The vitamin D receptor agonist elocalcitol inhibits IL-8-dependent benign prostatic hyperplasia stromal cell proliferation and inflammatory response by targeting the RhoA/Rho kinase and NF-kappaB pathways

Prostate. 2009 Apr 1;69(5):480-93. doi: 10.1002/pros.20896.

Abstract

Background: Benign prostatic hyperplasia (BPH) is characterized by an important inflammatory component. Stimulation of human prostate stromal cells from BPH tissues with proinflammatory cytokines leads to secretion of IL-8, a chemokine involved in BPH pathogenesis. The vitamin D receptor (VDR) agonist elocalcitol can arrest prostate growth in BPH patients, but its mechanism of action in this pathology is still incompletely understood.

Methods: IL-8 levels were measured by real-time RT-PCR and ELISA. NF-kappaB translocation and COX-2 expression were evaluated by confocal microscopy. RhoA and Rho-kinase (ROCK) gene expression and functional activity were studied by real-time RT-PCR, immuno-kinase assays, Western blot analysis, confocal microscopy, and cell invasion.

Results: Stimulation of BPH cells with IL-8 activates the calcium-sensitizing RhoA/ROCK pathway, as demonstrated by the increased membrane translocation of RhoA and by phosphorylation of the ROCK substrate myosin phosphatase target subunit 1 (MYPT-1). In agreement with these data, C3 exoenzyme, a selective RhoA inhibitor, inhibits IL-8-induced invasion of BPH cells. The VDR agonist elocalcitol significantly inhibits IL-8 production by BPH cells stimulated with inflammatory cytokines, and IL-8-induced proliferation of BPH cells. In addition, elocalcitol inhibits IL-8-induced membrane translocation of RhoA and MYPT-1 phosphorylation in BPH cells, and inhibits dose-dependently their IL-8-dependent invasion. The inhibition induced by elocalcitol of IL-8 production by BPH cells is accompanied by decreased COX-2 expression and PGE(2) production and by arrest of NF-kappaB p65 nuclear translocation, associated with inhibition of the RhoA/ROCK pathway.

Conclusions: These data provide a mechanistic explanation for the anti-proliferative and anti-inflammatory properties of elocalcitol in BPH cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calcitriol / analogs & derivatives*
  • Calcitriol / pharmacology
  • Cell Proliferation / drug effects
  • Cells, Cultured
  • Cyclooxygenase 2 / metabolism
  • Dinoprostone / metabolism
  • Humans
  • Inflammation / metabolism
  • Inflammation / pathology
  • Interferon-gamma / pharmacology
  • Interleukin-17 / pharmacology
  • Interleukin-8 / metabolism*
  • Male
  • NF-kappa B / metabolism*
  • Prostatic Hyperplasia / metabolism
  • Prostatic Hyperplasia / pathology*
  • Receptors, Calcitriol / agonists
  • Signal Transduction / drug effects
  • Stromal Cells / metabolism
  • Stromal Cells / pathology
  • Tumor Necrosis Factor-alpha / pharmacology
  • rho-Associated Kinases / metabolism*
  • rhoA GTP-Binding Protein / metabolism*

Substances

  • BXL628
  • Interleukin-17
  • Interleukin-8
  • NF-kappa B
  • Receptors, Calcitriol
  • Tumor Necrosis Factor-alpha
  • Interferon-gamma
  • Cyclooxygenase 2
  • rho-Associated Kinases
  • rhoA GTP-Binding Protein
  • Calcitriol
  • Dinoprostone