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    • 1. 发明授权
    • Pterostilbene as an agonist for the peroxisome proliferator-activated receptor alpha isoform
    • 作为过氧化物酶体增殖物激活受体α亚型的激动剂的P芪烯
    • US08133917B2
    • 2012-03-13
    • US12911376
    • 2010-10-25
    • Agnes M. RimandoDennis R. FellerWallace H. Yokoyama
    • Agnes M. RimandoDennis R. FellerWallace H. Yokoyama
    • A61K31/075A61K38/00A01N65/00
    • A61K31/704A23L33/105A23V2002/00A61K31/352A61K36/45A61K36/87A23V2200/3262A23V2250/21
    • Resveratrol, a stilbenoid antioxidant found in grapes, wine, peanuts and other berries, has been reported to have hypolipidemic properties. Resveratrol and its three analogs (pterostilbene, piceatannol and resveratrol trimethyl ether) were evaluated for their effects on the activation of the peroxisome proliferator-activated receptor alpha (PPARα) isoforms, a receptor shown to mediate the activity of lipid-lowering drugs such as the fibrates. The four stilbenes and ciprofibrate (positive control) were evaluated for the activation of endogenous PPARα in H4IIEC3 cells. Pterostilbene demonstrated the highest induction of PPARα demonstrating increases of 7- and 9-14 fold relative to control. The maximal responses to pterostilbene are similar to those obtained with the hypolipidemic drug, ciprofibrate; that is, pterostilbene acts as a PPARα agonist, like that of the fibrate class, and is a more effective hypolipidemic agent than resveratrol.
    • 据报道,白藜芦醇是葡萄,葡萄酒,花生和其他浆果中发现的芪类抗氧化剂,具有降血脂性质。 评估白藜芦醇及其三种类似物(ter芪二烯,白藜芦醇和白藜芦醇三甲基醚)对过氧化物酶体增殖物激活受体α(PPARα)同工型的活化的影响,所述受体显示为介导降脂药物的活性,例如 贝特类。 评估了四苯并苯和环丙沙星(阳性对照)在H4IIEC3细胞中内源性PPARα的活化。 Pterostilbene表现出最高的PPARα诱导,显示相对于对照增加7和9-14倍。 对ter芪烯的最大反应与用降血脂药物环丙沙星获得的相似; 也就是说,ter芪烯作为PPARα激动剂,与贝特类相似,是比白藜芦醇更有效的降血脂药。
    • 9. 发明申请
    • Pterostilbene as a New Agonist for the Peroxisome Proliferator-Activated Receptor Alpha Isoform
    • Pterostilbene作为过氧化物酶体增殖物激活受体α亚型的新激动剂
    • US20110060060A1
    • 2011-03-10
    • US12911376
    • 2010-10-25
    • Agnes M. RimandoDennis R. FellerWallace H. Yokoyama
    • Agnes M. RimandoDennis R. FellerWallace H. Yokoyama
    • A61K31/09A61P3/06B65D69/00
    • A61K31/704A23L33/105A23V2002/00A61K31/352A61K36/45A61K36/87A23V2200/3262A23V2250/21
    • Resveratrol, a stilbenoid antioxidant found in grapes, wine, peanuts and other berries, has been reported to have hypolipidemic properties. Resveratrol and its three analogs (pterostilbene, piceatannol and resveratrol trimethyl ether) were evaluated for their effects on the activation of the peroxisome proliferator-activated receptor alpha (PPARα) isoforms, a receptor shown to mediate the activity of lipid-lowering drugs such as the fibrates. The four stilbenes and ciprofibrate (positive control) were evaluated for the activation of endogenous PPARα in H4IIEC3 cells. Pterostilbene demonstrated the highest induction of PPARα demonstrating increases of 7- and 9-14 fold relative to control. The maximal responses to pterostilbene are similar to those obtained with the hypolipidemic drug, ciprofibrate; that is, pterostilbene acts as a PPARα agonist, like that of the fibrate class, and is a more effective hypolipidemic agent than resveratrol.
    • 据报道,白藜芦醇是葡萄,葡萄酒,花生和其他浆果中发现的芪类抗氧化剂,具有降血脂特性。 评估白藜芦醇及其三种类似物(ter芪二烯,白藜芦醇和白藜芦醇三甲基醚)对过氧化物酶体增殖物激活受体α(PPARα)同工型的活化的影响,所述受体显示为介导降脂药物的活性,例如 贝特类。 评估了四苯并苯和环丙沙星(阳性对照)在H4IIEC3细胞中内源性PPARα的活化。 Pterostilbene表现出最高的PPARα诱导,显示相对于对照增加7和9-14倍。 对ter芪烯的最大反应与使用降血脂药物环丙沙星获得的类似; 也就是说,ter芪烯作为PPARα激动剂,与贝特类相似,是比白藜芦醇更有效的降血脂药。