Mao Yu, Zhou Jing, Liu Xuesheng, Gu Erwei, Zhang Zhi, Tao Wenjuan
Department of Anesthesiology, First Affiliated Hospital of Anhui Medical University, Jixi Road 218, Hefei, Anhui Province, China.
School of Life Sciences, University of Science and Technology of China, Huangshan Road 443, Hefei, Anhui Province, China.
Pain Res Manag. 2019 Jan 27;2019:1648919. doi: 10.1155/2019/1648919. eCollection 2019.
Histone deacetylase inhibitors (HDACIs), which interfere with the epigenetic process of histone acetylation, have shown analgesic effects in animal models of persistent pain. The HDAC family comprises 18 genes; however, the different effects of distinct classes of HDACIs on pain relief remain unclear. The aim of this study was to determine the efficacy of these HDACIs on attenuating thermal hyperalgesia in persistent inflammatory pain. Persistent inflammatory pain was induced by injecting Complete Freund's Adjuvant (CFA) into the left hind paw of rats. Then, HDACIs targeting class I (entinostat (MS-275)) and class IIa (sodium butyrate, valproic acid (VPA), and 4-phenylbutyric acid (4-PBA)), or class II (suberoylanilide hydoxamic acid (SAHA), trichostatin A (TSA), and dacinostat (LAQ824)) were administered intraperitoneally once daily for 3 or 4 days. We found that the injection of SAHA once a day for 3 days significantly attenuated CFA-induced thermal hyperalgesia from day 4 and lasted 7 days. In comparison with SAHA, suppression of hyperalgesia by 4-PBA peaked on day 2, whereas that by MS-275 occurred on days 5 and 6. Fatigue was a serious side effect seen with MS-275. These findings will be beneficial for optimizing the selection of specific HDACIs in medical fields such as pain medicine and neuropsychiatry.
组蛋白去乙酰化酶抑制剂(HDACIs)可干扰组蛋白乙酰化的表观遗传过程,已在持续性疼痛的动物模型中显示出镇痛作用。HDAC家族由18个基因组成;然而,不同类别的HDACIs对疼痛缓解的不同作用仍不清楚。本研究的目的是确定这些HDACIs在减轻持续性炎性疼痛中热痛觉过敏方面的疗效。通过向大鼠左后爪注射完全弗氏佐剂(CFA)诱导持续性炎性疼痛。然后,每天腹腔注射一次靶向I类(恩替诺特(MS-275))、IIa类(丁酸钠、丙戊酸(VPA)和4-苯基丁酸(4-PBA))或II类(辛二酰苯胺异羟肟酸(SAHA)、曲古抑菌素A(TSA)和达西他司(LAQ824))的HDACIs,持续3或4天。我们发现,每天注射一次SAHA,持续3天,从第4天开始可显著减轻CFA诱导的热痛觉过敏,并持续7天。与SAHA相比,4-PBA对痛觉过敏的抑制在第2天达到峰值,而MS-275对痛觉过敏的抑制在第5天和第6天出现。疲劳是MS-275出现的严重副作用。这些发现将有助于在疼痛医学和神经精神病学等医学领域优化特定HDACIs的选择。