FLAVONE DERIVATIVES AND THEIR PREPARATIVE METHOD AND MEDICAL USE
    3.
    发明申请
    FLAVONE DERIVATIVES AND THEIR PREPARATIVE METHOD AND MEDICAL USE 有权
    FLAVONE衍生物及其制备方法和医疗用途

    公开(公告)号:US20130231492A1

    公开(公告)日:2013-09-05

    申请号:US13885063

    申请日:2010-11-12

    IPC分类号: C07D311/30

    CPC分类号: C07D311/30 A61K31/35

    摘要: Flavone derivatives, preparative method of the derivatives and use thereof as medicaments for treating diabetes. The structure of the derivatives is presented by formula 1: In the structure, R1 and R2, which are identical or not, represent hydrogen atom, halogen, cyano, hydroxyl, trifluoromethyl, thio-methyl, benzyloxy, C1-C8 linear chain or branch chain alkyl, C1-C8 linear chain or branch chain alkoxy. The pharmacological test indicates that the flavone derivatives can significantly increase the glucose consumption of Hep-G2 cell with insulin resistance activity, promote translocation of glucose transporter 4 of skeletal muscle cells (L6GLUT4myc) at different level, and significantly increase glucose intake and utilization by cells. The test proves the fact for the first time that the flavone derivatives can significantly promote translocation of glucose transporter 4 of skeletal muscle cells, and one of the mechanisms for treating diabetes is activating the cell AMPK phosphorylation and phosphorylating the downstream ACC.

    摘要翻译: 黄酮衍生物,衍生物的制备方法及其用作治疗糖尿病的药物。 衍生物的结构由式1表示:在结构中,相同或不相同的R1和R2表示氢原子,卤素,氰基,羟基,三氟甲基,硫代甲基,苄氧基,C1-C8直链或支链 链烷基,C1-C8直链或支链烷氧基。 药理试验表明,黄酮衍生物可显着增加Hep-G2细胞的葡萄糖消耗,具有胰岛素抵抗活性,促进骨骼肌细胞葡萄糖转运蛋白4(L6GLUT4myc)在不同水平的移位,并显着增加细胞摄入和利用细胞 。 该测试首次证实了黄酮衍生物可以第一次显着促进骨骼肌细胞葡萄糖转运蛋白4的移位,并且用于治疗糖尿病的机制之一是激活细胞AMPK磷酸化并磷酸化下游ACC。

    Flavone derivatives and their preparative method and medical use
    4.
    发明授权
    Flavone derivatives and their preparative method and medical use 有权
    黄酮衍生物及其制备方法和医疗用途

    公开(公告)号:US08946457B2

    公开(公告)日:2015-02-03

    申请号:US13885063

    申请日:2010-11-12

    CPC分类号: C07D311/30 A61K31/35

    摘要: Flavone derivatives, preparative method of the derivatives and use thereof as medicaments for treating diabetes. The structure of the derivatives is presented by formula 1: In the structure, R1 and R2, which are identical or not, represent hydrogen atom, halogen, cyano, hydroxyl, trifluoromethyl, thio-methyl, benzyloxy. C1-C8 linear chain or branch chain alkyl, C1-C8 linear chain or branch chain alkoxy. The pharmacological test indicates that the flavone derivatives can significantly increase the glucose consumption of Hep-G2 cell with insulin resistance activity, promote translocation of glucose transporter 4 of skeletal muscle cells (L6GLUT4myc) at different level, and significantly increase glucose intake and utilization by cells. The test proves the fact for the first time that the flavone derivatives can significantly promote translocation of glucose transporter 4 of skeletal muscle cells, and one of the mechanisms for treating diabetes is activating the cell AMPK phosphorylation and phosphorylating the downstream ACC.

    摘要翻译: 黄酮衍生物,衍生物的制备方法及其用作治疗糖尿病的药物。 衍生物的结构由式1表示:在结构中,相同或不同的R 1和R 2表示氢原子,卤素,氰基,羟基,三氟甲基,硫代甲基,苄氧基。 C1-C8直链或支链烷基,C1-C8直链或支链烷氧基。 药理试验表明,黄酮衍生物可显着增加Hep-G2细胞的葡萄糖消耗,具有胰岛素抵抗活性,促进骨骼肌细胞葡萄糖转运蛋白4(L6GLUT4myc)在不同水平的移位,并显着增加细胞摄取葡萄糖和细胞的利用 。 该测试首次证实了黄酮衍生物可以第一次显着促进骨骼肌细胞葡萄糖转运蛋白4的移位,并且用于治疗糖尿病的机制之一是激活细胞AMPK磷酸化并磷酸化下游ACC。