Effect of xy2004, a centchroman derivative, on proliferation of MCF-7 cells in vitro and the mechanism.
- Author:
Jin HOU
1
;
Ping LI
;
Jurong ZENG
;
Xiaoli XU
;
Xiaoyun XIONG
;
Man MI
Author Information
- Publication Type:Journal Article
- MeSH: Apoptosis; Breast Neoplasms; pathology; Cell Proliferation; Centchroman; pharmacology; Estrogen Receptor alpha; metabolism; Estrogen Receptor beta; metabolism; Humans; MCF-7 Cells; drug effects; Proto-Oncogene Proteins c-bcl-2; metabolism; Tamoxifen; bcl-2-Associated X Protein; metabolism
- From: Journal of Southern Medical University 2014;34(10):1511-1514
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo investigate the effect of xy2004, a centchroman derivative, on the proliferation of MCF-7 cells and the mechanisms.
METHODSThe 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).
RESULTSxy2004 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.
CONCLUSIONAt 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.