Rigo Flavia Karine, Trevisan Gabriela, De Prá Samira Dal-Toé, Cordeiro Marta Nascimento, Borges Marcia Helena, Silva Juliana Figueiredo, Santa Cecilia Flavia Viana, de Souza Alessandra Hubner, de Oliveira Adamante Gabriela, Milioli Alessandra Marcon, de Castro Junior Célio José, Ferreira Juliano, Gomez Marcus Vinicius
Programa de Pós-Graduação em Ciências da Saúde, Universidade do Extremo Sul Catarinense (UNESC), Criciúma, SC, Brazil.
Fundação Ezequiel Dias, Belo Horizonte, MG, Brazil.
Toxicon. 2017 Jul;133:145-152. doi: 10.1016/j.toxicon.2017.05.018. Epub 2017 May 17.
The native Phα1β - a Voltage-Gated Calcium Channel (VGCC) blocker - and its Recombinant Version - were both tested in rodent pain models with an intraplantar injections of capsaicin or formalin, a chronic constriction injury, and melanoma cancer related pain. The formalin nociceptive behaviour in the neurogenic phase was not affected by the toxin pre-treatments, while in the inflammatory phase, Phα1β and the Recombinant form caused a significant reduction. The nociception that was triggered by capsaicin, an agonist of the TRPV1 vanilloid receptor, was totally blocked by 100 pmol/site, i.t. of Phα1β or the recombinant version. For the neuropathic pain that was induced by a chronic constriction injury of the sciatic nerve, Phα1β and its Recombinant reduced the allodynia that was induced by the CCI procedure in the rats and the hypersensitivity lasted for 4 h. Fourteen days after the inoculation of the B16-F10 melanoma cells in the mice, a marked hyperalgesia was induced in the melanoma cancer pain model. Phα1β and the Recombinant form reduced the hyperalgesia with a full reversion at 100 pmol/site i.t. The inhibitory effects of the nociception that was induced by native Phα1β and the Recombinant in the studied pain models were not statistically different and they developed with no side effects.
天然的Phα1β（一种电压门控钙通道（VGCC）阻滞剂）及其重组形式，均在啮齿动物疼痛模型中进行了测试，这些模型包括足底注射辣椒素或福尔马林、慢性压迫损伤以及黑色素瘤相关疼痛。在神经源性阶段，福尔马林伤害性感受行为不受毒素预处理的影响，而在炎症阶段，Phα1β及其重组形式则导致了显著降低。由TRPV1香草酸受体激动剂辣椒素引发的伤害感受，在100 pmol/部位经皮内注射Phα1β或其重组形式后被完全阻断。对于坐骨神经慢性压迫损伤诱导的神经性疼痛，Phα1β及其重组形式减轻了大鼠CCI手术诱导的痛觉过敏，且超敏反应持续4小时。在小鼠接种B16-F10黑色素瘤细胞14天后，黑色素瘤癌症疼痛模型中诱导出明显的痛觉过敏。Phα1β及其重组形式减轻了痛觉过敏，在100 pmol/部位经皮内注射时完全恢复。在研究的疼痛模型中，天然Phα1β及其重组形式诱导的伤害感受抑制作用在统计学上无差异，且无副作用。
