title: [Effect of xy2004, a centchroman derivative, on proliferation of MCF-7 cells in vitro and the mechanism].
abstract: OBJECTIVE
  To investigate the effect of xy2004, a centchroman derivative, on the proliferation of MCF-7 cells and the mechanisms.
  
  
  METHODS
  The effects of xy2004 on MCF-7 cell proliferation and apoptosis were evaluated with MTT assay and flow cytometry, respectively. The expressions of the apoptosis-related proteins were examined with Western blotting. Competitive estrogen-receptor binding assay was used to investigate the affinity of xy2004 to estrogen receptors (ER).
  
  
  RESULTS
  xy2004 induced proliferation of MCF-7 cells at low concentrations but inhibited cell proliferation at high concentrations. The application of tamoxifen inhibited xy2004-induced proliferation of MCF-7 cells. The relative binding affinity of xy9906 to ERα and ERβ, presented as the IC50 value, was 7.38 × 10⁻³ mol/L and 4.12 × 10⁻⁷ mol/L, respectively. Treatment of MCF-7 cells with high-concentration xy2004 reduced the cellular expression of Bcl-2 protein and increased Bax protein expression.
  
  
  CONCLUSIONS
  At low concentrations, xy2004 directly stimulates the proliferation of MCF -7 cells through ligand-receptor binding, and at high concentrations, it inhibits the cell proliferation by regulating the expression levels of the apoptosis-related proteins.
authors.affiliation: Department of Pharmacology, Xi'an Medical College, Xi'an 710068, China.E-mail: houandjin@hotmail.com.
authors.forename: Jin
authors.initials: J
authors.lastname: Hou
authors.forename: Ping
authors.initials: P
authors.lastname: Li
authors.forename: Jurong
authors.initials: J
authors.lastname: Zeng
authors.forename: Xiaoli
authors.initials: X
authors.lastname: Xu
authors.forename: Xiaoyun
authors.initials: X
authors.lastname: Xiong
authors.forename: Man
authors.initials: M
authors.lastname: Mi
mesh_terms: D017209:Apoptosis; D001943:Breast Neoplasms / Q000473:pathology*; D049109:Cell Proliferation; D002486:Centchroman / Q000494:pharmacology*; D047628:Estrogen Receptor alpha / Q000378:metabolism; D047629:Estrogen Receptor beta / Q000378:metabolism; D006801:Humans; D061986:MCF-7 Cells / Q000187:drug effects; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism; D013629:Tamoxifen; D051028:bcl-2-Associated X Protein / Q000378:metabolism
chemical_list: C494826:BAX protein, human; C000595707:BCL2 protein, human; C506487:ESR1 protein, human; C000600034:ESR2 protein, human; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D019253:Proto-Oncogene Proteins c-bcl-2; D051028:bcl-2-Associated X Protein; D013629:Tamoxifen; D002486:Centchroman