A novel PI3K inhibitor alleviates fibrotic responses in fibroblasts derived from Peyronie's plaques

Int J Oncol. 2013 Jun;42(6):2001-8. doi: 10.3892/ijo.2013.1905. Epub 2013 Apr 16.

Abstract

Peyronie's disease (PD) is fibrosis localized in the tunica albuginea that is characterized by penile deformity and curvature. The pathogenesis of this disease remains unclear even though transforming growth factor-β (TGF-β)/smad signalling has been reported to be associated with PD. Recent studies have shown that phosphoinositide 3-kinase (PI3K)/Akt signalling regulates fibrotic responses including collagen synthesis and cell proliferation. Thus, we synthesized HS-173, a novel PI3K inhibitor, and determined whether this compound has anti-fibrotic effects on PD-derived primary fibroblasts. In this study, we found that HS-173 inhibited the growth of fibroblasts in a dose-dependent manner and induced apoptosis. In addition, HS-173 reduced the expression of α-smooth muscle actin (α-SMA), vimentin, PAI-1, fibronectin, collagen type I, collagen IV and TGF-β-activated smad2/3 in PD-derived primary fibroblasts. HS-173 blocked the PI3K/Akt signalling pathway by decreasing the activation of Akt, mTOR and P70S6K. Our results showed that HS-173 suppressed fibrotic responses such as cell proliferation and collagen synthesis by blocking PI3K/Akt signalling in PD-derived primary fibroblasts. Our findings provide molecular insights into the potential therapeutic action of HS-173 through targeting the PI3K/Akt pathway in PD-derived fibroblasts and demonstrated that HS-173 could be used as a pharmacological agent for treating other fibrotic diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Actins / metabolism
  • Apoptosis / drug effects
  • Cell Proliferation / drug effects
  • Collagen / metabolism
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / pharmacology*
  • Fibroblasts / drug effects*
  • Fibroblasts / metabolism*
  • Fibroblasts / pathology
  • Fibrosis / drug therapy
  • Humans
  • Male
  • Penile Induration / pathology*
  • Penis / pathology
  • Phosphoinositide-3 Kinase Inhibitors*
  • Proto-Oncogene Proteins c-akt / metabolism
  • Pyridines / pharmacology*
  • Signal Transduction / drug effects
  • Smad2 Protein / metabolism
  • Smad3 Protein / metabolism
  • Sulfonamides / pharmacology*
  • TOR Serine-Threonine Kinases / metabolism
  • Transforming Growth Factor beta1 / metabolism
  • Transforming Growth Factor beta1 / pharmacology
  • Vimentin / metabolism

Substances

  • ACTA2 protein, human
  • Actins
  • Enzyme Inhibitors
  • Phosphoinositide-3 Kinase Inhibitors
  • Pyridines
  • SMAD2 protein, human
  • SMAD3 protein, human
  • Smad2 Protein
  • Smad3 Protein
  • Sulfonamides
  • Transforming Growth Factor beta1
  • Vimentin
  • ethyl 6-(5-(phenylsulfonamido)pyridin-3-yl)imidazo(1,2-a)pyridine-3-carboxylate
  • Collagen
  • MTOR protein, human
  • Proto-Oncogene Proteins c-akt
  • TOR Serine-Threonine Kinases