Direct inhibition of ERK1/2 phosphorylation as a possible mechanism for the antiproliferative action of 3,4-diOH-PCB3 in the MCF-7 cell line

Toxicol Lett. 2009 Oct 28;190(2):187-92. doi: 10.1016/j.toxlet.2009.07.013. Epub 2009 Jul 18.

Abstract

Our previously published data showed that 260h of exposure to 3,4-diOH-PCB3 decreased proliferation in the MCF-7 cell line. In the present study, we sought to determine whether this is due to action on the SHBG/cAMP/PKA system, activation of which can inhibit cell proliferation, or to direct inhibition of ERK1/2 phosphorylation. MCF-7 human breast cancer cells were treated for 72h with 4-monochlorobiphenyl (PCB3), 4'-hydroxy-4-monochlorobiphenyl (4-OH-PCB3) or 3'4'-dihydroxy-4-monochlorobiphenyl (3,4-diOH-PCB3) (300nM). After the completion of the treatment, cell proliferation was measured with a BrdU incorporation assay. SHBG, cAMP, PKA and ERK1/2 levels in the cells were determined via ELISA. PCB3 and 4-OH-PCB3 had no effect on extra- or intracellular SHBG levels, while a stimulation of SHBG intra- but not extracellular levels was noted in cells exposed to 3,4-diOH-PCB3. Both, pre- and co-incubation with SHBG decreased the proliferation of 3,4-diOH-PCB3-treated cells. Neither PCB3 nor its metabolite had an effect on the cAMP/PKA pathway. A decrease of both ERK1/2 forms was noted under the influence of 3,4-diOH-PCB3. In conclusion, the data presented clearly showed that the antiproliferative action of 3,4-diOH-PCB3 is not mediated by activation of the SHBG/AMP/PKA pathway, but many other plasma membrane receptors seem to be involved in the non-genomic action of 3,4-diOH-PCB3, and instead is due to direct inhibition of the ERK1/2 system.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Biphenyl Compounds / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects*
  • Cyclic AMP / metabolism
  • Cyclic AMP-Dependent Protein Kinases / metabolism
  • Female
  • Humans
  • Mitogen-Activated Protein Kinase 1 / metabolism*
  • Mitogen-Activated Protein Kinase 3 / metabolism*
  • Phosphorylation
  • Polychlorinated Biphenyls / pharmacology*
  • Second Messenger Systems / drug effects
  • Sex Hormone-Binding Globulin / metabolism
  • Signal Transduction / drug effects

Substances

  • 3',4'-dihydroxy-4-monochlorobiphenyl
  • Antineoplastic Agents
  • Biphenyl Compounds
  • Sex Hormone-Binding Globulin
  • Polychlorinated Biphenyls
  • Cyclic AMP
  • Cyclic AMP-Dependent Protein Kinases
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3