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학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2013.1
- 수록면
- 353 - 356 (4page)
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초록· 키워드
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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.
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