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 acid
Catalpic acid
Abscisic acid
PPAR α reporter activity1
Yes
Yes
No
PPAR γ reporter activity1
Yes
No
Yes
PPAR δ reporter activity1
No
Unknown
No
PPAR γ ligand-binding activity2
Yes
Yes
No
PPAR γin silico Docking3
Yes
Yes
No
Changes in PPAR-responsive genes in vivo 4
PPAR α in adipose tissue PPAR γ in skeletal muscle
PPAR α in adipose tissue
PPAR γ in adipose tissue
Efficacy in tissue-specific PPAR γ null mice
Impaired
Unknown
Impaired
PPAR-independent Mechanisms
Modulation of eicosanoid synthesis
Decreases cyclooxygenase-2 expression
Lantionine synthetase component C-like 2, cAMP, and protein kinase A
Proposed utilities
Gut 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].