Bisphenol A exerts estrogenic effects by modulating CDK1/2 and p38 MAP kinase activity

Biosci Biotechnol Biochem. 2014;78(8):1371-5. doi: 10.1080/09168451.2014.921557. Epub 2014 Jun 12.

Abstract

Bisphenol A (BPA) is considered to be an endocrine disruptor, but the mechanisms by which it disrupts endocrine functions are poorly understood. Here, we have shown that BPA binds both estrogen receptor (ER)-α and ER-beta (ER-β) using a fluorescence polarization competitive binding assay. In addition, we found that BPA induced cell proliferation by modulating cell cycle-related genes in the MCF-7 human mammary cancer cell line. Moreover, using a BG1 luciferase ER transactivation assay, we found that BPA has estrogenic activity. Modulating the MAPK pathway by using an ERK inhibitor (PD98059) or a JNK inhibitor (SP600125) had no effect on the ability of BPA to induce estrogenic activity. However, the antiestrogen, ICI 182,780, and the p38 inhibitor, PD 169316 successfully blocked BPA-induced estrogenic activity. Our findings suggest that BPA mimics ER-dependent estrogenic activity by targeting proteins that regulate the cell cycle and p38 MAPK.

Keywords: CDK1/2; Endocrine disruptors; bisphenol A; estrogenic activity; p38 MAPK.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzhydryl Compounds / metabolism
  • Benzhydryl Compounds / pharmacology*
  • CDC2 Protein Kinase / metabolism*
  • Cell Cycle / drug effects
  • Cell Cycle / genetics
  • Cell Proliferation / drug effects
  • Cyclin-Dependent Kinase 2 / metabolism*
  • Estrogen Receptor alpha / metabolism
  • Estrogen Receptor beta / metabolism
  • Estrogens / metabolism
  • Estrogens / pharmacology*
  • Humans
  • MCF-7 Cells
  • Phenols / metabolism
  • Phenols / pharmacology*
  • p38 Mitogen-Activated Protein Kinases / metabolism*

Substances

  • Benzhydryl Compounds
  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Estrogens
  • Phenols
  • CDC2 Protein Kinase
  • Cyclin-Dependent Kinase 2
  • p38 Mitogen-Activated Protein Kinases
  • bisphenol A