Department of Biomedical Laboratory Science, Konyang University, Daejeon 35365, Korea.
Department of Biochemistry and Molecular Biology, University of Ulsan College of Medicine, Seoul 05505, Korea.
BMB Rep. 2020 Nov;53(10):527-532. doi: 10.5483/BMBRep.2020.53.10.059.
We recently reported that N-adamantyl-4-methylthiazol-2-amine (KHG26693) attenuates glutamate-induced oxidative stress and inflammation in the brain. In this study, we investigated KHG 26693 as a therapeutic agent against glutamate-induced autophagic death of cortical neurons. Treatment with KHG26693 alone did not affect the viability of cultured cortical neurons but was protective against glutamate-induced cytotoxicity in a concentration-dependent manner. KHG26693 attenuated the glutamate-induced increase in protein levels of LC3, beclin-1, and p62. Whereas glutamate decreased the phosphorylation of PI3K, Akt, and mTOR, these levels were restored by treatment with KHG26693. These results suggest that KHG26693 inhibits glutamate-induced autophagy by regulating PI3K/Akt/mTOR signaling. Finally, KHG26693 treatment also attenuated glutamateinduced increases in reactive oxygen species, glutathione, glutathione peroxidase, and superoxide dismutase levels in cortical neurons, indicating that KHG26693 also protects cortical neurons against glutamate-induced autophagy by regulating the reactive oxygen species scavenging system. [BMB Reports 2020; 53(10): 527-532].
我们最近报道了 N-金刚烷基-4-甲基噻唑-2-胺(KHG26693)可减轻大脑中谷氨酸引起的氧化应激和炎症。在这项研究中,我们研究了 KHG26693 作为一种治疗剂,对抗谷氨酸诱导的皮质神经元自噬性死亡。单独使用 KHG26693 处理不会影响培养的皮质神经元的活力,但以浓度依赖的方式对谷氨酸诱导的细胞毒性具有保护作用。KHG26693 可减轻谷氨酸诱导的 LC3、beclin-1 和 p62 蛋白水平的增加。虽然谷氨酸降低了 PI3K、Akt 和 mTOR 的磷酸化水平,但这些水平可通过 KHG26693 处理得到恢复。这些结果表明,KHG26693 通过调节 PI3K/Akt/mTOR 信号通路抑制谷氨酸诱导的自噬。最后,KHG26693 处理还可减轻谷氨酸诱导的皮质神经元中活性氧、谷胱甘肽、谷胱甘肽过氧化物酶和超氧化物歧化酶水平的增加,表明 KHG26693 还通过调节活性氧清除系统来保护皮质神经元免受谷氨酸诱导的自噬。[BMB 报告 2020;53(10):527-532]。