Stimulatory effect of genistein and apigenin on the growth of breast cancer cells correlates with their ability to activate ER alpha

Hye Sook Seo, David G. DeNardo, Yves Jacquot, Ioanna Laïos, Doris Salazar Vidal, Carmen Rojas Zambrana, Guy Leclercq, Powel H. Brown

Research output: Contribution to journalArticlepeer-review

120 Scopus citations

Abstract

Genistein and apigenin are phytoestrogens present in commercial preparations used for the treatment of postmenopausal symptoms. In this study, we assessed the influence of these compounds on mammary tumor growth. Both compounds stimulate the proliferation of MCF-7 and T47D cells [estrogen receptor alpha (ERα-positive)], but do not stimulate the proliferation of an ERα-negative cell line (MDA-MB-435 cells). Genistein appeared more efficient in this regard due to its higher binding affinity for ERα, a property explained by a structural analysis of the binding of these compounds to the ERα's ligand binding domain. As previously described for estradiol (E2), genistein and apigenin down regulated ERα and enhanced estrogen response element (ERE)-dependent gene expression. The additional finding that genistein antagonizes the anti-proliferative effect of hydroxytamoxifen suggests phytoestrogens may be detrimental in women with breast cancer who are being treated with tamoxifen. In addition, because of their ability to stimulate breast cell growth, the widespread use of phytoestrogens in postmenopausal women could be detrimental.

Original languageEnglish
Pages (from-to)121-134
Number of pages14
JournalBreast Cancer Research and Treatment
Volume99
Issue number2
DOIs
StatePublished - Sep 2006

Keywords

  • Apigenin
  • Breast cancer
  • Estrogen receptor
  • Genistein
  • Phytoestrogen

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