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Diarylheptanoids contribute to the estrogenic activity of Curcuma comosa.
Author(s) -
Tantrakool Wipawee,
Piyachaturawat Pawinee,
Suksamrarn Apichart,
Arao Yukitomo,
Hewitt Sylvia C.,
Korach Kenneth S.
Publication year - 2008
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.22.1_supplement.1220.4
Subject(s) - diarylheptanoids , pharmacology , chemistry , reporter gene , estrogen receptor , zingiberaceae , biology , biochemistry , medicine , traditional medicine , stereochemistry , rhizome , cancer , breast cancer , gene expression , gene
Extracts of Curcuma comosa , a plant in the Zingiberaceae family, exert estrogenic activity in in vivo and in vitro assays. Diarylheptanoids, a major component of C. comosa , are estrogenic in rat uterine bioassays, in an estrogen responsive yeast two‐hybrid system, and in MCF‐7 (human breast cancer) cells. This study aims to characterize further the estrogenic activity of C. comosa ‐derived diarylheptanoids. HepG2 cells expressing wild type or mutant forms of the mouse estrogen receptor‐α (ERα) and possessing an estrogen responsive reporter plasmid (3XERE‐TATA‐Luc) were exposed to increasing doses of diarylheptanoids. At 50 μM, the diarylheptanoids were equally efficient as 1 nM estradiol at stimulating ERE‐driven reporter activity, and this response was dose‐dependent. This activity was inhibited by the ER antagonist (ICI‐182780). A mutant ERα lacking the AF2 domain was unresponsive to the diarylheptanoids, while ERα lacking the AF1 domain exhibited wild type‐like activity. These data indicate that diarylheptanoids are active in an ER‐dependent system and this activity is dependent on ERα, more specifically its AF2 function. We therefore surmise that diarylheptanoids contribute to the estrogenic activity of C. comosa. Supported by Thailand Research Fund through Royal Golden Jubilee PhD Program (PHD/0255/2546) to WT and PP; BIOTEC grant to AS; NIEHS Division of Intramural Research Funding to WT, YA, SCH and KSK.