Tingenone, a pentacyclic triterpene, induces peripheral antinociception due to opioidergic activation.

Abstract

Plants belonging to the genus Maytenus are routinely used in folk medicine for the treatment of pain diseases. Our previous phytochemical study of the roots of Maytenus imbricata resulted in the isolation and characterization of tingenone, a pentacyclic triterpene. Natural triterpenoids are of growing interest because they have several biological activities, including analgesic properties. The present study assessed the involvement of the opiodergic pathway in the tingenone-induced antinociceptive effect against hyperalgesia induced by prostaglandin E2 (2 µg) in the peripheral pathway. We evaluated the effect of several antagonists to opioid receptors using the mouse paw pressure test. Tingenone administered into the right hind paw induced a local antinociceptive effect that was antagonized by naloxone, a nonselective antagonist to opioid receptors. Clocinnamox, naltrindole, and nor-binaltorphimine are selective antagonists to µ, δ, and κ receptors, respectively, which reverted the peripheral antinociception induced by tingenone. Bestatine acts as an inhibitor of aminopeptidase, an enzyme that degrades endogenous opioid peptides, and was shown to intensify the antinociceptive effect of tingenone. The results suggest that the opioidergic system participates in the peripheral antinociception induced by tingenone.

• Authors: Clarice de Carvalho Veloso, Vanessa Gregório Rodrigues, Renata Cristina Mendes Ferreira, Lucienir Pains Duarte, Andre Klein, Igor Dimitri Duarte, Thiago Roberto Lima Romero, Andrea de Castro Perez
• Journal: Planta medica (Planta Med) Vol. 80 Issue 17 Pg. 1615-21 (Nov 2014) ISSN: 1439-0221 [Electronic] Germany
• PMID: 25338214 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Georg Thieme Verlag KG Stuttgart · New York.

Chemical References

• Analgesics
• Analgesics, Opioid
• Triterpenes
• tingenone

Topics

• Analgesics (adverse effects, isolation & purification, pharmacology)
• Analgesics, Opioid (adverse effects, isolation & purification, pharmacology)
• Animals
• Hyperalgesia (drug therapy)
• Male
• Maytenus (chemistry)
• Mice
• Triterpenes (adverse effects, isolation & purification, pharmacology)