Laboratoire de Chimie Organique et Analytique, Faculté des Sciences et Techniques, Université Sultan Moulay Slimane, BP 523, 23000, Beni-Mellal, Morocco.
LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193, Aveiro, Portugal.
Eur J Med Chem. 2021 Mar 5;213:113140. doi: 10.1016/j.ejmech.2020.113140. Epub 2021 Jan 6.
The loss of neurons is strongly correlated with aging and aging-associated disorders. In this study, cell viability assays and mitochondrial function were performed to evaluate the effect of new spiro-pyrazole derivatives, prepared from aldehydes and 3-amino-1-phenyl-2-pyrazolin-5-one, on neuroprotection in an in vitro model of dopaminergic cell death induced by 1-methyl-4-phenylpyridinium (MPP). The percentages of neuroprotection by derivatives were found between 21.26% and 52.67% at selected concentrations (10-50 μM) with compound 4d exerting the best neuroprotective effect. The results show that the studied spiropyrazolones perform important roles in dopaminergic neuroprotection and can be used for potential new therapies in the treatment of neurodegenerative disorders including Parkinson's disease.
神经元的丢失与衰老和与衰老相关的疾病密切相关。在这项研究中，通过细胞活力测定和线粒体功能测定来评估新的螺吡唑衍生物对 1-甲基-4-苯基吡啶鎓（MPP）诱导的多巴胺能细胞死亡体外模型中神经保护的作用，这些螺吡唑衍生物是由醛和 3-氨基-1-苯基-2-吡唑啉-5-酮制备的。在选定的浓度（10-50 μM）下，衍生物的神经保护率在 21.26%和 52.67%之间，化合物 4d 表现出最好的神经保护作用。结果表明，所研究的螺吡唑酮在多巴胺能神经保护中发挥重要作用，可用于治疗包括帕金森病在内的神经退行性疾病的潜在新疗法。
