Modulation of G-Protein Coupled Oestrogen Receptor by Boerhavia diffusa
Nisaath Begum *
Department of Veterinary Pharmacology and Toxicology, College of Veterinary and Animal Sciences, Kerala Veterinary and Animal Sciences University, Mannuthy, Thrissur, Kerala, India.
S. Sujith
Department of Veterinary Pharmacology and Toxicology, College of Veterinary and Animal Sciences, Kerala Veterinary and Animal Sciences University, Mannuthy, Thrissur, Kerala, India.
AR. Nisha
Department of Veterinary Pharmacology and Toxicology, College of Veterinary and Animal Sciences, Kerala Veterinary and Animal Sciences University, Mannuthy, Thrissur, Kerala, India.
Preethy John
Department of Veterinary Pharmacology and Toxicology, College of Veterinary and Animal Sciences, Kerala Veterinary and Animal Sciences University, Mannuthy, Thrissur, Kerala, India.
R. Uma
Department of Veterinary Biochemistry, College of Veterinary and Animal Sciences, Kerala Veterinary and Animal Sciences University, Mannuthy, Thrissur, Kerala, India.
Dhanush Krishna
Department of Veterinary Pathology, College of Veterinary and Animal Sciences, Kerala Veterinary and Animal Sciences University, Mannuthy, Thrissur, Kerala, India.
VJ. Krishnanjana
Department of Veterinary Pharmacology and Toxicology, College of Veterinary and Animal Sciences, Kerala Veterinary and Animal Sciences University, Mannuthy, Thrissur, Kerala, India.
*Author to whom correspondence should be addressed.
Abstract
Aims: To investigate the effects of Boerhavia diffusa (B. diffusa) on oestrogen secretion and the expression of cytochrome P450 aromatase (CYP19) and G-protein-coupled oestrogen receptor (GPER) in Michigan Cancer Foundation-7 (MCF-7) cells, including their effects in combination with tamoxifen.
Study Design: In vitro experimental study involving phytochemical characterisation of B. diffusa extracts and fractions, followed by the evaluation of oestrogen concentrations in MCF-7 cell culture media and the subsequent analysis of CYP19 and GPER gene expression following combined treatment with B. diffusa and tamoxifen.
Place and Duration of Study: The study was conducted at the College of Veterinary and Animal Sciences, Mannuthy, Kerala Veterinary and Animal Sciences University (KVASU), Thrissur, Kerala, India, between December 2021 and November 2024.
Methodology: B. diffusa was prepared as a methanolic extract and its solvent fractions and characterised by phytochemical screening and Fourier transform infrared spectroscopy. MCF-7 cells were treated with concentrations corresponding to half IC₅₀, IC₅₀ and double IC₅₀ of B. diffusa and tamoxifen. Oestrogen concentrations in culture media were determined by radioimmunoassay after 48 and 96 h. The relative expression of CYP19 and GPER following combined treatment with B. diffusa and tamoxifen was evaluated using quantitative real-time PCR.
Results: Phytochemical analysis of B. diffusa revealed the presence of bioactive constituents, with functional groups confirmed by FTIR. Treatment with B. diffusa extract and its fractions reduced oestrogen concentrations in MCF-7 cell culture media compared with untreated controls, with a pronounced reduction observed after 96 h. The combination of the hexane fraction of B. diffusa and tamoxifen resulted in the lowest relative expression of CYP19 (0.02-fold) and GPER (0.26-fold) among the treatment groups.
Conclusion: B. diffusa inhibits MCF-7 cell proliferation and modulates GPER-mediated oestrogen signalling. This study highlights the potential of B. diffusa and its solvent fractions as sources of bioactive compounds capable of modulating GPER-related signalling, supporting further research into their possible application as complementary agents in hormone-dependent breast cancer.
Keywords: B. diffusa, GPER, CYP19, MCF-7, Tamoxifen