title: Estrogenic activity of xanthorrhizol isolated from curcuma xanthorrhiza ROXB.
abstract: Plant-derived estrogen-like compounds, or phytoestrogens, are given much attention due to their potential therapeutic use. In this study, xanthorrhizol, a natural sesquiterpenoid isolated from the rhizome of Curcuma xanthorrhiza ROXB. (Zingiberaceae), was evaluated for its estrogenic activity. It has been known that compounds acting as ligands for estrogen receptors (ERs) are considered to possess estrogenic activity. Therefore, the Gal-4/ER transactivation assay in transiently transfected African green monkey kidney (COS-7) cells was used to examine the estrogenic activity of xanthorrhizol. Both subtypes of ERs, ERalpha and ERbeta, were involved in this assay. Further transactivation assays and pS2 mRNA analysis were also conducted in estrogen receptor-positive human breast cancer (MCF-7). Our results showed that xanthorrhizol significantly increased Gal-4/ER luciferase activity in a dose-dependent manner and induced the endogenous ER-estrogen response element (ERE) interaction in MCF-7 cells. Xanthorrhizol also significantly enhanced the expression of the pS2 gene in MCF-7 cells. In contrast, treatment using ICI 182780, an ER antagonist, suppressed all activities induced by xanthorrhizol, indicating ER-dependant activities were involved. These results suggest that xanthorrhizol possesses estrogenic activity and its estrogenic effects are mediated by estrogen-induced gene expression.
authors.affiliation: Department of Biotechnology, Yonsei University, 134 Shinchon-dong, Seodaemun-gu, Seoul 120-749, South Korea.
authors.lastname: Anggakusuma
authors.lastname: Yanti
authors.forename: Myoungsu
authors.initials: M
authors.lastname: Lee
authors.forename: Jae-Kwan
authors.initials: JK
authors.lastname: Hwang
mesh_terms: D000818:Animals; D001483:Base Sequence; D019556:COS Cells; D045744:Cell Line, Tumor; D002522:Chlorocebus aethiops; D030024:Curcuma / Q000737:chemistry*; D017931:DNA Primers; D004958:Estradiol / Q000031:analogs & derivatives / Q000494:pharmacology; D020847:Estrogen Receptor Modulators / Q000494:pharmacology; D004967:Estrogens / Q000494:pharmacology*; D000077267:Fulvestrant; D006801:Humans; D010636:Phenols / Q000494:pharmacology*; D020133:Reverse Transcriptase Polymerase Chain Reaction
chemical_list: D017931:DNA Primers; D020847:Estrogen Receptor Modulators; D004967:Estrogens; D010636:Phenols; C120248:xanthorrhizol; D000077267:Fulvestrant; D004958:Estradiol