Carrel Andrew, Napoli Eleonora, Hixson Kathryn, Carlsen Jessica, Cruz Del Angel Yasmin, Strode Dana, Busquet Nicolas, Kumar Vijay, Wempe Michael F, Russek Shelley J, Brooks-Kayal Amy R
Department of Pediatrics, University of Colorado School of Medicine, Aurora, CO, USA.
Department of Neurology, University of California Davis School of Medicine, Sacramento, CA, USA.
Neurotherapeutics. 2025 Mar;22(2):e00506. doi: 10.1016/j.neurot.2024.e00506. Epub 2024 Dec 5.
Molecules with optimized pharmacokinetic properties selectively aimed at the inhibition of STAT3 phosphorylation in brain have recently emerged as potential disease modifying therapies for epilepsy. In the current study, pharmacological inhibition of JAK1/2 with the orally available, FDA-approved drug ruxolitinib, produced nearly complete inhibition of hippocampal STAT3 phosphorylation, and reduced the expression of its downstream target Cyclin D1, when administered to rats 30 min and 3 h after onset of pilocarpine-induced status epilepticus (SE). This effect was accompanied by significantly shorter seizure duration and lower overall seizure frequency throughout the 4 weeks of EEG recording, but did not completely prevent the development of epilepsy in ruxolitinib-treated male rats. Compared to DMSO-treated animals, administration of ruxolitinib also improved memory (Y maze) but did not impact motor function (open field) following SE. Taken together with our previous findings, the results of this study provide further evidence that inhibition of the JAK/STAT pathway may be a promising disease modifying strategy to reduce severity of acquired epilepsy after brain injury, but also point to the need to better understand and optimize inhibitors of this pathway.
近期,具有优化药代动力学特性、选择性作用于抑制大脑中信号转导和转录激活因子3(STAT3)磷酸化的分子,已成为癫痫潜在的疾病改善疗法。在本研究中,使用美国食品药品监督管理局(FDA)批准的口服药物鲁索替尼对Janus激酶1/2(JAK1/2)进行药理抑制,在匹鲁卡品诱导的癫痫持续状态(SE)发作30分钟和3小时后给予大鼠,几乎完全抑制了海马体中STAT3的磷酸化,并降低了其下游靶点细胞周期蛋白D1的表达。在整个4周的脑电图记录中,这种作用伴随着癫痫发作持续时间显著缩短和总体发作频率降低,但并未完全阻止鲁索替尼治疗的雄性大鼠癫痫的发展。与二甲基亚砜(DMSO)处理的动物相比,给予鲁索替尼还改善了癫痫持续状态后的记忆(Y迷宫),但不影响运动功能(旷场试验)。结合我们之前的研究结果,本研究结果进一步证明,抑制JAK/STAT信号通路可能是一种有前景的疾病改善策略,可降低脑损伤后获得性癫痫的严重程度,但也表明需要更好地理解和优化该信号通路的抑制剂。