Analgesic Effects of Huwentoxin-IV on Animal Models of Inflammatory and Neuropathic Pain

作者:Liu, Yu; Wu, Zhe; Tang, Dongfang; Xun, Xiaohong; Liu, Lichao; Li, Xianlei; Nie, Dongsong; Xiang, Yang; Yi, Jianming; Yi, Jizu*
来源:Protein and Peptide Letters, 2014, 21(2): 153-158.

摘要

Huwentoxin-IV (HWTX-IV), a peptide with 35 amino acid residues, was discovered in the venom of spider Ornithoctonus huwena. The peptide had an inhibitory effect on a tetrodotoxin-sensitive (TTX-S) sodium channel with highly sensitive to Nav1.7, an attractive target for pain release therapy. In this study we further demonstrated the analgesic effects of HWTX-IV using mouse and rat as an inflammatory pain model and/or a neuropathic pain models. In the both cases, the analgesic effects of the peptide were dose-dependent, and statistically significant. In the inflammatory model, 100 mu g/kg of HWTX-IV produced an efficient reversal of hyperalgesia up to 63.6% after injection of formalin in rats with the efficiency equivalent to that of morphine at 50 mu g/kg, and 200 mu g/kg of HWTX-IV produced protective effect up to 55.6% after injection of acetic acid with the efficiency equivalent to that of morphine at 100 mu g/kg. In the spinal nerve model, the peptide produced the longer and higher reversal effect on allodynia than Mexiletine. These results demonstrated that HWTX-IV released efficiently the acute inflammatory pain and chronic neuropathic pain in these animals, suggesting that HWTX-IV was a potential and efficient candidate for further clinical drug development against inflammatory and neuropathic pain.