Effect of nomegestrol acetate on estrone-sulfatase and 17β-hydroxysteroid dehydrogenase activities in human breast cancer cells

Steroid sulfatase inhibitors

“…(vi) Finally, medrogestone, a progestogen, blocked formation of E2 from E1S in intact breast cancer cells with IC 50 values of 1.9 mM (MCF-7 cells) or 0.21 mM (T-47D cells). 143 Mechanistic information with respect to STS is not available, but the compound also has stimulatory and inhibitory effects of sulfotransferase 143 and 17-b-hydroxysteroid dehydrogenase, 142 respectively.…”

“…(v) Nomegestrol acetate blocked formation of E2 from E1S in intact breast cancer cells by $70% at 50 mM, and also blocked the E1 to E2 conversion. 142 Again, the mechanism of STS inhibition is unknown. (vi) Finally, medrogestone, a progestogen, blocked formation of E2 from E1S in intact breast cancer cells with IC 50 values of 1.9 mM (MCF-7 cells) or 0.21 mM (T-47D cells).…”

Effect of nomegestrol acetate on estrogen biosynthesis and transformation in MCF-7 and T47-D breast cancer cells

“…NOMAC blocked significantly the conversion of E 1 S to E 2 at 50 M, 77% in the MCF-7 cells and 71% for the T47-D cells as can be seen in Fig. 3; [21]. At 1 M NOMAC and R5020 were equipotent on sulfatase activity in MCF-7 cells with 30% inhibition [22].…”

“…Since MCF-7 and T47-D cells are both PgR+ [71] and contain high levels of sulfatase activity (Table 5; [21,[72][73][74]), they are convenient models for the in vitro determination of anti-sulfatase potential of compounds such as progestins. For example, it has been shown that R5020 can significantly decrease the mRNA of the estrone sulfatase in MCF-7 cells [76].…”

“…As a 19-norprogesterone derived progestin nomegestrol acetate (NOMAC) has been shown to possess a global beneficial effect on the enzymes involved in estrogen biosynthesis in hormone-dependant breast cancer cells [18][19][20][21][22]. NO-MAC was also shown to inhibit the estrogen secretion of cultured granulosa cells from rat ovary in vitro [23].…”