Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2021-08-08 , DOI: 10.1016/j.bmcl.2021.128312 Baskar Selvaraj 1 , Dae Woon Kim 2 , Jin-Soo Park 3 , Hak Cheol Kwon 3 , Heesu Lee 4 , Ki-Yeon Yoo 4 , Jae Wook Lee 1
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The neuroprotective activity of 2-heptyl-3-hydroxy-4(1H)-quinolone (compound 1) was evaluated using the neurotoxicity of glutamate in the HT22 cell line. Compound 1, known as a signal molecule of the bacterial quorum-sensing system, protects neuronal cells from glutamate-induced neurotoxicity by inhibiting cellular Ca2+ uptake and glutamate-triggered ROS accumulation. MAPK signaling pathway inhibition by compound 1 was evaluated by immunoblotting the phosphorylation status of the proteins. Furthermore, pro-apoptotic protein levels and AIF translocation to the nucleus were found to be reduced by compound 1. In conclusion, compound 1 showed neuroprotective effects by inhibiting apoptotic neuronal cell death.
中文翻译:
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2-庚基-3-羟基-4-喹诺酮对 HT22 小鼠海马神经元细胞的神经保护作用
使用 HT22 细胞系中谷氨酸的神经毒性评估 2-庚基-3-羟基-4(1H)-喹诺酮(化合物 1)的神经保护活性。化合物 1 被称为细菌群体感应系统的信号分子,通过抑制细胞 Ca 2+摄取和谷氨酸触发的 ROS 积累,保护神经元细胞免受谷氨酸诱导的神经毒性。通过免疫印迹蛋白质的磷酸化状态来评估化合物 1 对 MAPK 信号通路的抑制作用。此外,发现化合物1可降低促凋亡蛋白水平和AIF向细胞核的易位。总之,化合物1通过抑制凋亡性神经元细胞死亡而显示出神经保护作用。