King's College London, Wolfson Centre for Age-Related Diseases, London SE1 1UL, United Kingdom Pain Research Group, Department of Surgery and Cancer, Imperial College London, London SW10 9NH, United Kingdom Neusentis, Pfizer Worldwide R&D, Cambridge CB21 6GS, United Kingdom King's College London, Institute of Psychiatry, Centre for the Cellular Basis of Behaviour, London SE5 9NU, United Kingdom UCL Genomics, UCL Cancer Institute and Wolfson Institute for Biomedical Research, London WC1E 6BT, United Kingdom Computational Sciences Center of Emphasis, Pfizer Worldwide Research and Development, Cambridge, MA, United States.
Pain. 2013 Sep;154(9):1668-1679. doi: 10.1016/j.pain.2013.05.021. Epub 2013 May 18.
Histone deacetylase inhibitors (HDACIs) interfere with the epigenetic process of histone acetylation and are known to have analgesic properties in models of chronic inflammatory pain. The aim of this study was to determine whether these compounds could also affect neuropathic pain. Different class I HDACIs were delivered intrathecally into rat spinal cord in models of traumatic nerve injury and antiretroviral drug-induced peripheral neuropathy (stavudine, d4T). Mechanical and thermal hypersensitivity was attenuated by 40% to 50% as a result of HDACI treatment, but only if started before any insult. The drugs globally increased histone acetylation in the spinal cord, but appeared to have no measurable effects in relevant dorsal root ganglia in this treatment paradigm, suggesting that any potential mechanism should be sought in the central nervous system. Microarray analysis of dorsal cord RNA revealed the signature of the specific compound used (MS-275) and suggested that its main effect was mediated through HDAC1. Taken together, these data support a role for histone acetylation in the emergence of neuropathic pain.
组蛋白去乙酰化酶抑制剂(HDACIs)干扰组蛋白乙酰化的表观遗传过程,已知在慢性炎症性疼痛模型中具有镇痛作用。本研究旨在确定这些化合物是否也会影响神经病理性疼痛。在创伤性神经损伤和抗逆转录病毒药物引起的周围神经病变(司他夫定、d4T)模型中,不同的 I 类 HDACIs 通过鞘内给药进入大鼠脊髓。HDACI 治疗可使机械和热敏感性降低 40%至 50%,但前提是在任何损伤之前开始治疗。这些药物在脊髓中普遍增加了组蛋白乙酰化,但在这种治疗模式下,似乎对相关的背根神经节没有可测量的影响,这表明任何潜在的机制都应该在中枢神经系统中寻找。背柱 RNA 的微阵列分析显示了特定化合物(MS-275)的特征,并表明其主要作用是通过 HDAC1 介导的。综上所述,这些数据支持组蛋白乙酰化在神经病理性疼痛出现中的作用。