Vianey de la Rosa-Lugo1, Macdiel Acevedo-Quiroz1, Myrna Déciga-Campos2, María Yolanda Rios1. 1. Centro de Investigaciones Químicas, IICBA, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, México. 2. Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, Ciudad de México, México.
Abstract
OBJECTIVE: 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). METHODS: 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. KEY FINDINGS: 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. CONCLUSIONS: 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.
OBJECTIVE: 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). METHODS: 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 alkamidecapsaicin was used as positive control, while capsazepine was used to evaluate the possible participation of TRPV1 receptor in alkamide-induced antinociception. KEY FINDINGS: 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. CONCLUSIONS: 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.