Key Laboratory of Receptors-Mediated Gene Regulation and Drug Discovery, School of Medicine, Henan University, Kaifeng, China.
Laboratory of Cell Signal Transduction, School of Medicine, Henan University, Kaifeng, China.
Am J Pathol. 2019 Apr;189(4):886-899. doi: 10.1016/j.ajpath.2018.12.009. Epub 2019 Jan 19.
Spexin/NPQ is a novel highly conserved neuropeptide. It has a widespread expression in the periphery and central nervous system. However, the effects of central spexin on acute inflammatory pain are still unknown. This study explored the mechanisms and effects of supraspinal spexin on inflammatory pain. The results from the mouse formalin test show that i.c.v. administration of spexin decreased licking/biting time during the late and early phases. The nonamidated spexin had no effect on pain response. The antinociception of spexin was blocked by galanin receptor 3 antagonist SNAP 37889. The Galr3 and Adcy4 mRNA levels in the brain were increased after injection with spexin. The antinociceptive effects of spexin were completely reversed by opioid receptor antagonist naloxone and κ-opioid receptor antagonist nor-binaltorphimine dihydrochloride. Spexin up-regulated the dynorphin and κ-opioid receptor gene and protein expression. PCR array assay and real-time PCR analysis show that spexin up-regulated the mRNA level of the FBJ osteosarcoma oncogene (Fos). T-5224, the inhibitor of c FBJ osteosarcoma oncogene (c-Fos)/activator protein 1 (AP-1), blocked the increased mRNA level of Pdyn and Oprk1 induced by spexin. I.C.V. spexin (2.43 mg/kg) increased the number of c-Fos-positive neurons in most subsections of periaqueductal gray. In addition, in the acetic acid-induced writhing test, i.c.v. spexin produced an antinociceptive effect. Our results indicate that spexin might be a novel neuropeptide with an antinociceptive effect against acute inflammatory pain.
Spexin/NPQ 是一种新型高度保守的神经肽。它在外周和中枢神经系统中广泛表达。然而,中枢 Spexin 对急性炎症性疼痛的影响尚不清楚。本研究探讨了中枢 Spexin 对炎症性疼痛的机制和作用。小鼠福尔马林试验结果表明,脑室注射 Spexin 可减少晚期和早期的舔/咬时间。非酰胺化 Spexin 对疼痛反应没有影响。Galanin 受体 3 拮抗剂 SNAP 37889 阻断 Spexin 的镇痛作用。注射 Spexin 后大脑中的 Galr3 和 Adcy4 mRNA 水平增加。Spexin 的镇痛作用被阿片受体拮抗剂纳洛酮和 κ-阿片受体拮抗剂 nor-binaltorphimine dihydrochloride 完全逆转。Spexin 上调了强啡肽和 κ-阿片受体基因和蛋白的表达。PCR 阵列分析和实时 PCR 分析表明,Spexin 上调了 FBJ 骨肉瘤癌基因 (Fos) 的 mRNA 水平。c-FBJ 骨肉瘤癌基因 (c-Fos)/激活蛋白 1 (AP-1) 的抑制剂 T-5224 阻断了 Spexin 诱导的 Pdyn 和 Oprk1 mRNA 水平的增加。脑室注射 Spexin(2.43mg/kg)增加了导水管周围灰质大多数亚区中 c-Fos 阳性神经元的数量。此外,在醋酸诱导的扭体试验中,脑室注射 Spexin 产生镇痛作用。我们的结果表明,Spexin 可能是一种新型的具有抗急性炎症性疼痛作用的神经肽。