Tingenone, a Pentacyclic Triterpene, Induces Peripheral Antinociception Due to Opioidergic Activation

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

doi:10.1055/s-0034-1383147

Planta Medica, Inhaltsverzeichnis

Planta Med 2014; 80(17): 1615-1621
DOI: 10.1055/s-0034-1383147

Biological and Pharmacological Activity

Original Papers

Georg Thieme Verlag KG Stuttgart · New York

Tingenone, a Pentacyclic Triterpene, Induces Peripheral Antinociception Due to Opioidergic Activation

Clarice de Carvalho Veloso

¹Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais (UFMG), Belo Horizonte, Minas Gerais, Brazil

,

Vanessa Gregório Rodrigues

²Department of Chemistry, Institute of Exact Sciences, UFMG, Belo Horizonte, Minas Gerais, Brazil

,

Renata Cristina Mendes Ferreira

¹Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais (UFMG), Belo Horizonte, Minas Gerais, Brazil

,

Lucienir Pains Duarte

²Department of Chemistry, Institute of Exact Sciences, UFMG, Belo Horizonte, Minas Gerais, Brazil

,

Andre Klein

¹Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais (UFMG), Belo Horizonte, Minas Gerais, Brazil

,

Igor Dimitri Duarte

¹Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais (UFMG), Belo Horizonte, Minas Gerais, Brazil

,

Thiago Roberto Lima Romero

¹Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais (UFMG), Belo Horizonte, Minas Gerais, Brazil

,

Andrea de Castro Perez

¹Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais (UFMG), Belo Horizonte, Minas Gerais, Brazil

› Institutsangaben

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.

Key words

Maytenus imbricata - Celastraceae - tingenone - pentacyclic triterpene - opioid receptors - peripheral antinociception

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Referenzen

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