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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.

ABSTRACT

Diarylheptanoids from Curcuma comosa (C. comosa), 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 being estrogen agonist at low concentrations (0.1-1 μM) and antagonist at higher 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 uterotrophic effect of estrogen in immature ovariectomized rats. Of note, compound-092 promoted mouse preosteoblastic (MC3T3-E1) cells 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 the scientific evidence supporting its potential as a dietary supplement to prevent bone loss with low risk of breast and uterine cancers in post-menopausal women.