Longhi-Balbinot Daniela T, Rossaneis Ana C, Pinho-Ribeiro Felipe A, Bertozzi Mariana M, Cunha Fernando Q, Alves-Filho José C, Cunha Thiago M, Peron Jean P S, Miranda Katrina M, Casagrande Rubia, Verri Waldiceu A
Departamento de Ciências Patológicas, Centro de Ciências Biológicas, Universidade Estadual de Londrina, Rod. Celso Garcia Cid PR 445, Km 380, Cx. Postal 10.011, 86057-970, Londrina, Parana, Brazil.
Department of Pharmacology, Ribeirão Preto Medical School, University of São Paulo, Avenida Bandeirantes, 3900, Ribeirão Preto, 14049-900, São Paulo, Brazil.
Chem Biol Interact. 2016 Aug 25;256:1-8. doi: 10.1016/j.cbi.2016.06.009. Epub 2016 Jun 7.
Chronic pain is a major health problem worldwide. We have recently demonstrated the analgesic effect of the nitroxyl donor, Angeli's salt (AS) in models of inflammatory pain. In the present study, the acute and chronic analgesic effects of AS was investigated in chronic constriction injury of the sciatic nerve (CCI)-induced neuropathic pain in mice. Acute (7th day after CCI) AS treatment (1 and 3 mg/kg; s.c.) reduced CCI-induced mechanical, but not thermal hyperalgesia. The acute analgesic effect of AS was prevented by treatment with 1H-[1,2, 4]oxadiazolo[4,3,-a]quinoxalin-1-one (ODQ, a soluble guanylate cyclase inhibitor), KT5823 (an inhibitor of protein kinase G [PKG]) or glibenclamide (GLB, an ATP-sensitive potassium channel blocker). Chronic (7-14 days after CCI) treatment with AS (3 mg/kg, s.c.) promoted a sustained reduction of CCI-induced mechanical and thermal hyperalgesia. Acute AS treatment reduced CCI-induced spinal cord allograft inflammatory factor 1 (known as Iba-1), interleukin-1β (IL-1β), and ST2 receptor mRNA expression. Chronic AS treatment reduced CCI-induced spinal cord glial fibrillary acidic protein (GFAP), Iba-1, IL-1β, tumor necrosis factor-α (TNF-α), interleukin-33 (IL-33) and ST2 mRNA expression. Chronic treatment with AS (3 mg/kg, s.c.) did not alter aspartate aminotransferase, alanine aminotransferase, urea or creatinine plasma levels. Together, these results suggest that the acute analgesic effect of AS depends on activating the cGMP/PKG/ATP-sensitive potassium channel signaling pathway. Moreover, chronic AS diminishes CCI-induced mechanical and thermal hyperalgesia by reducing the activation of spinal cord microglia and astrocytes, decreasing TNF-α, IL-1β and IL-33 cytokines expression. This spinal cord immune modulation was more prominent in the chronic treatment with AS. Thus, nitroxyl limits CCI-induced neuropathic pain by reducing spinal cord glial cells activation.
慢性疼痛是全球范围内的一个主要健康问题。我们最近在炎症性疼痛模型中证实了硝酰基供体安吉利盐(AS)的镇痛作用。在本研究中,研究了AS对小鼠坐骨神经慢性压迫损伤(CCI)诱导的神经性疼痛的急性和慢性镇痛作用。急性(CCI后第7天)AS处理(1和3mg/kg;皮下注射)可减轻CCI诱导的机械性痛觉过敏,但不能减轻热痛觉过敏。用1H-[1,2,4]恶二唑并[4,3,-a]喹喔啉-1-酮(ODQ,一种可溶性鸟苷酸环化酶抑制剂)、KT5823(蛋白激酶G[PKG]抑制剂)或格列本脲(GLB,一种ATP敏感性钾通道阻滞剂)处理可阻断AS的急性镇痛作用。慢性(CCI后7 - 14天)AS处理(3mg/kg,皮下注射)可使CCI诱导的机械性和热痛觉过敏持续减轻。急性AS处理可降低CCI诱导的脊髓同种异体移植炎症因子1(即Iba-1)、白细胞介素-1β(IL-1β)和ST2受体mRNA表达。慢性AS处理可降低CCI诱导的脊髓胶质纤维酸性蛋白(GFAP)、Iba-1、IL-1β、肿瘤坏死因子-α(TNF-α)、白细胞介素-33(IL-33)和ST2 mRNA表达。慢性AS处理(3mg/kg,皮下注射)未改变天冬氨酸转氨酶、丙氨酸转氨酶、尿素或肌酐的血浆水平。总之,这些结果表明AS的急性镇痛作用依赖于激活cGMP/PKG/ATP敏感性钾通道信号通路。此外,慢性AS通过减少脊髓小胶质细胞和星形胶质细胞的激活、降低TNF-α、IL-1β和IL-33细胞因子表达,减轻CCI诱导的机械性和热痛觉过敏。这种脊髓免疫调节在慢性AS处理中更为显著。因此,硝酰基通过减少脊髓胶质细胞激活来限制CCI诱导的神经性疼痛。