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Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation.
Guzzo, L S; Oliveira, C C; Ferreira, R C M; Machado, D P D; Castor, M G M; Perez, A C; Piscitelli, F; Marzo, V Di; Romero, T R L; Duarte, I D G.
Afiliação
  • Guzzo LS; Departamento de Farmacologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brasil.
  • Oliveira CC; Departamento de Farmacologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brasil.
  • Ferreira RCM; Departamento de Farmacologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brasil.
  • Machado DPD; Departamento de Farmacologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brasil.
  • Castor MGM; Departamento de Farmacologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brasil.
  • Perez AC; Departamento de Farmacologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brasil.
  • Piscitelli F; Endocannabinoid Research Group, Institute of Biomolecular Chemistry, National Research Council, Pozzuoli, Napoli, Italy.
  • Marzo VD; Endocannabinoid Research Group, Institute of Biomolecular Chemistry, National Research Council, Pozzuoli, Napoli, Italy.
  • Romero TRL; Departamento de Farmacologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brasil.
  • Duarte IDG; Departamento de Farmacologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brasil.
Braz J Med Biol Res ; 54(12): e11071, 2021.
Article em En | MEDLINE | ID: mdl-34730678
Kahweol is a compound derived from coffee with reported antinociceptive effects. Based on the few reports that exist in the literature regarding the mechanisms involved in kahweol-induced peripheral antinociceptive action, this study proposed to investigate the contribution of the endocannabinoid system to the peripheral antinociception induced in rats by kahweol. Hyperalgesia was induced by intraplantar injection of prostaglandin E2(PGE2) and was measured with the paw pressure test. Kahweol and the drugs to test the cannabinoid system were administered locally into the right hind paw. The endocannabinoids were purified by open-bed chromatography on silica and measured by LC-MS. Kahweol (80 µg/paw) induced peripheral antinociception against PGE2-induced hyperalgesia. This effect was reversed by the intraplantar injection of the CB1 cannabinoid receptor antagonist AM251 (20, 40, and 80 µg/paw), but not by the CB2 cannabinoid receptor antagonist AM630 (100 µg/paw). Treatment with the endocannabinoid reuptake inhibitor VDM11 (2.5 µg/paw) intensified the peripheral antinociceptive effect induced by low-dose kahweol (40 µg/paw). The monoacylglycerol lipase (MAGL) inhibitor, JZL184 (4 µg/paw), and the dual MAGL/fatty acid amide hydrolase (FAAH) inhibitor, MAFP (0.5 µg/paw), potentiated the peripheral antinociceptive effect of low-dose kahweol. Furthermore, kahweol increased the levels of the endocannabinoid anandamide, but not of the other endocannabinoid 2-arachidonoylglycerol nor of anandamide-related N-acylethanolamines, in the plantar surface of the rat paw. Our results suggested that kahweol induced peripheral antinociception via anandamide release and activation of CB1 cannabinoid receptors and this compound could be used to develop new drugs for pain relief.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Endocanabinoides / Diterpenos Limite: Animals Idioma: En Revista: Braz J Med Biol Res Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Brasil País de publicação: Brasil
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Endocanabinoides / Diterpenos Limite: Animals Idioma: En Revista: Braz J Med Biol Res Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Brasil País de publicação: Brasil