Effects of protease activated receptor (PAR)2 blocking peptide on endothelin-1 levels in kidney tissues in endotoxemic rat mode

Life Sci. 2014 May 2;102(2):127-33. doi: 10.1016/j.lfs.2014.03.013. Epub 2014 Mar 16.

Abstract

Aims: Septic shock, the severe form of sepsis, is associated with development of progressive damage in multiple organs. Kidney can be injured and its functions altered by activation of coagulation, vasoactive-peptide and inflammatory processes in sepsis. Endothelin (ET)-1, a potent vasoconstrictor, is implicated in the pathogenesis of sepsis and its complications. Protease-activated receptors (PARs) are shown to play an important role in the interplay between inflammation and coagulation. We examined the time-dependent alterations of ET-1 and inflammatory cytokine, such as tumor necrosis factor (TNF)-α in kidney tissue in lipopolysaccharide (LPS)-induced septic rat model and the effects of PAR2 blocking peptide on the LPS-induced elevations of renal ET-1 and TNF-α levels.

Main methods: Male Wistar rats at 8 weeks of age were administered with either saline solution or LPS at different time points (1, 3, 6 and 10h). Additionally, we treated LPS-administered rats with PAR2 blocking peptide for 3h to assess whether blockade of PAR2 has a regulatory role on the ET-1 level in septic kidney.

Key findings: An increase in ET-1 peptide level was observed in kidney tissue after LPS administration time-dependently. Levels of renal TNF-α peaked (around 12-fold) at 1h of sepsis. Interestingly, PAR2 blocking peptide normalized the LPS-induced elevations of renal ET-1 and TNF-α levels.

Significance: The present study reveals a distinct chronological expression of ET-1 and TNF-α in LPS-administered renal tissues and that blockade of PAR2 may play a crucial role in treating renal injury, via normalization of inflammation, coagulation and vaso-active peptide.

Keywords: Endothelin-1; Kidney; Lipopolysaccharide; Protease activated receptor 2; Tumor necrosis factor-α.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Disease Models, Animal*
  • Endothelin-1 / antagonists & inhibitors
  • Endothelin-1 / biosynthesis*
  • Endothelin-1 / metabolism
  • Endotoxemia / chemically induced
  • Endotoxemia / drug therapy
  • Endotoxemia / metabolism*
  • Kidney Diseases / chemically induced
  • Kidney Diseases / drug therapy
  • Kidney Diseases / metabolism*
  • Lipopolysaccharides / administration & dosage
  • Male
  • Peptide Fragments / pharmacology*
  • Peptide Fragments / therapeutic use
  • Rats
  • Rats, Wistar
  • Receptor, PAR-2 / antagonists & inhibitors*
  • Receptor, PAR-2 / metabolism*
  • Treatment Outcome
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Endothelin-1
  • Lipopolysaccharides
  • Peptide Fragments
  • Receptor, PAR-2
  • Tumor Necrosis Factor-alpha