Piotrowska Dorota G, Mediavilla Laura, Cuarental Leticia, Głowacka Iwona E, Marco-Contelles José, Hadjipavlou-Litina Dimitra, López-Muñoz Francisco, Oset-Gasque María Jesús
Bioorganic Chemistry Laboratory, Faculty of Pharmacy, Medical University of Lodz, Muszyńskiego 1, 90-151 Łódź, Poland.
Department of Biochemistry and Molecular Biology, Faculty of Pharmacy, Complutense University of Madrid, Plaza Ramón y Cajal s/n, Ciudad Universitaria, 28040 Madrid, Spain.
ACS Omega. 2019 May 16;4(5):8581-8587. doi: 10.1021/acsomega.9b00189. eCollection 2019 May 31.
Herein, we report the synthesis and neuroprotective power of some N-substituted -(dialkoxy)phosphorylated nitrones -, by studying their ability to increase the cell viability, as well as their capacity to reduce necrosis and apoptosis. We have identified ()---butyl-1-(diethoxyphosphoryl)methanimine oxide () as the most potent, nontoxic, and neuroprotective agent, with a high activity against neuronal necrotic cell death, a result that correlates very well with its great capacity for the inhibition of the superoxide production (72%), as well as with the inhibition of lipid peroxidation (62%), and the 5-lipoxygenase activity (45%) at 100 μM concentrations. Thus, nitrone could be a convenient promising compound for further investigation.
在此,我们通过研究一些N-取代的-(二烷氧基)磷酰化硝酮增加细胞活力的能力及其减少坏死和凋亡的能力,报告了它们的合成及神经保护作用。我们已确定()---丁基-1-(二乙氧基磷酰基)甲亚胺氧化物()是最有效、无毒且具有神经保护作用的试剂,对神经元坏死性细胞死亡具有高活性,这一结果与其在100 μM浓度下对超氧化物生成(72%)、脂质过氧化(62%)及5-脂氧合酶活性(45%)的强大抑制能力密切相关。因此,硝酮可能是一种便于进一步研究的有前景化合物。