (MG 63, HOS TE-85). specific inhibitor, EMATE, showed all lines. Just as estrone sulfate, 3α-sulfated also converted unconjugated 3α-hydroxy-tibolone intracellularly tissue pattern suggest that could be protective against development mammary carcinomas, whereas it retains favorable estrogenic effects on bone.
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