Ashley N Ewens, Alexander Pilski, Shayne D Hastings, Chris Krook-Magnuson, Steven M Graves, Esther Krook-Magnuson, Stanley A Thayer
{"title":"在艾滋病毒相关神经认知障碍的 HIV-1 TAT 转基因小鼠模型中,左乙拉西坦能预防神经生理学变化并保护认知功能。","authors":"Ashley N Ewens, Alexander Pilski, Shayne D Hastings, Chris Krook-Magnuson, Steven M Graves, Esther Krook-Magnuson, Stanley A Thayer","doi":"10.1124/jpet.124.002272","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":16798,"journal":{"name":"Journal of Pharmacology and Experimental Therapeutics","volume":" ","pages":"104-118"},"PeriodicalIF":3.1000,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11413936/pdf/","citationCount":"0","resultStr":"{\"title\":\"Levetiracetam Prevents Neurophysiological Changes and Preserves Cognitive Function in the Human Immunodeficiency Virus (HIV)-1 Transactivator of Transcription Transgenic Mouse Model of HIV-Associated Neurocognitive Disorder.\",\"authors\":\"Ashley N Ewens, Alexander Pilski, Shayne D Hastings, Chris Krook-Magnuson, Steven M Graves, Esther Krook-Magnuson, Stanley A Thayer\",\"doi\":\"10.1124/jpet.124.002272\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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. 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引用次数: 0
摘要
在 3900 万艾滋病毒感染者中,近一半人患有艾滋病毒相关神经认知障碍(HAND)。HAND 的症状从亚临床认知障碍到痴呆不等;HAND 的发病机制尚不清楚,也没有治疗方法。艾滋病毒蛋白转录激活因子(TAT)被认为是导致 HAND 的原因,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。神经网络过度兴奋与神经退行性疾病的认知能力加速下降有关。在这里,我们发现抗癫痫药物左乙拉西坦(LEV)可以减轻异常兴奋性突触传递,保护突触可塑性,降低癫痫发作的易感性,并保护诱导性TAT(iTAT)转基因雄性小鼠的认知能力。iTAT小鼠在海马切片记录中的自发兴奋性突触后电流频率增加,长期电位(一种突触可塑性形式,是学习和记忆的基础)受损。通过渗透性微型泵给药两周的LEV可防止这两种损害。给 iTAT 小鼠注射凯尼酸会诱发较高的最大行为发作评分、较长的发作持续时间和较短的首次发作潜伏期,这与较低的发作阈值相符。LEV治疗可防止这些体内过度兴奋的迹象。最后,在巴恩斯迷宫中,与接受 LEV 治疗的 iTAT 小鼠相比,接受 LEV 治疗的 iTAT 小鼠需要更多时间才能到达目标,犯的错误更多,认知得分更低。因此,TAT的表达驱动了功能缺陷,表明它在手足徐动症中起着致病作用。由于LEV不仅能防止iTAT小鼠的突触活动异常,还能防止认知功能障碍,因此它可能为治疗手足徐动症提供一种很有前景的药理学方法。意义声明 约有一半的艾滋病病毒感染者患有艾滋病相关神经认知障碍(HAND),目前尚无治疗方法。艾滋病病毒蛋白 TAT 会引起毒性,被认为是导致 HAND 的原因之一。在这里,我们展示了一种抗癫痫药物--左乙拉西坦(LEV)--能防止TAT表达小鼠出现突触和认知障碍。左乙拉西坦被广泛用于治疗癫痫发作,在人类(包括艾滋病毒感染者)中的耐受性良好。这项研究支持进一步研究 LEV 治疗对 HAND 神经保护的作用。
Levetiracetam Prevents Neurophysiological Changes and Preserves Cognitive Function in the Human Immunodeficiency Virus (HIV)-1 Transactivator of Transcription Transgenic Mouse Model of HIV-Associated Neurocognitive Disorder.
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.
期刊介绍:
A leading research journal in the field of pharmacology published since 1909, JPET provides broad coverage of all aspects of the interactions of chemicals with biological systems, including autonomic, behavioral, cardiovascular, cellular, clinical, developmental, gastrointestinal, immuno-, neuro-, pulmonary, and renal pharmacology, as well as analgesics, drug abuse, metabolism and disposition, chemotherapy, and toxicology.