Vol. 9, Special Issue 6, Part A (2024)

Oestrogen, the female reproductive hormone, acts through the classical nuclear (ERα and ERβ) and novel G protein coupled (GPER) receptor to carry out various physiological and pathological functions. Various plant extracts are known to modulate these receptor pathways and Boerrhavia diffusa, a rasayana herb having anticonvulsant, hepatoprotective, antibacterial, antiproliferative and anti-oestrogenic activities has been evaluated for its potential to modulate these receptors in the landscape of cancer therapeutics.

Methanolic extract and fractions of B. diffusa plant were assayed for cytotoxicity by MTT assay in MCF-7 cells. The IC50 was calculated by Graph pad prism and the cells were then exposed to half IC50, IC50 and double IC50 concentrations of the extracts for 96 hours and qRT-PCR was carried out for finding out the changes in the expression of ERα, ERβ and GPER genes by keeping GAPDH as control gene.

Methanolic, n-hexane, dichloromethane, n-butanol and water fractions of B. diffusa exhibited dose dependent decrease in cell viability as indicated by the increase in cytotoxicity. The extract and fractions of the plant caused significant modulation of the receptors. The methanolic and n-hexane fractions of the extract down regulated the expression of all the receptors with the butanol and water fractions upregulating ERα, Erβ. Tamoxifen downregulated expression of ERα, whereas it upregulated Erβ and GPER. The observed differential effects suggest a promising venue for target therapy in cancer mitigation.