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

Abstract

Secoisolariciresinol diglucoside (SDG) is isolated from Linum usitatissimum seeds. 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. Lignan 1 has not shown cytotoxic effects on MCF-7 cells, while derivatives 2 and 3 have inhibited cell growth with IC50 values of 25 and 11 µM, respectively. Estrogen receptor alpha is a key growth driver in MCF-7 cells. Compound 1 did not affect the activity of ERα, while derivatives 2 and 3 showed significant antiestrogenic effects. Compounds 2 and 3 caused apoptosis in the MCF-7 line, determined by the cleavage of PARP. SDG derivative 3 enhanced 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.

• Authors: Alexander M Scherbakov, Olga V Stasevich, Diana I Salnikova, Olga E Andreeva, Ekaterina I Mikhaevich
• Journal: Natural product research (Nat Prod Res) Vol. 35 Issue 24 Pg. 6099-6105 (Dec 2021) ISSN: 1478-6427 [Electronic] England
• PMID: 33025821 (Publication Type: Journal Article)

Chemical References

• Butylene Glycols
• Glucosides
• Lignans
• secoisolariciresinol diglucoside

Topics

• Breast Neoplasms (drug therapy)
• Butylene Glycols (pharmacology)
• Female
• Flax
• Glucosides (pharmacology)
• Humans
• Lignans (pharmacology)
• MCF-7 Cells