title: Estrogen receptor mediated effects of Cimicifuga extracts on human breast cancer cells.
abstract: Cimicifuga racemosa extracts have long been used to treat female reproductive disorders both in Asia and Europe. Here in this study, we examined the possible estrogen receptor (ER)alpha effects of Cimicifuga heracleifolia var. bifida ethanol extract (C-Ex), which has been used traditionally in Asia, in MCF-7 cells. The activity of C-Ex was characterized in a transient transfection system, using ERa and estrogen-responsive luciferase plasmids in HEK 293 cells and endogenous target genes were studied in MCF-7 cells. C-Ex failed to activate ERalpha and at a concentration of 0.005-0.5 mg/ml as examined by reporter activity. In addition, no statistically significant antiestrogenic activity was observed. However, to our interest, C-Ex enhanced expression of VEGF at 0.5 mg/ml concentration and repressed ERalpha both at the mRNA and protein levels in MCF-7 cells. These results suggested that C-Ex does not activate or inactivate ERalpha in a direct manner, but the extracts may affect factors in ER signal transduction pathway.
authors.affiliation: College of Life Science, Institute of Biotechnology, Department of Bioscience and Biotechnology, Sejong University, Seoul, Korea.
authors.forename: Joonwoo
authors.initials: J
authors.lastname: Park
authors.forename: Myeongkuk
authors.initials: M
authors.lastname: Shim
authors.forename: Mee-Ra
authors.initials: MR
authors.lastname: Rhyu
authors.forename: YoungJoo
authors.initials: Y
authors.lastname: Lee
mesh_terms: D015153:Blotting, Western; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D049109:Cell Proliferation / Q000187:drug effects; D031885:Cimicifuga / Q000737:chemistry*; D015536:Down-Regulation / Q000187:drug effects; D047628:Estrogen Receptor alpha / Q000187:drug effects / Q000235:genetics; D005260:Female; D057809:HEK293 Cells; D006801:Humans; D008156:Luciferases / Q000235:genetics; D061986:MCF-7 Cells; D010936:Plant Extracts / Q000494:pharmacology; D060888:Real-Time Polymerase Chain Reaction; D011960:Receptors, Estrogen / Q000187:drug effects*; D015533:Transcriptional Activation / Q000187:drug effects; D042461:Vascular Endothelial Growth Factor A / Q000235:genetics
chemical_list: D047628:Estrogen Receptor alpha; D010936:Plant Extracts; D011960:Receptors, Estrogen; D042461:Vascular Endothelial Growth Factor A; D008156:Luciferases