de la Rosa-Lugo Vianey, Acevedo-Quiroz Macdiel, Déciga-Campos Myrna, Rios María Yolanda
Centro de Investigaciones Químicas, IICBA, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, México.
Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, Ciudad de México, México.
J Pharm Pharmacol. 2017 Jul;69(7):884-895. doi: 10.1111/jphp.12721. Epub 2017 Apr 4.
To establish the role of TRPV1 receptor in the antinociceptive effect of natural alkamides (i.e. affinin, longipinamide A, longipenamide A and longipenamide B) isolated from Heliopsis longipes (A. Gray) S.F. Blake and some related synthetic alkamides (i.e. N-isobutyl-feruloylamide and N-isobutyl-dihydroferuloylamide).
The orofacial formalin test was used to assess the antinociceptive activity of natural (1-30 μg, orofacial region) and synthetic alkamides (0.1-100 μg, orofacial region). The alkamide capsaicin was used as positive control, while capsazepine was used to evaluate the possible participation of TRPV1 receptor in alkamide-induced antinociception.
Natural (1-30 μg) and synthetic (0.1-100 μg) alkamides administered to the orofacial region produced antinociception in mice. The antinociceptive effect induced by affinin, N-isobutyl-feruloylamide and N-isobutyl-dihydroferuloylamide was antagonized by capsazepine but not by vehicle.
These results suggest that alkamide affinin, longipinamide A, longipenamide A and longipenamide B isolated from Heliopsis longipes as well as the synthesized analogue compounds N-isobutyl-feruloylamide and N-isobutyl-dihydroferuloylamide produce their effects by activating TRPV1 receptor and they may have potential for the development of new analgesic drugs for the treatment of orofacial pain.
确定瞬时受体电位香草酸亚型1（TRPV1）受体在从长柄向日葵（A. Gray）S.F. Blake中分离出的天然烷酰胺（即阿菲宁、长柄酰胺A、长柄戊酰胺A和长柄戊酰胺B）以及一些相关合成烷酰胺（即N - 异丁基 - 阿魏酸酰胺和N - 异丁基 - 二氢阿魏酸酰胺）的抗伤害感受作用中的作用。
采用口腔面部福尔马林试验评估天然（1 - 30微克，口腔面部区域）和合成烷酰胺（0.1 - 100微克，口腔面部区域）的抗伤害感受活性。将烷酰胺辣椒素用作阳性对照，而辣椒平用于评估TRPV1受体在烷酰胺诱导的抗伤害感受中可能的参与情况。
给予口腔面部区域的天然（1 - 30微克）和合成（0.1 - 100微克）烷酰胺在小鼠中产生了抗伤害感受作用。阿菲宁、N - 异丁基 - 阿魏酸酰胺和N - 异丁基 - 二氢阿魏酸酰胺诱导的抗伤害感受作用被辣椒平拮抗，但未被赋形剂拮抗。
这些结果表明，从长柄向日葵中分离出的烷酰胺阿菲宁、长柄酰胺A、长柄戊酰胺A和长柄戊酰胺B以及合成类似物化合物N - 异丁基 - 阿魏酸酰胺和N - 异丁基 - 二氢阿魏酸酰胺通过激活TRPV1受体发挥作用，它们可能具有开发用于治疗口腔面部疼痛的新型镇痛药的潜力。
