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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Discovery of ethyl urea derivatives as inhibitors of islet amyloid polypeptide fibrillization and cytotoxicity
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Discovery of ethyl urea derivatives as inhibitors of islet amyloid polypeptide fibrillization and cytotoxicity

机译：发现乙基脲衍生物可抑制胰岛淀粉样多肽的原纤维化和细胞毒性

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Islet amyloid polypeptide (IAPP) has been shown to form amyloid deposits in pancreatic islets, thereby furthering type 2 diabetes disease progression. Further discovery of new molecules is needed to create a diverse set of molecules that impede pancreatic amyloidosis. We have recently designed and synthesized N-phenyl-N'-(2-ethyl)ureas (EU) that are non-cytotoxic small molecules, to evaluate the role of the aryl-substituted moiety on the inhibition of hIAPP fibrillization. Several EUs were tested in vitro for their anti-amyloidogenic activity using the fluorometric ThT assay, the photo-induced cross-linking (PIUCP) assay, and cell survival assay in pancreatic MIN-6 cells. EU-362 and EU-418 were able to significantly inhibit the formation of hIAPP fibrils and protected cells from amyloid cytotoxic effects. Our results suggest that increasing the nucleophilic potency of the aryl moiety significantly enhances the anti-amyloidogenic activity of the molecules.
机译：胰岛淀粉样多肽（IAPP）已显示在胰岛中形成淀粉样沉积物，从而进一步促进了2型糖尿病的发展。需要新的分子的进一步发现以产生多种多样的阻止胰腺淀粉样变性的分子。我们最近设计和合成了非细胞毒性的小分子N-苯基-N'-（2-乙基）脲（EU），以评估芳基取代部分对hIAPP原纤维化抑制的作用。使用荧光ThT分析，光诱导交联（PIUCP）分析和胰腺MIN-6细胞的细胞存活分析，体外测试了几个EU的抗淀粉样生成活性。 EU-362和EU-418能够显着抑制hIAPP原纤维的形成，并保护细胞免受淀粉样蛋白的细胞毒性作用。我们的结果表明，增加芳基部分的亲核能力可显着增强分子的抗淀粉样活性。

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