XIAP inhibitor and antiestrogen embelin abrogates metastasis and augments apoptosis in estrogen receptor positive human breast adenocarcinoma cell line MCF-7

Mol Biol Rep. 2014 Feb;41(2):935-46. doi: 10.1007/s11033-013-2938-z. Epub 2014 Jan 4.

Abstract

Tamoxifen therapy for the treatment of hormone responsive breast cancer has limitations due to acquired resistance in the case of recurrences. Embelin, a known inhibitor of X-linked inhibitor of apoptosis protein (XIAP) was also reported to exhibit strong antiestrogenic effects in animal models. Dual role of embelin as a proapoptotic and antiestrogenic agent may have potential benefits in the therapy of breast cancer. In this study, the effects of embelin treatment on estrogen receptor positive Human breast adenocarcinoma (MCF-7) cells was investigated to primarily understand if embelin being an antiestrogen and XIAP inhibitor could be a potential alternative to tamoxifen therapy. Results revealed that, embelin at a concentration of 65 μg/ml attenuated proliferation, inhibited metastatic migration, modulated the expression of Bcl2, Caspases and induced apoptosis in MCF-7 cells which was found to be p53 mediated. Hence, chemotherapy with embelin could be a promising strategy to be experimented in hormone responsive breast cancers.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma
  • Apoptosis / drug effects
  • Benzoquinones / pharmacology*
  • Cell Proliferation
  • Estrogen Receptor Modulators / pharmacology*
  • Female
  • Humans
  • MCF-7 Cells
  • Neoplasm Metastasis / drug therapy*
  • Receptors, Estrogen / metabolism
  • X-Linked Inhibitor of Apoptosis Protein / antagonists & inhibitors
  • X-Linked Inhibitor of Apoptosis Protein / genetics*

Substances

  • Benzoquinones
  • Estrogen Receptor Modulators
  • Receptors, Estrogen
  • X-Linked Inhibitor of Apoptosis Protein
  • XIAP protein, human
  • embelin