Effect of tibolone and its principal metabolites (3α- and 3β-hydroxy, 3α-sulfate, and 4-ene derivatives) on estrone sulfatase activity in normal and cancerous human breast tissue

Abstract

AbstractTibolone (Org-OD14) is the active substance of LivialTissue minces were incubated with physiological concentrations of [The sulfatase activity was significantly higher in cancerous breast but strongly inhibited by tibolone and the different metabolites, whereas 3α- and 3β-hydroxy derivatives were the most potent inhibitors.This very significant inhibitory effect of tibolone and its principal metabolites on the enzyme involved in E