Estrogen modulation properties of mangiferin and quercetin and the mangiferin metabolite norathyriol.
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.
School of Pharmacy, The University of Queensland, Brisbane, QLD 4072, Australia. sarahrt@uq.edu.au.
Ashley S
AS
Wilkinson
Meng-Wong
MW
Taing
Jean Thomas
JT
Pierson
Chun-Nam
CN
Lin
Ralf G
RG
Dietzgen
P Nicholas
PN
Shaw
Michael J
MJ
Gidley
Gregory R
GR
Monteith
Sarah J
SJ
Roberts-Thomson
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D019556:COS Cells; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D065171:Estrogen Receptor Antagonists / Q000494:pharmacology; D047628:Estrogen Receptor alpha / Q000819:agonists* / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D047629:Estrogen Receptor beta / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D005260:Female; D005638:Fruit / Q000737:chemistry; D017930:Genes, Reporter / Q000187:drug effects; D006801:Humans; D061986:MCF-7 Cells; D031022:Mangifera / Q000737:chemistry; D009363:Neoplasm Proteins / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D048789:Phytoestrogens / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000494:pharmacology*; D011794:Quercetin / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000737:chemistry / Q000378:metabolism; D020218:Response Elements / Q000187:drug effects; D015533:Transcriptional Activation / Q000187:drug effects; D014966:Xanthenes / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000494:pharmacology*; D044004:Xanthones / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000494:pharmacology*
D000972:Antineoplastic Agents, Phytogenic; C506487:ESR1 protein, human; C000600034:ESR2 protein, human; D065171:Estrogen Receptor Antagonists; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D009363:Neoplasm Proteins; D048789:Phytoestrogens; D011994:Recombinant Proteins; D014966:Xanthenes; D044004:Xanthones; C013592:mangiferin; C069053:norathyriol; D011794:Quercetin