Abstract
The peroxisome proliferator-activated receptor subtype α (PPARα) was established as a molecular target in drug discovery research for new lipid-lowering drugs. Pterostilbene is a naturally occurring PPARα agonist that has been shown to lower plasma lipid concentrations via the activation of PPARα. In this study, various pterostilbene conjugates with methyl, amino acid, and pivaloxymethyl (POM) groups at the 4-OH position were synthesized, and the activating effect on PPARα were investigated. Of the conjugates investigated, 4-OMe-pterostilbene had lower activating effect than pterostilbene, but the pterostilbenes with either amino acid (4a and 4b) or POM moiety (5) showed a small but significant increase in PPARα activation of PPARα activity compared to pterostilbene. Therefore, the structure-activity relationship of the pterostilbene conjugates studied indicates that substitution of the free 4-OH moiety of pterostilbene with a nonmethyl group can increase PPARα agonistic activity. This finding warrants further investigation of the structure-activity relationship of the pterostilbene conjugates as potent PPARα agonists.
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