Department of Anesthesiology, The Second Hospital of Lanzhou University, Lanzhou, Gansu 730030, P.R. China.
Mol Med Rep. 2021 Jul;24(1). doi: 10.3892/mmr.2021.12159. Epub 2021 May 20.
Carbenoxolone (CBX) is primarily used to relieve various types of neuropathic and inflammatory pain. However, little is known concerning the role of CBX in acute pain and its functional mechanisms therein and this was investigated in the present study. Rats underwent toe incision and behavioral tests were performed to assess mechanical hypersensitivity. The expression levels of pannexin 1 (Px1) and connexin 43 (Cx43) were detected using western blot analysis 2, 4, 6 or 24 h after toe incision, and the expression of TNF‑α, IL‑1β and P substance (SP) was determined by ELISA; Px1 and Cx43 expression was also examined by immunofluorescence staining. At 2, 6 and 12 h post‑toe incision, the postoperative pain threshold was significantly reduced, which was subsequently recovered at 2 and 6 h post‑surgery following pretreatment with CBX or pannexin 1 mimetic inhibitory peptide. CBX reduced Px1 levels at 4 and 24 h post‑incision. However, Cx43 levels were reduced by CBX as little as 2 h post‑surgery. Furthermore, CBX not only distinctly decreased the levels of Px1 and Cx43, but also reduced the co‑localization of Px1 or Cx43 with glial fibrillary acidic protein, 2 h after incision. It was also observed that the protein levels of inflammatory makers (IL‑1β, SP and TNF‑α) showed a tendency to decline at 2, 4, 6 and 24 h after incision. Collectively, the expression of Px1 and Cx43 in astrocytes may be involved in pain behaviors diminished by CBX, and CBX potentially reduces acute pain by decreasing Px1 and Cx43 levels. Px1 and Cx43 from spinal astrocytes may serve important roles in the early stages and maintenance of acute pain, while preoperative injection of CBX has the potential to relieve hyperalgesia.
卡波氯铵 (CBX) 主要用于缓解各种类型的神经性和炎症性疼痛。然而,关于 CBX 在急性疼痛中的作用及其在其中的功能机制知之甚少,本研究对此进行了探讨。大鼠进行趾切口,进行行为测试以评估机械性感觉过敏。使用 Western blot 分析在趾切口后 2、4、6 或 24 小时检测全通道蛋白 1(Px1)和连接蛋白 43(Cx43)的表达水平,并通过 ELISA 测定 TNF-α、IL-1β 和 P 物质(SP)的表达;通过免疫荧光染色检查 Px1 和 Cx43 的表达。在趾切口后 2、6 和 12 小时,术后疼痛阈值显著降低,随后在 CBX 预处理或全通道蛋白 1 模拟抑制肽预处理后,在术后 2 和 6 小时恢复。CBX 可降低术后 4 和 24 小时的 Px1 水平。然而,CBX 可在术后 2 小时降低 Cx43 水平。此外,CBX 不仅明显降低 Px1 和 Cx43 的水平,而且在切口后 2 小时还降低 Px1 或 Cx43 与神经胶质纤维酸性蛋白的共定位。还观察到,炎性标志物(IL-1β、SP 和 TNF-α)的蛋白水平在切口后 2、4、6 和 24 小时呈下降趋势。总之,星形胶质细胞中 Px1 和 Cx43 的表达可能参与了 CBX 减弱的疼痛行为,CBX 可能通过降低 Px1 和 Cx43 水平来减轻急性疼痛。脊髓星形胶质细胞中的 Px1 和 Cx43 可能在急性疼痛的早期阶段和维持中发挥重要作用,而术前注射 CBX 有可能缓解痛觉过敏。