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Design, Synthesis, and Biological Evaluation of Resveratrol Derivatives as $PPAR{\alpha}$ Agonists
Kim, Mi Kyoung,Chong, Youhoon 한국응용생명화학회 2013 Applied Biological Chemistry (Appl Biol Chem) Vol.56 No.3
The peroxisome proliferator-activated receptor subtype ${\alpha}$ ($PPAR{\alpha}$) was established as a molecular target in drug discovery research for new lipid-lowering drugs. Pterostilbene is a naturally occurring $PPAR{\alpha}$ agonist that has been shown to lower plasma lipid concentrations via the activation of $PPAR{\alpha}$. 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 $PPAR{\alpha}$ 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 $PPAR{\alpha}$ activation of $PPAR{\alpha}$ 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 $PPAR{\alpha}$ agonistic activity. This finding warrants further investigation of the structure-activity relationship of the pterostilbene conjugates as potent $PPAR{\alpha}$ agonists.
Plant Flavonoid O-Methyltransferases: Substrate Specificity and Application
김봉규,Su Hyun Sung,Youhoon Chong,Yoongho Lim,Joong-Hoon Ahn 한국식물학회 2010 Journal of Plant Biology Vol.54 No.5
Flavonoids consist of a large family of compounds,which has been estimated to bemore than 10,000 compounds. The structural diversity of these compounds comes from different modification reactions. The O-methylation reaction is one of the most important modification reactions of flavonoids and the resulting O-methylated flavonoids have been shown to display new biological activities. The regioselective and substrate specific O-methylation is mediated by O-methyltranferases (OMTs). To date, 30 flavonoid OMTs (FOMTs) have been biochemically characterized from various plants. FOMTs utilize common reaction mechanisms to transfer a methyl group to the hydroxyl group of the flavonoid. Phylogenetic tree analysis along with biochemical characterization of FOMTs provides clues about their substrate specificity and regioselectivity. FOMTs can be used for the production of O-methylated flavonoids that have a particular biological activity.