The dual PPAR-α/γ agonist saroglitazar ameliorates thioacetamide-induced liver fibrosis in rats through regulating leptin

Naunyn Schmiedebergs Arch Pharmacol. 2019 Dec;392(12):1569-1576. doi: 10.1007/s00210-019-01703-5. Epub 2019 Jul 31.

Abstract

Liver fibrosis is a challenging global health problem resulting from chronic liver injury with no treatment currently available. It has been shown that activators for different peroxisome proliferator-activated receptor (PPAR) isoforms (α, γ, and δ) can affect different pathways in liver fibrosis. To evaluate the effects of the dual PPAR-α/γ agonist saroglitazar (SGZ) against thioacetamide (TAA)-induced fibrosis in rats, SGZ was administered for 6 weeks together with TAA injection. Administration of SGZ ameliorated TAA-induced elevation in hepatic biomarkers. SGZ was able to inhibit periportal and intralobular fibrous connective tissue proliferation, to decrease hydroxyproline content, and to lower alpha smooth muscle actin (α-SMA) protein expression. To unearth the antifibrotic mechanism of SGZ, the role of several fibrotic markers was studied. SGZ possesses inhibitory effect on protein levels of leptin, transforming growth factor-beta 1 (TGF-β1) and platelet-derived growth factor-BB (PDGF-BB). Furthermore, SGZ rectified matrix degradation through decreasing tissue inhibitor of metalloproteinases-1 (TIMP-1). This study suggests that SGZ could have a possible antifibrotic effect via suppression of leptin that can repress TGF-β1 and PDFG-BB, with subsequent inhibition of TIMP-1.

Keywords: Leptin; Liver fibrosis; PDGF-BB; Saroglitazar (SGZ); TGF-β1; TIMP-1.

MeSH terms

  • Actins / metabolism
  • Animals
  • Becaplermin / metabolism
  • Leptin / metabolism
  • Liver / drug effects
  • Liver / metabolism
  • Liver / pathology
  • Liver Cirrhosis / chemically induced
  • Liver Cirrhosis / drug therapy*
  • Liver Cirrhosis / metabolism
  • Liver Cirrhosis / pathology
  • Male
  • PPAR alpha / agonists*
  • PPAR gamma / agonists*
  • Phenylpropionates / pharmacology
  • Phenylpropionates / therapeutic use*
  • Pyrroles / pharmacology
  • Pyrroles / therapeutic use*
  • Rats, Sprague-Dawley
  • Thioacetamide
  • Tissue Inhibitor of Metalloproteinase-1 / metabolism
  • Transforming Growth Factor beta1 / metabolism

Substances

  • Actins
  • Leptin
  • PPAR alpha
  • PPAR gamma
  • Phenylpropionates
  • Pyrroles
  • TIMP1 protein, rat
  • Tgfb1 protein, rat
  • Tissue Inhibitor of Metalloproteinase-1
  • Transforming Growth Factor beta1
  • smooth muscle actin, rat
  • Thioacetamide
  • Becaplermin
  • saroglitazar