Funes, Matias and Tosso, Rodrigo D. and Machado, Noelia D. and Fernandez, Mariana A. and Garro, Maria and Diaz, David Diaz and Hikawczuk, Virginia Juan and Enriz, Ricardo D. (2023) 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, 169: 105622. ISSN 0367-326X, 1873-6971
Full text not available from this repository. (Request a copy)Abstract
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 respective complexes; such information might be useful for designing and searching for new inhibitors of KORs.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | KAPPA-OPIOID RECEPTOR; CLERODANE DITERPENOIDS; ANTIFEEDANT ACTIVITY; INFLAMMATION; SALVINORIN; SOFTWARE; Baccharis; Neoclerodane; Antinociceptive; KOR; Niosomes |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Chemistry and Pharmacy > Institut für Organische Chemie Chemistry and Pharmacy > Institut für Organische Chemie > Arbeitskreis Prof. Dr. David Díaz Díaz |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 30 Jan 2024 12:42 |
| Last Modified: | 30 Jan 2024 12:42 |
| URI: | https://pred.uni-regensburg.de/id/eprint/60790 |
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