Effect of xy2004, a centchroman derivative, on proliferation of MCF-7 cells in vitro and the mechanism / 南方医科大学学报
Journal of Southern Medical University
;
(12): 1511-1514, 2014.
Article
in Chinese
| WPRIM
| ID: wpr-329257
ABSTRACT
<p><b>OBJECTIVE</b>To investigate the effect of xy2004, a centchroman derivative, on the proliferation of MCF-7 cells and the mechanisms.</p><p><b>METHODS</b>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).</p><p><b>RESULTS</b>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.</p><p><b>CONCLUSION</b>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.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pathology
/
Pharmacology
/
Tamoxifen
/
Breast Neoplasms
/
Centchroman
/
Apoptosis
/
Proto-Oncogene Proteins c-bcl-2
/
Estrogen Receptor alpha
/
Estrogen Receptor beta
/
Cell Proliferation
Limits:
Humans
Language:
Chinese
Journal:
Journal of Southern Medical University
Year:
2014
Type:
Article
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