Guangxi Key Laboratory of Drug Discovery and Optimization, School of Pharmacy, Guilin Medical University, Guilin 541199, China; Lushan Rehabilitation and Recuperation Center, Jiujiang 332000, China.
Guangxi Key Laboratory of Drug Discovery and Optimization, School of Pharmacy, Guilin Medical University, Guilin 541199, China; The First Affiliated Hospital of Traditional Chinese Medicine of Guangzhou University, Ghuangzhou 510405, China.
Neuroscience. 2024 Aug 30;554:96-106. doi: 10.1016/j.neuroscience.2024.06.026. Epub 2024 Jul 2.
Cerebral ischemia/reperfusion injury (CIRI) is a common feature of ischemic stroke leading to a poor prognosis. Effective treatments targeting I/R injury are still insufficient. The study aimed to investigate the mechanisms, by which glycyrrhizic acid (18β-GA) in ameliorates CIRI. Our results showed that 18β-GA significantly decreased the infarct volume, neurological deficit scores, and pathological changes in the brain tissue of rats after middle cerebral artery occlusion. Western blotting showed that 18β-GA inhibited the expression levels of phosphorylated JAK2 and phosphorylated STAT3. Meanwhile, 18β-GA increased LC3-II protein levels in a reperfusion duration-dependent manner, which was accompanied by an increase in the Bcl-2/Bax ratio. Inhibition of 18β-GA-induced autophagy by 3-methyladenine (3-MA) enhanced apoptotic cell death. In addition, 18β-GA inhibited the JAK2/STAT3 pathway, which was largely activated in response to oxygen-glucose deprivation/reoxygenation. However, the JAK2/STAT3 activator colivelin TFA abolished the inhibitory effect of 18β-GA, suppressed autophagy, and significantly decreased the Bcl-2/Bax ratio. Taken together, these findings suggested that 18β-GA pretreatment ameliorated CIRI partly by triggering a protective autophagy via the JAK2/STAT3 pathway. Therefore might be a potential drug candidate for treating ischemic stroke.
脑缺血/再灌注损伤(CIRI)是缺血性脑卒中的共同特征,导致预后不良。针对 I/R 损伤的有效治疗方法仍然不足。本研究旨在探讨甘草酸(18β-GA)改善 CIRI 的机制。我们的结果表明,18β-GA 可显著减少大脑中动脉闭塞后大鼠的梗死体积、神经功能缺损评分和脑组织病理变化。Western blot 结果显示,18β-GA 抑制了磷酸化 JAK2 和磷酸化 STAT3 的表达水平。同时,18β-GA 以再灌注持续时间依赖性方式增加 LC3-II 蛋白水平,同时 Bcl-2/Bax 比值增加。3-甲基腺嘌呤(3-MA)抑制 18β-GA 诱导的自噬会增加细胞凋亡。此外,18β-GA 抑制 JAK2/STAT3 通路,该通路在氧葡萄糖剥夺/再复氧后被大量激活。然而,JAK2/STAT3 激活剂 colivelin TFA 消除了 18β-GA 的抑制作用,抑制自噬,并显著降低 Bcl-2/Bax 比值。综上所述,这些发现表明,18β-GA 预处理通过触发 JAK2/STAT3 通路的保护性自噬来改善 CIRI,因此可能是治疗缺血性脑卒中的潜在药物候选物。