Selective Estrogen Receptor Modulator (SERM)-like Activities of Diarylheptanoid, a Phytoestrogen from Curcuma comosa, in Breast Cancer Cells, Pre-osteoblast Cells, and Rat Uterine Tissues.
Diarylheptanoids from Curcuma comosa, of the Zingiberaceae family, exhibit diverse estrogenic activities. In this study we investigated the estrogenic activity of a major hydroxyl diarylheptanoid, 7-(3,4 -dihydroxyphenyl)-5-hydroxy-1-phenyl-(1E)-1-heptene (compound 092) isolated from C. comosa. The compound elicited different transcriptional activities of estrogen agonist at low concentrations (0.1-1 μM) and antagonist at high concentrations (10-50 μM) using luciferase reporter gene assay in HEK-293T cells. In human breast cancer (MCF-7) cells, compound 092 showed an anti-estrogenic activity by down-regulating ERα-signaling and suppressing estrogen-responsive genes, whereas it attenuated the uterotrophic effect of estrogen in immature ovariectomized rats. Of note, compound 092 promoted mouse pre-osteoblastic (MC3T3-E1) cell differentiation and the related bone markers, indicating its positive osteogenic effect. Our findings highlight a new, nonsteroidal, estrogen agonist/antagonist of catechol diarylheptanoid from C. comosa, which is scientific evidence supporting its potential as a dietary supplement to prevent bone loss with low risk of breast and uterine cancers in postmenopausal women.
['Thongon|Natthakan|N|', 'Boonmuen|Nittaya|N|', 'Suksen|Kanoknetr|K|', 'Wichit|Patsorn|P|', 'Chairoungdua|Arthit|A|', 'Tuchinda|Patoomratana|P|', 'Suksamrarn|Apichart|A|', 'Winuthayanon|Wipawee|W|', 'Piyachaturawat|Pawinee|P|http://orcid.org/0000-0002-1677-0777']
D016475:3T3 Cells D000818:Animals D001943:Breast Neoplasms D002454:Cell Differentiation D049109:Cell Proliferation D030024:Curcuma D036381:Diarylheptanoids D047628:Estrogen Receptor alpha D005260:Female D006801:Humans D051379:Mice D010006:Osteoblasts D048789:Phytoestrogens D010936:Plant Extracts D051381:Rats D017208:Rats, Wistar D020845:Selective Estrogen Receptor Modulators D014599:Uterus
diarylheptanoid phytoestrogens Curcuma comosa breast cancer estrogen agonist bone estrogen antagonist uterus