Pithadia Amit, Brender Jeffrey R, Fierke Carol A, Ramamoorthy Ayyalusamy
Biophysics and Department of Chemistry, University of Michigan, Ann Arbor, MI 48109-1055, USA.
J Diabetes Res. 2016;2016:2046327. doi: 10.1155/2016/2046327. Epub 2015 Nov 15.
Fibrillar aggregates of human islet amyloid polypeptide, hIAPP, a pathological feature seen in some diabetes patients, are a likely causative agent for pancreatic beta-cell toxicity, leading to a transition from a state of insulin resistance to type II diabetes through the loss of insulin producing beta-cells by hIAPP induced toxicity. Because of the probable link between hIAPP and the development of type II diabetes, there has been strong interest in developing reagents to study the aggregation of hIAPP and possible therapeutics to block its toxic effects. Natural products are a class of compounds with interesting pharmacological properties against amyloids which have made them interesting targets to study hIAPP. Specifically, the ability of polyphenolic natural products, EGCG, curcumin, and resveratrol, to modulate the aggregation of hIAPP is discussed. Furthermore, we have outlined possible mechanistic discoveries of the interaction of these small molecules with the peptide and how they may mitigate toxicity associated with peptide aggregation. These abundantly found agents have been long used to combat diseases for many years and may serve as useful templates toward developing therapeutics against hIAPP aggregation and toxicity.
人胰岛淀粉样多肽(hIAPP)的纤维状聚集体是一些糖尿病患者的病理特征,可能是胰腺β细胞毒性的致病因素,通过hIAPP诱导的毒性导致胰岛素产生β细胞的丧失,从而使机体从胰岛素抵抗状态转变为II型糖尿病。由于hIAPP与II型糖尿病的发生可能存在联系,人们对开发研究hIAPP聚集的试剂以及阻止其毒性作用的可能疗法有着浓厚兴趣。天然产物是一类对淀粉样蛋白具有有趣药理特性的化合物,这使得它们成为研究hIAPP的有趣靶点。具体讨论了多酚类天然产物表没食子儿茶素没食子酸酯(EGCG)、姜黄素和白藜芦醇调节hIAPP聚集的能力。此外,我们概述了这些小分子与该肽相互作用可能的机制发现,以及它们如何减轻与肽聚集相关的毒性。这些广泛存在的物质多年来一直用于对抗疾病,可能成为开发针对hIAPP聚集和毒性疗法的有用模板。