Non-classical estrogen receptors action on human dermal fibroblasts

Taiwan J Obstet Gynecol. 2011 Dec;50(4):474-8. doi: 10.1016/j.tjog.2011.10.013.

Abstract

Objective: To study the possible non-genomic effect of selective estrogen receptor modulators on human dermal fibroblasts (HDF).

Materials and methods: WS1 cells were used to test the effect of raloxifene. The mRNA expressions of estrogen receptor (ER) α and β and G protein-coupled ER 1(GRP30) were examined by reverse transcription polymerase chain reaction. Apoptosis was identified by TUNEL assay and FACS analysis. MAPK and PI3 K/Akt pathways were determined by immunoblotting analysis.

Results: Neither ERα nor ERβ, but GPR30 was detected in WS1 cells. Raloxifene increased apoptosis, which was blocked by pertussis toxin, an inhibitor of G protein, or by LY294002. Phosphorylated p38 MAPK and Akt were also increased after raloxifene treatment.

Conclusion: SERMs could induce apoptosis of HDF through G protein and PI3 K/Akt signaling, which may help understand the role of SERMs on the skin.

MeSH terms

  • Apoptosis / drug effects*
  • Cell Line
  • Dermis / cytology
  • Dermis / drug effects*
  • Estrogen Receptor alpha / metabolism
  • Estrogen Receptor beta / metabolism
  • Fibroblasts / drug effects*
  • Fibroblasts / metabolism
  • Humans
  • Immunoblotting
  • In Situ Nick-End Labeling
  • Mitogen-Activated Protein Kinases / metabolism
  • Phosphatidylinositol 3-Kinases / metabolism
  • Proto-Oncogene Proteins c-akt / metabolism
  • Raloxifene Hydrochloride / pharmacology*
  • Receptors, Estrogen / metabolism
  • Receptors, G-Protein-Coupled / metabolism
  • Reverse Transcriptase Polymerase Chain Reaction
  • Selective Estrogen Receptor Modulators / pharmacology*

Substances

  • ESR1 protein, human
  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • GPER1 protein, human
  • Receptors, Estrogen
  • Receptors, G-Protein-Coupled
  • Selective Estrogen Receptor Modulators
  • Raloxifene Hydrochloride
  • Proto-Oncogene Proteins c-akt
  • Mitogen-Activated Protein Kinases