Review Article

Treatment of Obesity-Related Complications with Novel Classes of Naturally Occurring PPAR Agonists

Table 1

Summary of activities of novel classes of peroxisome proliferator-activated receptor (PPAR) agonists.

Punicic acidCatalpic acidAbscisic acid

PPAR α reporter activity1YesYesNo
PPAR γ reporter activity1YesNoYes
PPAR δ reporter activity1NoUnknownNo
PPAR γ ligand-binding activity2YesYesNo
PPAR γin silico Docking3YesYesNo
Changes in PPAR-responsive
genes in vivo 4
PPAR α in adipose tissue
PPAR γ in skeletal muscle
PPAR α in adipose tissuePPAR γ in adipose tissue
Efficacy in tissue-specific
PPAR γ null mice
ImpairedUnknownImpaired
PPAR-independent
Mechanisms
Modulation of eicosanoid synthesisDecreases cyclooxygenase-2 expressionLantionine synthetase
component C-like 2, cAMP, and protein kinase A
Proposed utilitiesGut Anti-inflammatory
Blood sugar control
Immune modulator
Antiobesity
Lipid-lowering
Anticancer
Systemic anti-inflammatory
Blood sugar control
Antiatherosclerotic
Immune modulator

1 PPAR α, γ, and δ reporter activity assays were conducted as previously described [22].
2 PPAR γ ligand-binding assay was performed using a commercially available competitive tracer displacement kit as previously described [42].
3 Molecular modeling and docking studies were performed as previously described [27, 43].
4 PPAR-responsive gene expression was measured in vivo as previously described [12].