Pterostilbene as a new agonist for the peroxisome proliferator-activated receptor alpha isoform
    3.
    发明申请
    Pterostilbene as a new agonist for the peroxisome proliferator-activated receptor alpha isoform 审中-公开
    作为过氧化物酶体增殖物激活受体α亚型的新型激动剂

    公开(公告)号:US20060057231A1

    公开(公告)日:2006-03-16

    申请号:US11207038

    申请日:2005-08-18

    摘要: Resveratrol, a stilbenoid antioxidant found in grapes, wine, peanuts and other berries, has been reported to have hypolipidemic properties. We investigated whether resveratrol and its three analogs (pterostilbene, piceatannol and resveratrol trimethyl ether) would activate the peroxisome proliferator-activated receptor alpha (PPARα) isoform. This nuclear receptor is proposed to mediate the activity of lipid-lowering drugs such as the fibrates. The four stilbenes were evaluated along with ciprofibrate (positive control) at 1, 10, 100, 300 μM concentrations, for the activation of endogenous PPARα in H4IIEC3 cells. Cells were transfected with a peroxisome proliferator response element-AB (rat fatty acyl CoA β-oxidase response element)—luciferase gene reporter construct. Of the four analogs, pterostilbene demonstrated the highest induction of PPARα showing 7- and 9-14 fold increases in luciferase activity at 100 and 300 μM, respectively, relative to control. The maximal luciferase activity responses to pterostilbene at 100 μM are similar to those obtained with the hypolipidemic drug, ciprofibrate. These results suggest that pterostilbene acts as a PPARα agonist, like that of the fibrate class, and may be a more effective hypolipidemic agent than resveratrol.

    摘要翻译: 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。 我们调查了白藜芦醇及其三种类似物(ter il ene,白藜芦醇和白藜芦醇三甲基醚)是否会激活过氧化物酶体增殖物激活受体α(PPARα)同种型。 提议这种核受体介导降脂药物如贝特类药物的活性。 在1,10,100,300μM浓度下,四环己烷与环丙哌酸(阳性对照)一起进行评估,以激活H4IIEC3细胞中的内源性PPARα。 用过氧化物酶体增殖物反应元件-AB(大鼠脂肪酰辅酶A氧化酶应答元件) - 荧光素酶基因报道构建体转染细胞。 在四种类似物中,萜烯二烯显示PPARα的诱导最高,显示相对于对照,分别为100和300μM的荧光素酶活性增加7和9-14倍。 对100μM的p芪烯的最大荧光素酶活性的反应与用降血脂药物环丙哌酸得到的相似。 这些结果表明,ter il ene ene ene。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。

    PREVENTING OR REDUCING OXIDATIVE STRESS OR OXIDATIVE CELL INJURY
    6.
    发明申请
    PREVENTING OR REDUCING OXIDATIVE STRESS OR OXIDATIVE CELL INJURY 审中-公开
    预防或减少氧化应激或氧化性细胞损伤

    公开(公告)号:US20090093441A1

    公开(公告)日:2009-04-09

    申请号:US11874663

    申请日:2007-10-18

    IPC分类号: A61K31/717 A61P3/00

    CPC分类号: A61K31/717

    摘要: A water-insoluble cellulose derivative, such as ethyl cellulose is useful for preventing or reducing oxidative stress or oxidative cell injury in tissues of an animal and in particular for influencing the level Stearoyl-CoA Desaturase-1 (SCD1) gene expression or ATP synthase mitochondrial F1 complex assembly factor 1 (ATPAF1) gene expression in non-adipose tissues of the animal.

    摘要翻译: 水不溶性纤维素衍生物如乙基纤维素可用于预防或减少动物组织中的氧化应激或氧化性细胞损伤,特别是用于影响硬脂酰辅酶A去饱和酶-1(SCD1)基因表达或ATP合成酶线粒体的水平 F1复合装配因子1(ATPAF1)基因在动物非脂肪组织中的表达。