Diaryheptanoid,
a structurally related phytoestrogen inhibiting the growth of estrogen dependent
breast cancer cells and its interaction with estrogen receptors
Bharathi Raja R., Anand S., Muthusamy V.S., Sarath Kumar B. and Lakshmi B.S.
Res. J. Biotech.; Vol. 20(4); 18-24;
doi: https://doi.org/10.25303/204rjbt018024; (2025)
Abstract
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.
