First Clinical Medical College of Shanxi Medical University, Taiyuan, China.
Department of Pharmacy, Precision Pharmacy and Drug Development Center, Tangdu Hospital, Fourth Military Medical University, Xi'an, China.
Mol Pain. 2021 Jan-Dec;17:1744806921990934. doi: 10.1177/1744806921990934.
Chronic pain is highly prevalent worldwide and severely affects daily lives of patients and family members. Praeruptorin C (Pra-C) is a main active ingredient derived from Dunn, traditionally used as antibechic, anti-bronchitis and anti-hypertension drug. Here, we evaluated the effects of Pra-C in a chronic inflammatory pain mouse model induced by complete Freund's adjuvant (CFA) injection. Pra-C (3 mg/kg) treatment for just 3 days after CFA challenge relieved CFA-induced mechanical allodynia and hindpaw edema in mice. In the anterior cingulate cortex (ACC), Pra-C treatment inhibited microglia activation and reduced levels of proinflammatory cytokines, TNF-α and IL-1β, and suppressed upregulation of glutamate receptors caused by CFA injection. In addition, Pra-C attenuated neuronal hyperexcitability in ACC of CFA-injected mice. In vitro studies confirmed the analgesic effect of Pra-C was due to its inhibitory ability on microglial activation. In conclusion, Pra-C administration had a certain effect on relieving chronic pain by inhibiting microglial activation, attenuating proinflammatory cytokine releasing and regulating excitatory synaptic proteins in the ACC of the CFA-injected mice.
慢性疼痛在全球范围内普遍存在，严重影响了患者和家属的日常生活。白花前胡丙素（Pra-C）是一种主要的活性成分，来源于白花前胡，传统上用作止喘药、支气管炎药和抗高血压药。在这里，我们评估了 Pra-C 在完全弗氏佐剂（CFA）注射诱导的慢性炎症性疼痛小鼠模型中的作用。CFA 注射后仅用 Pra-C（3mg/kg）治疗 3 天即可缓解 CFA 引起的机械性痛觉过敏和后爪水肿。在扣带前皮质（ACC）中，Pra-C 治疗抑制小胶质细胞激活并降低促炎细胞因子 TNF-α和 IL-1β的水平，并抑制 CFA 注射引起的谷氨酸受体的上调。此外，Pra-C 减轻了 CFA 注射小鼠 ACC 中的神经元过度兴奋。体外研究证实 Pra-C 的镇痛作用是由于其抑制小胶质细胞激活的能力。总之，Pra-C 通过抑制小胶质细胞激活、减轻促炎细胞因子释放以及调节 CFA 注射小鼠 ACC 中的兴奋性突触蛋白，对缓解慢性疼痛有一定的作用。
