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Anti-Inflammatory, Antioxidant, and WAT/BAT-Conversion Stimulation Induced by Novel PPAR Ligands: Results from Ex

Lucia Recinella1, Barbara De Filippis1, Maria Loreta Libero1

  • 1Department of Pharmacy, G. d'Annunzio University, 66100 Chieti, Italy.

Pharmaceuticals (Basel, Switzerland)
|March 29, 2023
PubMed

Insights

New peroxisome proliferator-activated receptor (PPAR) ligands were tested for their effects on inflammation and oxidative stress. PPAR agonist 1a significantly reduced inflammatory markers and promoted browning in adipocytes, suggesting its potential as a therapeutic lead.

Area of Science:

  • Pharmacology and Molecular Biology
  • Metabolic Regulation and Inflammation

Background:

  • Peroxisome proliferator-activated receptors (PPARs) are key regulators of metabolic pathways, inflammation, and oxidative stress.
  • Developing novel PPAR ligands is crucial for understanding and modulating these biological processes.

Purpose of the Study:

  • To investigate the effects of four novel PPAR ligands (agonists 1a, 1b and antagonists 2a, 2b) with a fibrate scaffold.
  • To evaluate their impact on inflammatory and oxidative stress biomarkers in liver tissue and on gene expression in adipocytes.

Main Methods:

  • Tested PPAR ligands (0.1-10 μM) on isolated liver specimens treated with lipopolysaccharide (LPS).
  • Measured lactate dehydrogenase (LDH), prostaglandin E2 (PGE2), and 8-iso-PGF2α levels.
  • Assessed gene expression of adipose tissue browning markers (UCP1, PRDM16, DIO2) and PPARα/γ in 3T3-L1 cells.

Main Results:

  • PPAR agonist 1a significantly reduced LPS-induced LDH, PGE2, and 8-iso-PGF2α levels.
  • PPAR agonist 1a and 1b modulated gene expression of browning markers (UCP1, DIO2) and PPARs in 3T3-L1 cells.
  • PPAR antagonists 2a and 2b reduced browning markers and PPARα/γ gene expression.

Conclusions:

  • The novel PPARα agonist 1a shows promise as a lead compound for managing inflammation and oxidative stress.
  • PPAR agonist 1b may have a role in regulating inflammatory pathways.
  • PPAR antagonists 2a and 2b negatively impacted adipocyte browning and PPAR expression.
Keywords:
PPAR modulatorsUCP1adipose tissueobesity

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