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用于生物医学应用的苯并二呋喃:BZ4,一种具有选择性抗增殖和抗淀粉样蛋白作用的先导化合物。

Benzodifurans for biomedical applications: BZ4, a selective anti-proliferative and anti-amyloid lead compound.

作者信息

Vicidomini Caterina, Cioffi Federica, Broersen Kerensa, Roviello Valentina, Riccardi Claudia, Montesarchio Daniela, Capasso Domenica, Gaetano Sonia Di, Musumeci Domenica, Roviello Giovanni N

机构信息

CNR, Institute of Biostructure & Bioimaging, Via Mezzocannone site & Headquarters, 80134 Naples, Italy.

Nanobiophysics, Faculty of Science & Technology (TNW), Technical Medical Centre, University of Twente, The Netherlands.

出版信息

Future Med Chem. 2019 Feb;11(4):285-302. doi: 10.4155/fmc-2018-0473. Epub 2019 Feb 25.

Abstract

Our goal is to evaluate benzodifuran-based scaffolds for biomedical applications. We here explored the anticancer and anti-amyloid activities of a novel compound (BZ4) in comparison with other known benzodifuran analogs, previously studied in our group, and we have explored its ability to interact with different DNA model systems. BZ4 shows antiproliferative activity on different cancer cells; does not affect noncancerous control cells and alters the aggregation properties of β-amyloid, as ascertained by circular dichroism, fluorescence spectroscopy and scanning electron microscopy analysis. An overall, qualitative picture on the mechanistic aspects related to the biological activities is discussed in light of the dynamic light scattering, UV, circular dichroism and fluorescence data, as well as of the metal ion-binding properties of BZ4.

摘要

我们的目标是评估基于苯并二呋喃的支架在生物医学领域的应用。在此,我们探究了一种新型化合物(BZ4)与我们小组之前研究过的其他已知苯并二呋喃类似物相比的抗癌和抗淀粉样蛋白活性,并研究了它与不同DNA模型系统相互作用的能力。BZ4对不同癌细胞显示出抗增殖活性;不影响非癌对照细胞,并改变β-淀粉样蛋白的聚集特性,这通过圆二色性、荧光光谱和扫描电子显微镜分析得以确定。根据动态光散射、紫外、圆二色性和荧光数据以及BZ4的金属离子结合特性,讨论了与生物活性相关的作用机制方面的整体定性情况。

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