在匹罗卡平颞叶癫痫大鼠模型中,鲁索利替尼依赖性癫痫发作负荷和持续时间的减少伴随着空间记忆的改善。

IF 5.6 2区 医学 Q1 CLINICAL NEUROLOGY
Andrew Carrel, Eleonora Napoli, Kathryn Hixson, Jessica Carlsen, Yasmin Cruz Del Angel, Dana Strode, Nicolas Busquet, Vijay Kumar, Michael F Wempe, Shelley J Russek, Amy R Brooks-Kayal
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引用次数: 0

摘要

具有优化药代动力学特性的分子选择性地抑制大脑中STAT3磷酸化,最近成为癫痫的潜在疾病修饰疗法。在目前的研究中,fda批准的口服药物ruxolitinib对JAK1/2的药理学抑制,在匹罗卡品诱导的癫痫持续状态(SE)发作后30分钟和3小时给药时,几乎完全抑制海马STAT3磷酸化,并降低其下游靶点Cyclin D1的表达。在4周的脑电图记录中,这种作用伴随着癫痫发作持续时间明显缩短和总体发作频率明显降低,但并不能完全阻止鲁索利替尼治疗的雄性大鼠癫痫的发展。与dmso处理的动物相比,鲁索利替尼也改善了SE后的记忆(Y迷宫),但不影响运动功能(开放场)。结合我们之前的研究结果,本研究的结果进一步证明,抑制JAK/STAT通路可能是一种有希望的疾病调节策略,可以降低脑损伤后获得性癫痫的严重程度,但也指出需要更好地了解和优化该通路的抑制剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Ruxolitinib-dependent reduction of seizure load and duration is accompanied by spatial memory improvement in the rat pilocarpine model of temporal lobe epilepsy.

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.

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来源期刊
Neurotherapeutics
Neurotherapeutics 医学-神经科学
CiteScore
11.00
自引率
3.50%
发文量
154
审稿时长
6-12 weeks
期刊介绍: Neurotherapeutics® is the journal of the American Society for Experimental Neurotherapeutics (ASENT). Each issue provides critical reviews of an important topic relating to the treatment of neurological disorders written by international authorities. The Journal also publishes original research articles in translational neuroscience including descriptions of cutting edge therapies that cross disciplinary lines and represent important contributions to neurotherapeutics for medical practitioners and other researchers in the field. Neurotherapeutics ® delivers a multidisciplinary perspective on the frontiers of translational neuroscience, provides perspectives on current research and practice, and covers social and ethical as well as scientific issues.
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