Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARα

Kinetic mechanism and product characterization of the enzymatic peroxidation of pterostilbene as model of the detoxification process of stilbene-type phytoalexins

“…It also appears to be a constituent of the bark of Guibourtia tessmanii, a tree found in central Africa and is commonly used in folk medicine (Fuendjiep et al, 2002). In addition to its antifungal role (Pezet and Pont, 1990;Mazullo et al, 2000), pterostilbene presents other biological activities, including antihyperglycemic (Manickam et al, 1997), antioxidative (Rimando et al, 2002;Kathryn et al, 2006;Remsberg et al, 2008), anticancer (Rimando et al, 2005;Kathryn et al, 2006;Remsberg et al, 2008;Pan et al, 2007;Nanjoo et al, 2007;Ferrer et al, 2005), antiinflammatory (Remsberg et al, 2008), anticholesterol (Mizuno et al, 2008;Mazullo et al, 2000), hypolipidemic (Mazullo et al, 2000) and analgesic (Mazullo et al, 2000) activities.…”

Pan‐PPAR Agonists Based on the Resveratrol Scaffold: Biological Evaluation and Docking Studies

“…In previous studies, simple functional groups were introduced at the 4'-position, and methoxy groups were introduced at the 3-and 5-positions of resveratrol. [12] From ongoing studies in our research group, a series of phenoxyalkylcarboxylic acid derivatives based on the resveratrol scaffold appear to have good hypolipidemic activity in vivo, and compound 3 was found to be the most potent. It was predicted that the hypolipidemic activity of 3 may be due to the activation of the PPARa, and the results of these studies will be reported elsewhere.…”

Natural Products of Dietary Origin as Lead Compounds in Virtual Screening and Drug Design

“…For instance, resveratrol has not been shown to be a powerful activator of the peroxisome proliferator receptor alpha (PPAR ), but its dimethylether analog was shown to activate PPAR (Rimando et al [26] cited in Mizuno et al [27]). Since PPAR is an important drug target in treating hypercholesterolemia, compound 9 can serve as a lead compound for developing additional agonists.…”

“…Since PPAR is an important drug target in treating hypercholesterolemia, compound 9 can serve as a lead compound for developing additional agonists. Mizuno et al [27] synthesized a series of pterostilbene analogs in an attempt of finding potent PPAR agonists. Compound 10, which is a phosphate derivative of compound 9, was observed to increase the activation of PPAR at least 100-fold when tested at 100 μM, which was more potent than the control compound ciprofibrate.…”