Antiestrogenic and antiproliferative potency of secoisolariciresinol diglucoside derivatives on MCF-7 breast cancer cells. Issue 24 (17th December 2021)

• Record Type: Journal Article
• Authors: Scherbakov, Alexander M.; Stasevich, Olga V.; Salnikova, Diana I.; Andreeva, Olga E.; Mikhaevich, Ekaterina I.
• Is Part Of: Natural product research. Volume 35:Issue 24(2021)
• Page Start: 6099
• Page End: 6105
• Publication Date: 2021-12-17
• Subjects: Lignans -- secoisolariciresinol diglucoside -- derivatives -- secoisolariciresinol -- secoisolariciresinol-4′, 4″-diacetate -- breast cancer cells -- apoptosis -- cytotoxicity -- estrogen receptor; Natural products -- Periodicals; Natural products -- Research -- Periodicals; Biological Factors -- Periodicals; Biological Products -- Periodicals; 547
• DOI: 10.1080/14786419.2020.1826479
• Languages: English
• ISSNs: 1478-6419

Abstract

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. Abstract : UF0001