Department of Pharmacology and Toxicology, Faculty of Pharmacy, Cairo University, Kasr El Aini st., Cairo, 11562, Egypt.
Department of Biochemistry, Graduate School of Medicine and Pharmaceutical Sciences, Toyama University, 2630 Sugitani, Toyama, 930-0194, Japan.
J Mol Neurosci. 2019 May;68(1):78-90. doi: 10.1007/s12031-019-01284-1. Epub 2019 Mar 12.
Long-term memory impairment is reported in more than 50% of cardiac arrest survivors. Monosialoganglioside (GM1) provided neuroprotection in experimental models of stroke but failed to replicate its promise clinically for unknown reasons. GM1 stimulates the release of nerve growth factor (NGF), which is synthesized as a precursor protein (pro-NGF) that either mediates apoptosis through the p75 neurotrophin receptor (p75NTR) or is cleaved by the protease furin (FUR) to yield mature NGF, the latter supporting survival through tropomyosin kinase receptor (Trk). The flavanol epicatechin (EPI) inhibits p75NTR-mediated signaling and apoptosis by pro-NGF. The aim of the current work is to test whether these two drugs affect, or communicate with, each other in the setting of CNS injuries. Using the two-vessel occlusion model of global ischemia/reperfusion (I/R), we tested if pharmacological modulation of Trk, p75NTR, and NGF balance with GM1, EPI, and their combination, can correct the memory deficit that follows this insult. Finally, we tested if FUR insufficiency and/or p75NTR-mediated apoptosis negatively affect the neurotherapeutic effect of GM1. Key proteins for Trk and p75NTR, FUR, and both forms of NGF were assessed. All treatment regiments successfully improved spatial memory retention and acquisition. A week after the insult, most Trk and p75NTR proteins were normal, but pro/mature NGF ratio remained sharply elevated and was associated with the poorest memory performance. Pharmacological correction of this balance was achieved by reinforcing Trk and p75NTR signaling. GM1 increased FUR levels, while concomitant administration of EPI weakened GM1 effect on pro-survival Trk and p75NTR mediators. GM1 neuroprotection is therefore not limited by FUR but could be dependent on p75NTR. Graphical Abstract "."
长期记忆损伤在超过 50%的心脏骤停幸存者中被报道。单唾液酸四己糖神经节苷脂 (GM1) 在实验性中风模型中提供了神经保护作用,但由于未知原因未能在临床上复制其疗效。GM1 刺激神经生长因子 (NGF) 的释放,NGF 作为前体蛋白 (pro-NGF) 合成,通过 p75 神经生长因子受体 (p75NTR) 介导细胞凋亡,或被蛋白酶 furin (FUR) 切割产生成熟的 NGF,后者通过原肌球蛋白激酶受体 (Trk) 支持存活。黄烷醇表儿茶素 (EPI) 通过 pro-NGF 抑制 p75NTR 介导的信号和细胞凋亡。目前的工作旨在测试这两种药物在中枢神经系统损伤的情况下是否相互影响或相互作用。我们使用两血管闭塞全脑缺血/再灌注 (I/R) 模型,测试 GM1、EPI 及其组合对 Trk、p75NTR 和 NGF 平衡的药理学调节是否可以纠正这种损伤后的记忆缺陷。最后,我们测试了 FUR 不足和/或 p75NTR 介导的细胞凋亡是否会对 GM1 的神经治疗效果产生负面影响。评估了用于 Trk 和 p75NTR 的关键蛋白、FUR 和两种形式的 NGF。所有治疗方案均成功改善了空间记忆保留和获得。损伤后一周,大多数 Trk 和 p75NTR 蛋白正常,但 pro/成熟 NGF 比值仍明显升高,并与最差的记忆表现相关。通过增强 Trk 和 p75NTR 信号转导来实现对这种平衡的药物矫正。GM1 增加了 FUR 水平,而同时给予 EPI 则削弱了 GM1 对生存促进的 Trk 和 p75NTR 介质的作用。因此,GM1 的神经保护作用不受 FUR 限制,而可能依赖于 p75NTR。