Han Xu, Tian Chuan, Gandra Ingrid, Eslava Valeria, Galindres Diana, Vargas Edgar, Leblanc Roger
Department of Chemistry, University of Miami, Coral Gables, FL, 33146, United States.
Department of Chemistry and Laufer Center for Physical and Quantitative Biology, Stony Brook University, Stony Brook, New York, 11794-3400, United States.
Chemistry. 2017 Dec 19;23(71):17903-17907. doi: 10.1002/chem.201704932. Epub 2017 Dec 4.
Different tail-engineered resorcinarenes have been examined for insulin fibrillation by experimental and computational studies. The resorcinarene showed a promising effect on the inhibition of insulin fibrillation, studied using a ThT assay, circular dichroism spectroscopy, and atomic force microscopy. Both the ThT assay and computational results indicate the tail from the resorcinarene has an impact on insulin fibrillation by either inhibition or promotion because of the resident position on insulin. These observations have significant biological implications in the design of drug molecules as well as the development of potential therapeutic strategies.
通过实验和计算研究，对不同尾部工程化的间苯二酚芳烃进行了胰岛素纤维化研究。使用硫黄素T（ThT）测定法、圆二色光谱法和原子力显微镜研究发现，间苯二酚芳烃对抑制胰岛素纤维化显示出有前景的效果。ThT测定法和计算结果均表明，由于间苯二酚芳烃的尾部在胰岛素上的驻留位置，其对胰岛素纤维化有抑制或促进作用。这些观察结果在药物分子设计以及潜在治疗策略开发方面具有重要的生物学意义。
