Estrogen modulation properties of mangiferin and quercetin and the mangiferin metabolite norathyriol

Abstract

Mango fruit contain many bioactive compounds, some of which are transcription factor regulators. Estrogen receptor alpha (ERα) and beta (ERβ) are two regulators of gene transcription that are important in a variety of physiological processes and also in diseases including breast cancer. We examined the ability of the mango constituents quercetin, mangiferin, and the aglycone form of mangiferin, norathyriol, to activate both isoforms of the estrogen receptor. Quercetin and norathyriol decreased the viability of MCF-7 breast cancer cells whereas mangiferin had no effect on MCF-7 cells. We also determined that quercetin and mangiferin selectively activated ERα whereas norathyriol activated both ERα and ERβ. Despite quercetin, mangiferin and norathyriol having similar polyphenolic structural motifs, only norathyriol activated ERβ, showing that bioactive agents in mangoes have very specific biological effects. Such specificity may be important given the often-opposing roles of ERα and ERβ in breast cancer proliferation and other cellular processes.

Mangiferin: a natural miracle bioactive compound against lifestyle related disorders

“…Estrogen receptor alpha (ERα) and beta (ERβ) are two regulators of gene transcription responsible for breast cancer. Mangiferin activates the estrogen receptor alpha (ERα) [39]. …”

Risks and benefits related to alimentary exposure to xenoestrogens

“…Recently, some PhyEs extracted from mango fruit, such as mangiferin and quercetin, were found to selectively activate ERα in breast cancer MCF-7 cells, whereas norathyriol, which is a metabolite of mangiferin, activates also ERβ (Wilkinson et al, 2015). Oleocanthal, a bioactive compound found in olive oil, showed to bind to both estrogen receptors, inducing either agonistic or antagonistic effects depending on the cell line.…”

Mangiferin and Cancer: Mechanisms of Action

“…In HL-60 cells, Li et al reinforced that mangiferin reduced proliferation [ 14 ]. In contrast, Wilkinson et al found that mangiferin did not suppress proliferation in MCF-7 cells, while mangiferin aglycone did [ 74 ]. This may be a result of differential activation of estrogen receptors [ 74 ].…”

“…In contrast, Wilkinson et al found that mangiferin did not suppress proliferation in MCF-7 cells, while mangiferin aglycone did [ 74 ]. This may be a result of differential activation of estrogen receptors [ 74 ]. Kim et al also reported no significant effect on proliferation when HeLa cells were treated with 25–200 µM of mangiferin [ 36 ] and Garcia-Rivera et al found no significant inhibition of proliferation in MDA-MB231 cells when treated with mangiferin, but proliferation was inhibited by Vimang ® [ 41 ].…”