Pecora Desirée, Annunziata Francesca, Pegurri Sergio, Picone Pasquale, Pinto Andrea, Nuzzo Domenico, Tamborini Lucia
Department of Pharmaceutical Sciences, University of Milan, Via Mangiagalli 25, 20133 Milan, Italy.
Istituto per la Ricerca e l'Innovazione Biomedica (IRIB), CNR, Via Ugo La Malfa 153, 90146 Palermo, Italy.
Antioxidants (Basel). 2022 Oct 31;11(11):2160. doi: 10.3390/antiox11112160.
A series of phenolic derivatives designed to selectively target mitochondria were synthesized under flow conditions starting from natural phenolic acids. The two-step continuous flow protocol, performed in Cyrene, a bioavailable dipolar aprotic solvent, allowed the isolation of the MITO compounds in moderate to good yields. The MITO compounds obtained, as a first step, were tested for their safety by cell viability analysis. The cytocompatible dose, in human neuronal cell line SH-SH5Y, depends on the type of compound and the non-toxic dose is between 3.5 and 125 µM. Among the seven MITO compounds synthesized, two of them have shown interesting performances, being able to protect mitochondria from oxidative insult.
以天然酚酸为起始原料，在流动条件下合成了一系列旨在选择性靶向线粒体的酚类衍生物。在生物可利用的偶极非质子溶剂环丁砜中进行的两步连续流动方案，使得能够以中等至良好的产率分离出线粒体化合物（MITO化合物）。首先，通过细胞活力分析对所获得的MITO化合物的安全性进行了测试。在人神经母细胞瘤细胞系SH-SH5Y中，细胞相容性剂量取决于化合物的类型，无毒剂量在3.5至125 μM之间。在合成的七种MITO化合物中，其中两种表现出了有趣的性能，能够保护线粒体免受氧化损伤。
