伊布地尔是一种磷酸二酯酶抑制剂,可防止人类免疫缺陷病毒-1 Tat 介导的小胶质细胞激活。

Ibudilast, a pharmacologic phosphodiesterase inhibitor, prevents human immunodeficiency virus-1 Tat-mediated activation of microglial cells.

机构信息

Department of Microbiology and Immunology, University of Rochester School of Medicine and Dentistry, Rochester, New York, United States of America.

出版信息

PLoS One. 2011 Apr 8;6(4):e18633. doi: 10.1371/journal.pone.0018633.

Abstract

Human Immunodeficiency Virus-1 (HIV-1)-associated neurocognitive disorders (HAND) occur, in part, due to the inflammatory response to viral proteins, such as the HIV-1 transactivator of transcription (Tat), in the central nervous system (CNS). Given the need for novel adjunctive therapies for HAND, we hypothesized that ibudilast would inhibit Tat-induced excess production of pro-inflammatory cytokines, such as tumor necrosis factor-alpha (TNFα) in microglial cells. Ibudilast is a non-selective cyclic AMP phosphodiesterase inhibitor that has recently shown promise as a treatment for neuropathic pain via its ability to attenuate glial cell activation. Accordingly, here we demonstrate that pre-treatment of both human and mouse microglial cells with increasing doses of ibudilast inhibited Tat-induced synthesis of TNFα by microglial cells in a manner dependent on serine/threonine protein phosphatase activity. Ibudilast had no effect on Tat-induced p38 MAP kinase activation, and blockade of adenosine A(2A) receptor activation did not reverse ibudilast's inhibition of Tat-induced TNFα production. Interestingly, ibudilast reduced Tat-mediated transcription of TNFα, via modulation of nuclear factor-kappa B (NF-κB) signaling, as shown by transcriptional activity of NF-κB and analysis of inhibitor of kappa B alpha (IκBα) stability. Together, our findings shed light on the mechanism of ibudilast's inhibition of Tat-induced TNFα production in microglial cells and may implicate ibudilast as a potential novel adjunctive therapy for the management of HAND.

摘要

人类免疫缺陷病毒 1(HIV-1)相关的神经认知障碍(HAND)的发生部分归因于中枢神经系统(CNS)中病毒蛋白(如 HIV-1 转录激活物(Tat))引起的炎症反应。鉴于 HAND 需要新的辅助治疗方法,我们假设伊布地尔将抑制 Tat 诱导的促炎细胞因子(如肿瘤坏死因子-α(TNFα))的过度产生。伊布地尔是一种非选择性环 AMP 磷酸二酯酶抑制剂,最近因其通过减轻神经胶质细胞激活来治疗神经性疼痛的能力而显示出希望。因此,在这里,我们证明伊布地尔预处理人和小鼠小胶质细胞,用递增剂量的伊布地尔抑制 Tat 诱导的 TNFα的合成由小胶质细胞以依赖丝氨酸/苏氨酸蛋白磷酸酶活性的方式。伊布地尔对 Tat 诱导的 p38 MAP 激酶激活没有影响,并且腺苷 A(2A)受体激活的阻断不能逆转伊布地尔对 Tat 诱导的 TNFα产生的抑制作用。有趣的是,伊布地尔通过调节核因子-κB(NF-κB)信号转导,降低 Tat 介导的 TNFα转录,如 NF-κB 的转录活性和抑制剂 kappa B alpha(IκBα)稳定性分析所示。总之,我们的研究结果阐明了伊布地尔抑制 Tat 诱导的小胶质细胞中 TNFα产生的机制,并可能暗示伊布地尔作为 HAND 管理的潜在新型辅助治疗方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f147/3072977/4e3066d201b7/pone.0018633.g001.jpg

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