Investigating the effect of hesperitine on estrogen receptor expression, phosphorylation and activity in MCF-7 cells

Abstract

Abstract Background The most typical malignancy among women worldwide is breast cancer. Estrogen receptor play a vital role in this cancer. One of the most known mechanisms that affect the activity of this receptor is its phosphorylation by protein kinase pathways. Studies have shown that hesperetin has an effect on intracellular kinase pathways. Purpose The aim of this study was to investigate the effect of hesperetin on the level of expression, phosphorylation and activity of estrogen receptor . Study design and methods: MCF-7 cells were cultured in RPMI 1640 phenol red free medium containing charcoal stripped FBS and treated with hesperetin. MTT method was used to evaluate cell survival. The level of ERα protein and its phosphorylated form (Ser118) was determined by western blot technique. Luciferase reporter vector was used to evaluate ERE activity. Results The results of this study indicated that hesperetin reduced the survival of MCF-7 cells in a dose dependent manner. The level of expression and phosphorylation (Ser118) of estrogen receptor indicated a significant increase and decrease in the groups treated with hesperetin, respectively. Hesperetin increased the activity of the estrogen receptor in the nonexistence of E2, while in the existence of E2 it caused a significant decrease in receptor activity. Conclusion Based on the results of this study, it can be concluded that hesperetin has a significant effect on estrogen receptor expression, phosphorylation and activity probably through protein kinase pathways.