Antiestrogenic and antiproliferative potency of secoisolariciresinol diglucoside derivatives on MCF-7 breast cancer cells

Secoisolariciresinol diglucoside (SDG) is isolated fromLinum usitatissimumseeds. The antiproliferative effects of SDG(1)and its derivatives secoisolariciresinol(2)and secoisolariciresinol-4 ', 4 ''-diacetate (3)have been evaluated on MCF-7 breast cancer cells and normal breast epithelial line MCF-10A. Lignan1has not shown cytotoxic effects on MCF-7 cells, while derivatives2and3have inhibited cell growth with IC(50)values of 25 and 11 mu M, respectively. Estrogen receptor alpha is a key growth driver in MCF-7 cells. Compound1did not affect the activity of ER alpha, while derivatives2and3showed significant antiestrogenic effects. Compounds2and3caused apoptosis in the MCF-7 line, determined by the cleavage of PARP. SDG derivative3enhanced the effect of doxorubicin. SDG derivatives can be considered as promising agents that exhibit a combined antiestrogen and proapoptotic effect in hormone-dependent breast cancer cells.

Automated summary

Research has shown that secoisolariciresinol diglucoside (SDG) and its derivatives exhibit inhibitory effects on cell growth and promotion of apoptosis in breast cancer cells, with significant impact on estrogen receptor activity.