Groupe de Recherche en Pharmacologie Animal du Québec (GREPAQ), Département de biomédecine vétérinaire, Faculté de médecine vétérinaire, Université de Montréal, Saint-Hyacinthe, Québec, Canada.
Phytother Res. 2013 Aug;27(8):1251-4. doi: 10.1002/ptr.4837. Epub 2012 Sep 12.
[6]-Gingerol, a structural analog of capsaicin, is an agonist of the transient receptor potential vanilloid 1 channel, which is known to have therapeutic properties for the treatment of pain and inflammation. The main objective of this study was to determine the central effect of [6]-gingerol on neuropathic pain when injected intrathecally at the level of the lumbar spinal cord. [6]-Gingerol distribution was evaluated following a 40 mg/kg intraperitoneal injection, and the brain-to-plasma and spinal cord-to-plasma ratios (0.73 and 1.7, respectively) suggest that [6]-gingerol penetrates well the central nervous system of rats. Induction of pain was performed using the sciatic nerve ligation model on rats, and a 10-µg intrathecal injections of [6]-gingerol was performed to evaluate its central effect. The results suggest a significant decrease of secondary mechanical allodynia after 30 min, 2 h and 4 h (p < 0.05, p < 0.01 and p < 0.001) and thermal hyperalgesia after 30 min, 2 h and 4 h (p < 0.05, p < 0.01 and p < 0.01). These promising results illustrate that [6]-gingerol could alleviate neuropathic pain by acting centrally at the level of the spinal cord.
[6]-姜酚是辣椒素的结构类似物，是瞬时受体电位香草素 1 通道的激动剂，已知具有治疗疼痛和炎症的特性。本研究的主要目的是确定[6]-姜酚鞘内注射到腰椎水平时对神经病理性疼痛的中枢作用。[6]-姜酚在腹腔内注射 40mg/kg 后进行分布评估，脑-血浆和脊髓-血浆比（分别为 0.73 和 1.7）表明[6]-姜酚很好地穿透了大鼠的中枢神经系统。使用大鼠坐骨神经结扎模型诱导疼痛，并进行 10μg鞘内注射[6]-姜酚以评估其中枢作用。结果表明，在 30 分钟、2 小时和 4 小时后，二次机械性痛觉过敏显著降低（p<0.05、p<0.01 和 p<0.001），在 30 分钟、2 小时和 4 小时后，热痛觉过敏显著降低（p<0.05、p<0.01 和 p<0.01）。这些有希望的结果表明，[6]-姜酚可以通过在脊髓水平的中枢作用来缓解神经病理性疼痛。
