Department of Pharmacology, University of Minnesota Medical School, Minneapolis, Minnesota (A.N.E., A.P., S.M.G., S.A.T.); and Department of Neuroscience, University of Minnesota, Minneapolis, Minnesota (S.D.H., C.K.-M., E.K.-M.).
Department of Pharmacology, University of Minnesota Medical School, Minneapolis, Minnesota (A.N.E., A.P., S.M.G., S.A.T.); and Department of Neuroscience, University of Minnesota, Minneapolis, Minnesota (S.D.H., C.K.-M., E.K.-M.)
J Pharmacol Exp Ther. 2024 Sep 18;391(1):104-118. doi: 10.1124/jpet.124.002272.
Human immunodeficiency virus (HIV)-associated neurocognitive disorder (HAND) affects nearly half of the 39 million people living with HIV. HAND symptoms range from subclinical cognitive impairment to dementia; the mechanisms that underlie HAND remain unclear and there is no treatment. The HIV protein transactivator of transcription (TAT) is thought to contribute to HAND because it persists in the central nervous system and elicits neurotoxicity in animal models. Network hyperexcitability is associated with accelerated cognitive decline in neurodegenerative disorders. Here we show that the antiepileptic drug levetiracetam (LEV) attenuated aberrant excitatory synaptic transmission, protected synaptic plasticity, reduced seizure susceptibility, and preserved cognition in inducible TAT (iTAT) transgenic male mice. iTAT mice had an increased frequency of spontaneous excitatory postsynaptic currents in hippocampal slice recordings and impaired long-term potentiation, a form of synaptic plasticity that underlies learning and memory. Two-week administration of LEV by osmotic minipump prevented both impairments. Kainic acid administered to iTAT mice induced a higher maximum behavioral seizure score, longer seizure duration, and shorter latency to first seizure, consistent with a lower seizure threshold. LEV treatment prevented these in vivo signs of hyperexcitability. Lastly, in the Barnes maze, iTAT mice required more time to reach the goal, committed more errors, and received lower cognitive scores relative to iTAT mice treated with LEV. Thus, TAT expression drives functional deficits, suggesting a causative role in HAND. As LEV not only prevented aberrant synaptic activity in iTAT mice but also prevented cognitive dysfunction, it may provide a promising pharmacological approach to the treatment of HAND. SIGNIFICANCE STATEMENT: Approximately half of people living with human immunodeficiency virus (HIV) also suffer from HIV-associated neurocognitive disorder (HAND), for which there is no treatment. The HIV protein transactivator of transcription (TAT) causes toxicity that is thought to contribute to HAND. Here, the antiepileptic drug levetiracetam (LEV) prevented synaptic and cognitive impairments in a TAT-expressing mouse. LEV is widely used to treat seizures and is well-tolerated in humans, including those with HIV. This study supports further investigation of LEV-mediated neuroprotection in HAND.
人类免疫缺陷病毒(HIV)相关的神经认知障碍(HAND)影响了近 3900 万 HIV 感染者中的近一半。HAND 的症状范围从亚临床认知障碍到痴呆;导致 HAND 的机制仍不清楚,也没有治疗方法。HIV 蛋白转录激活剂(TAT)被认为是 HAND 的原因之一,因为它在中枢神经系统中持续存在,并在动物模型中引起神经毒性。网络过度兴奋与神经退行性疾病中认知能力的加速衰退有关。在这里,我们显示抗癫痫药物左乙拉西坦(LEV)减弱了异常的兴奋性突触传递,保护了突触可塑性,降低了癫痫易感性,并在诱导型 TAT(iTAT)转基因雄性小鼠中保存了认知功能。iTAT 小鼠在海马切片记录中具有更高的自发性兴奋性突触后电流频率,并损害了长时程增强,这是学习和记忆的基础形式的突触可塑性。通过渗透微泵给予两周的 LEV 治疗可预防这两种损伤。给予 iTAT 小鼠海人酸可诱导更高的最大行为性癫痫发作评分、更长的癫痫持续时间和更短的首次癫痫发作潜伏期,表明癫痫发作阈值降低。LEV 治疗可预防这些体内过度兴奋的迹象。最后,在 Barnes 迷宫中,iTAT 小鼠到达目标所需的时间更长,犯的错误更多,并且相对于用 LEV 治疗的 iTAT 小鼠,认知得分更低。因此,TAT 表达导致功能缺陷,提示其在 HAND 中起因果作用。由于 LEV 不仅预防了 iTAT 小鼠异常的突触活动,而且预防了认知功能障碍,因此它可能为 HAND 的治疗提供一种有前途的药物治疗方法。意义声明:大约一半的人类免疫缺陷病毒(HIV)感染者也患有 HIV 相关的神经认知障碍(HAND),目前尚无治疗方法。HIV 蛋白转录激活剂(TAT)引起的毒性被认为是 HAND 的原因之一。在这里,抗癫痫药物左乙拉西坦(LEV)预防了 TAT 表达的小鼠中的突触和认知障碍。LEV 被广泛用于治疗癫痫,并且在人类中包括 HIV 感染者中耐受良好。这项研究支持进一步研究 LEV 介导的 HAND 中的神经保护作用。