Embelin inhibits proliferation, induces apoptosis and alters gene expression profiles in breast cancer cells.

ABSTRACT

PURPOSE: To investigate effect of embelin on proliferation, apoptosis and gene expression profile changes in breast cancer cells. METHODS: Cell viability was determined by MTT assay and apoptosis assayed using flow cytometry. Differential expression of 84 genes commonly involved in breast cancer carcinogenesis was assessed by real-time PCR using the Human Breast Cancer RT(2) Profiler PCR Array. RESULTS: MCF-7 and MDA-MB-231 cells were treated with embelin (0-25µM) for 24 and 96h. Embelin exhibited time and dose dependence in both cell lines and was more potent in inhibiting MDA-MB-231 cell proliferation compared to MCF-7 cells. IC50 for embelin in MDA-MB-231 cells was ∼4.45µM and 3.28µM at 24h and 96h, respectively. In contrast, IC50 for embelin in MCF-7 cells was ∼6.04µM and 4.51µM at 24h and 96h, respectively. Embelin (50µM) induced apoptosis and activated caspase 3 activity in both cell lines when exposed for 72h. Treatment of MDA-MB-231 cells with embelin (10µM) for 24h resulted in significant differential expression of 27 genes commonly involved in breast cancer carcinogenesis. CONCLUSIONS: Our findings show that embelin inhibits cell proliferation, induces apoptosis and alters expression of breast cancer focused genes in MCF-7 and MDA-MB-231 cells. Based on RT(2)-PCR array analysis, embelin down-regulated expression of pivotal oncogenes. This knowledge could be beneficial in the development of effective embelin-based therapies for treating breast cancer.