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    Tryptamine derivatives, their preparation and their use in gastropathy
    8.
    发明授权
    Tryptamine derivatives, their preparation and their use in gastropathy 有权
    色胺衍生物，它们的制备及其在胃病中的应用

    公开(公告)号：US08901317B2

    公开(公告)日：2014-12-02

    申请号：US13822463

    申请日：2011-09-14

    申请人： Uday Bandyopadhyay ,  Chinmay Pal ,  Samik Bindu ,  Susanta Sekhar Adhikari

    发明人： Uday Bandyopadhyay ,  Chinmay Pal ,  Samik Bindu ,  Susanta Sekhar Adhikari

    IPC分类号： C07D209/16

    CPC分类号： C07D209/16

    摘要： The synthesis and evaluation of gastroprotective effect of different tryptamine derivatives. Tryptamine derivatives have been synthesized by formation of amide or ester with some known anti oxidant molecules. These derivatives show excellent antioxidant property in vitro. Among all the derivatives the compound SEGA (3a), that was prepared by the combination of serotonin with gallic acid shows the greater antioxidant property than the other synthesized compounds both in vivo and in vitro. SEGA(3a) shows the gastroprotective effect against NSAIDs (indomethacin or diclofenac)-induced gastropathy in dose dependent manner and also accelerates the healing from injury. It prevents the NSAIDs-induced mitochondrial oxidative stress in vivo. This derivative prevents NSAID-induced mitochondrial oxidative stress-mediated apoptosis in vivo by preventing the activation of caspase 9 and caspase-3 and restores NSAIDs-mediated collapse of mitochondroial transmembrane potential and dehydrogenase activity. SEGA (3a) plays an important role as an iron chelator as well as intra mitochondrial ROS scavenger. Thus, SEGA (3a) is a potent antioxidant antiapototic molecule, which efficiently prevents NSAID-induced gastropathy and stress or alcohol-mediated gastric damage.

    摘要翻译： 不同色胺衍生物胃保护作用的合成与评价。 已经通过用一些已知的抗氧化剂分子形成酰胺或酯来合成色胺衍生物。 这些衍生物在体外显示出优异的抗氧化性能。 在所有衍生物中，通过5-羟色胺与没食子酸的组合制备的化合物SEGA（3a）在体内和体外都显示出比其它合成化合物更大的抗氧化性能。 SEGA（3a）显示了以剂量依赖的方式对NSAIDs（吲哚美辛或双氯芬酸）引起的胃肠病的胃保护作用，并加速了损伤愈合。 它可以预防体内NSAIDs诱导的线粒体氧化应激。 该衍生物通过阻止胱天蛋白酶9和半胱天冬酶-3的活化并且恢复NSAIDs介导的线粒体跨膜电位和脱氢酶活性的崩解来阻止NSAID诱导的线粒体氧化应激介导的细胞凋亡。 SEGA（3a）作为铁螯合剂以及内线粒体ROS清除剂起着重要的作用。 因此，SEGA（3a）是一种有效的抗氧化剂抗受损分子，可有效预防NSAID诱发的胃病和压力或醇介导的胃损伤。