Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARalpha.
Pterostilbene, a naturally occurring analog of resveratrol, has previously shown PPARalpha activation in H4IIEC3 cells and was found to decrease cholesterol levels in animals. In this study, analogs of pterostilbene were synthesized and their ability to activate PPARalpha was investigated. Among analogs that was synthesized (E)-4-(3,5-dimethoxystyryl)phenyl dihydrogen phosphate showed activity higher than pterostilbene and control drug ciprofibrate. Docking of the stilbenes inside PPARalpha showed the presence of important hydrogen bond interactions for PPARalpha activation.
Mizuno
Cassia S
CS
USDA-ARS, Natural Products Utilization Research Unit, PO Box 8048, University, MS 38677, United States.
Ma
Guoyi
G
Khan
Shabana
S
Patny
Akshay
A
Avery
Mitchell A
MA
Rimando
Agnes M
AM
D000818:Animals; D045744:Cell Line, Tumor; D015195:Drug Design; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D047493:PPAR alpha / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding; D051381:Rats; D000077185:Resveratrol; D013267:Stilbenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D008024:Ligands; D047493:PPAR alpha; D013267:Stilbenes; C107773:pterostilbene; D000077185:Resveratrol