RT info:eu-repo/semantics/article
T1 Antinociceptive effect of cyclic and linear diterpenoids as new atypical agonists of κ-opioid receptors obtained from four species of the Baccharis genus, and vehiculated in nanometric niosomes
A1 Díaz Díaz, David
A1 Funes, Matías
A1 Tosso, Rodrigo D.
A1 Machado, Noelia D.
A1 Fernández, Mariana A.
A1 Garro, María
A1 Hikawczuk, Virginia Juan
A1 Enriz, Ricardo D.
K1 Baccharis
K1 Neoclerodane
K1 Antinociceptive
K1 KOR
K1 Niosomes
AB New natural analgesic compounds that act in KORs are important alternatives for potential therapeutical use in medicine. In this work, we report and compare here the antinociceptive activity displayed by cyclic and linear diterpenes, obtained from the genus Baccharis. The antinociceptive activities determined were relatively strong, in comparison whit morphine. The antinociceptive mechanism of action was made through naloxone administration (a non-selective antagonist of opioid receptors). The more active compounds were vehiculized successfully in niosomes at nanometric scale. The observed antinociceptive activity for Bartemidiolide oxide (BARTO), obtain from Baccharis artemisioides, was greater than Flabeloic acid dimer (DACD), the first compound isolated from Baccharis flabellata that was reported possessing antinociceptive effects. We also conducted docking calculations and molecular dynamics simulations, which suggested that the newly identified diterpenes might share the molecular action mechanism reported for Salvinorin A (SalA). Molecular simulations have allowed us to appreciate some subtle differences between molecular interactions of these ligands stabilizing their respectivecomplexes; such information might be useful for designing and searching for new inhibitors of KORs.
PB Elsevier
SN 0367-326X
YR 2023
FD 2023
LK http://riull.ull.es/xmlui/handle/915/42242
UL http://riull.ull.es/xmlui/handle/915/42242
LA en
NO Matías Funes, Rodrigo D. Tosso, Noelia D. Machado, Mariana A. Fernández, María Garro, David Díaz Díaz, Virginia Juan Hikawczuk, Ricardo D. Enriz, Antinociceptive effect of cyclic and linear diterpenoids as new atypical agonists of κ-opioid receptors obtained from four species of the Baccharis genus, and vehiculated in nanometric niosomes, Fitoterapia, Volume 169, 2023, 105622, ISSN 0367-326X, https://doi.org/10.1016/j.fitote.2023.105622
DS Repositorio institucional de la Universidad de La Laguna
RD 17-jul-2025