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Tingenone, a pentacyclic triterpene, induces peripheral antinociception due to cannabinoid receptors activation in mice.
Inflammopharmacology. 2018 Feb; 26(1):227-233.I

Abstract

Several works have shown that triterpenes induce peripheral antinociception by activation of cannabinoid receptors and endocannabinoids; besides, several research groups have reported activation of cannabinoid receptors in peripheral antinociception. The aim of this study was to assess the involvement of the cannabinoid system in the antinociceptive effect induced by tingenone against hyperalgesia evoked by prostaglandin E2 (PGE2) at peripheral level. The paw pressure test was used and the hyperalgesia was induced by intraplantar injection of PGE2 (2 μg/paw). All drugs were injected subcutaneously in the hind paws of male Swiss mice. Tingenone (200 µg/paw) administered into the right hind paw induced a local antinociceptive effect, that was antagonized by AM630, a selective antagonist to CB2 cannabinoid receptor. AM251, a selective antagonist to CB1 cannabinoid receptor, did not alter the peripheral antinociceptive effect of tingenone. MAFP, a fatty acid amide hydrolase (FAAH) inhibitor; VDM11, an anandamide reuptake inhibitor; and JZL184, monoacylglycerol lipase (MAGL) inhibitor did not potentiate the peripheral antinociceptive effect of the lower dose of tingenone (50 µg/paw). The results suggest that tingenone induced a peripheral antinociceptive effect via cannabinoid receptor activation. Therefore, this study suggests a pharmacological potential for a new analgesic drug.

Authors+Show Affiliations

Faculdade de Ciências Farmacêuticas, Universidade Federal do Amazonas (UFAM), Av. General Rodrigo Octávio Jordão Ramos, 3000, Coroado I, Manaus, AM, 69.077-000, Brazil. clariceveloso@ufam.edu.br.Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais (UFMG), Belo Horizonte, MG, Brazil.Department of Chemistry, Institute of Exact Sciences, UFMG, Belo Horizonte, MG, Brazil.Department of Chemistry, Institute of Exact Sciences, UFMG, Belo Horizonte, MG, Brazil.Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais (UFMG), Belo Horizonte, MG, Brazil.Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais (UFMG), Belo Horizonte, MG, Brazil.Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais (UFMG), Belo Horizonte, MG, Brazil.Department of Pharmacology, Institute of Biological Sciences, Federal University of Minas Gerais (UFMG), Belo Horizonte, MG, Brazil.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28889355

Citation

Veloso, C C., et al. "Tingenone, a Pentacyclic Triterpene, Induces Peripheral Antinociception Due to Cannabinoid Receptors Activation in Mice." Inflammopharmacology, vol. 26, no. 1, 2018, pp. 227-233.
Veloso CC, Ferreira RCM, Rodrigues VG, et al. Tingenone, a pentacyclic triterpene, induces peripheral antinociception due to cannabinoid receptors activation in mice. Inflammopharmacology. 2018;26(1):227-233.
Veloso, C. C., Ferreira, R. C. M., Rodrigues, V. G., Duarte, L. P., Klein, A., Duarte, I. D., Romero, T. R. L., & Perez, A. C. (2018). Tingenone, a pentacyclic triterpene, induces peripheral antinociception due to cannabinoid receptors activation in mice. Inflammopharmacology, 26(1), 227-233. https://doi.org/10.1007/s10787-017-0391-7
Veloso CC, et al. Tingenone, a Pentacyclic Triterpene, Induces Peripheral Antinociception Due to Cannabinoid Receptors Activation in Mice. Inflammopharmacology. 2018;26(1):227-233. PubMed PMID: 28889355.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Tingenone, a pentacyclic triterpene, induces peripheral antinociception due to cannabinoid receptors activation in mice. AU - Veloso,C C, AU - Ferreira,R C M, AU - Rodrigues,V G, AU - Duarte,L P, AU - Klein,A, AU - Duarte,I D, AU - Romero,T R L, AU - Perez,A C, Y1 - 2017/09/09/ PY - 2017/06/07/received PY - 2017/08/23/accepted PY - 2017/9/11/pubmed PY - 2018/8/9/medline PY - 2017/9/11/entrez KW - Cannabinoid receptors KW - Pentacyclic triterpene KW - Peripheral antinociception KW - Tingenone SP - 227 EP - 233 JF - Inflammopharmacology JO - Inflammopharmacology VL - 26 IS - 1 N2 - Several works have shown that triterpenes induce peripheral antinociception by activation of cannabinoid receptors and endocannabinoids; besides, several research groups have reported activation of cannabinoid receptors in peripheral antinociception. The aim of this study was to assess the involvement of the cannabinoid system in the antinociceptive effect induced by tingenone against hyperalgesia evoked by prostaglandin E2 (PGE2) at peripheral level. The paw pressure test was used and the hyperalgesia was induced by intraplantar injection of PGE2 (2 μg/paw). All drugs were injected subcutaneously in the hind paws of male Swiss mice. Tingenone (200 µg/paw) administered into the right hind paw induced a local antinociceptive effect, that was antagonized by AM630, a selective antagonist to CB2 cannabinoid receptor. AM251, a selective antagonist to CB1 cannabinoid receptor, did not alter the peripheral antinociceptive effect of tingenone. MAFP, a fatty acid amide hydrolase (FAAH) inhibitor; VDM11, an anandamide reuptake inhibitor; and JZL184, monoacylglycerol lipase (MAGL) inhibitor did not potentiate the peripheral antinociceptive effect of the lower dose of tingenone (50 µg/paw). The results suggest that tingenone induced a peripheral antinociceptive effect via cannabinoid receptor activation. Therefore, this study suggests a pharmacological potential for a new analgesic drug. SN - 1568-5608 UR - https://www.unboundmedicine.com/medline/citation/28889355/Tingenone_a_pentacyclic_triterpene_induces_peripheral_antinociception_due_to_cannabinoid_receptors_activation_in_mice_ DB - PRIME DP - Unbound Medicine ER -