蟾毒灵抗炎镇痛作用及其对NF-κB信号通路的影响

Anti-inflammatory and Analgesic Activities of Bufalin and Its Effect on NF-κB Signaling

【目的】研究蟾毒灵动物体内抗炎、镇痛作用及相关机制。【方法】采用角叉菜胶致大鼠足肿胀模型,通过测量蟾毒灵对足肿胀率的影响,Western blot法检测炎症组织中iNOS、COX-2、TNF-α及胞核内NF-κB p65的表达评估其抗炎作用,采用小鼠醋酸扭体实验和甲醛溶液实验评估蟾毒灵镇痛作用。【结果】蟾毒灵可产生剂量依赖性的抗炎镇痛作用。0.3 mg/kg、0.6 mg/kg蟾毒灵可显著抑制角叉菜胶致炎的大鼠足跖肿胀和炎症组织中iNOS、COX-2、TNF-α及胞核内NF-κB p65的蛋白水平,显著减少小鼠醋酸扭体反应次数和甲醛致痛引起的舔足时间。【结论】蟾毒灵可产生剂量依赖性抗炎镇痛作用,其机制可能与下调NF-κB入核并抑制其下游炎症介质有关。

[Objective] To study the anti-inflammatory and analgesic activities of bufalin in vivo.[Methods] Carrageenan-induced paw edema assessed the anti-inflammatory activity of this compound.Western blot detected the NF-κB signaling during this effect.The anti-nociceptive activities were evaluated with acetic acid-induced writhing test and formalin test.[Results] Our data showed that bufalin （0.3,0.6 mg/kg,i.p.） potently decreased carrageenan-induced paw edema.Bufalin down-regulated the expression level of nitric oxide synthase （iNOS）,cyclooxygenase-2 （COX-2）,and tumor necrosis factor-α （TNF-α） during this effect.Further studies demonstrated that bufalin significantly inhibited the nuclear translocation of NF-κB p65.Bufalin also reduced acetic acidinduced writhing and the licking time in formalin test.[Conclusion] Bufalin presented in vivo anti-inflammatory and analgesic effects,probably through the inhibition of NF-κB activation.