Department of Pharmacy, University of Naples Federico II, Napoli 80134, Italy.
Department of Translational Medical Science, University of Naples Federico II, Napoli 80131, Italy.
Int J Mol Sci. 2019 Feb 14;20(4):829. doi: 10.3390/ijms20040829.
Platinum(II) complexes with different cinnamic acid derivatives as ligands were investigated for their ability to inhibit the aggregation process of amyloid systems derived from Aβ, Yeast Prion Protein Sup35p and the C-terminal domain of nucleophosmin 1. Thioflavin T binding assays and circular dichroism data indicate that these compounds strongly inhibit the aggregation of investigated peptides exhibiting IC values in the micromolar range. MS analysis confirms the formation of adducts between peptides and Pt(II) complexes that are also able to reduce amyloid cytotoxicity in human SH-SY5Y neuroblastoma cells. Overall data suggests that bidentate ligands based on β-hydroxy dithiocinnamic esters can be used to develop platinum or platinoid compounds with anti-amyloid aggregation properties.
研究了不同肉桂酸衍生物作为配体的铂(II)配合物,以评估它们抑制源自 Aβ、酵母朊病毒蛋白 Sup35p 和核仁磷酸蛋白 1 末端结构域的淀粉样系统聚集过程的能力。噻唑蓝 T 结合分析和圆二色性数据表明,这些化合物强烈抑制所研究肽的聚集,其 IC 值在微摩尔范围内。MS 分析证实了肽与 Pt(II)配合物之间形成加合物,这些加合物还能够降低人 SH-SY5Y 神经母细胞瘤细胞中的淀粉样细胞毒性。总体数据表明,基于β-羟基二硫代肉桂酸酯的双齿配体可用于开发具有抗淀粉样聚集特性的铂或类铂化合物。