Parthenolide, an NF-κB inhibitor, alleviates peritoneal fibrosis by suppressing the TGF-β/Smad pathway

Int Immunopharmacol. 2020 Jan:78:106064. doi: 10.1016/j.intimp.2019.106064. Epub 2019 Dec 12.

Abstract

Transforming growth factor (TGF)-β/Smad signalling plays a central role in the pathogenesis of peritoneal fibrosis related to peritoneal dialysis (PD). Parthenolide (PTL), a naturally occurring phytochemical, is isolated from the shoots of feverfew (Tanacetum parthenium) and displays analgesia, anti-inflammation and anticancer activities. In this study, we examined the therapeutic potential of PTL on PD-related peritoneal fibrosis induced by daily intraperitoneal injection of 4.25% dextrose-containing PD fluid (PDF) in vivo and TGF-β1-induced epithelial-mesenchymal transition (EMT) in vitro. PTL was administered daily before PDF injection or after 14 days of PDF injection. Both PTL treatments showed a protective effect on peritoneal fibrosis and prevented peritoneal dysfunction. Similarly, PTL suppressed the expression of fibrotic markers (fibronectin and collagen I) and restored the expression of the epithelial marker (E-cadherin) in TGF-β1-treated HMrSV5 cells. Furthermore, PTL inhibited TGF-β1-induced Smad2 and Smad3 phosphorylation and nuclear translocation but did not influence Smad1/5/9 phosphorylation or activate other downstream signalling pathways of TGF-β1, including AKT, extracellular signal-regulated kinase (ERK) or p38. In conclusion, PTL treatment may represent an effective and novel therapy for PD-associated peritoneal fibrosis by suppressing the TGF-β/Smad pathway.

Keywords: Parthenolide; Peritoneal fibrosis; Smad; TGF-β1.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use
  • Cell Line
  • Dialysis Solutions / administration & dosage
  • Dialysis Solutions / adverse effects
  • Disease Models, Animal
  • Drug Evaluation, Preclinical
  • Epithelial-Mesenchymal Transition / drug effects
  • Epithelial-Mesenchymal Transition / immunology
  • Female
  • Humans
  • Male
  • Mice
  • Peritoneal Dialysis / adverse effects*
  • Peritoneal Fibrosis / drug therapy*
  • Peritoneal Fibrosis / etiology
  • Peritoneal Fibrosis / immunology
  • Peritoneal Fibrosis / pathology
  • Peritoneum / cytology
  • Peritoneum / drug effects
  • Peritoneum / immunology
  • Peritoneum / pathology
  • Phosphorylation / drug effects
  • Phosphorylation / immunology
  • Sesquiterpenes / pharmacology*
  • Sesquiterpenes / therapeutic use
  • Signal Transduction / drug effects*
  • Signal Transduction / immunology
  • Smad Proteins / immunology
  • Smad Proteins / metabolism
  • Transforming Growth Factor beta1 / immunology
  • Transforming Growth Factor beta1 / metabolism

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Dialysis Solutions
  • Sesquiterpenes
  • Smad Proteins
  • Transforming Growth Factor beta1
  • parthenolide