会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 7. 发明申请
    • Pterostilbene as a new 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亚型的新型激动剂
    • US20060057231A1
    • 2006-03-16
    • US11207038
    • 2005-08-18
    • Agnes RimandoDennis FellerWallace Yokoyama
    • Agnes RimandoDennis FellerWallace Yokoyama
    • A61K36/45A61K36/87A61K31/704
    • 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. 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.
    • 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。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。