Diaryheptanoid, a structurally related phytoestrogen inhibiting the growth of estrogen dependent breast cancer cells and its interaction with estrogen receptors

A decreased prevalence of breast cancer is associated with the excessive consumption of phytoestrogens which are biologically active plant-derived phenolic compounds that structurally mimic the mammalian estrogen, estradiol-17β. Consequently, hormone replacement therapy during the postmenopausal period is contraindicated in women with breast cancer. This study investigated the anti-estrogenic effects of DAH on the MCF-7 cell line, comparing its effects to the known anti-estrogen ICI182780. The anti-estrogenic effect was confirmed through an estrogen-inducible cell proliferation assay. The MTT assay demonstrated the anti-proliferative activity of DAH by confirming cell viability. An estrogen receptor binding assay showed DAH's capacity to bind to estrogen receptors. Furthermore, mRNA expression levels of pS2, an early-stage estrogen-responsive gene in estrogen-dependent breast cancer cell lines, were downregulated, further confirming the anti-estrogenic effect. Additionally, docking analysis using Autodock demonstrated the binding ability of DAH to the estrogen receptor.