Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation

Detalhes bibliográficos
Autor(a) principal: Guzzo,L.S.
Data de Publicação: 2021
Outros Autores: 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.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Brazilian Journal of Medical and Biological Research
Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2021001200607
Resumo: 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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spelling Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activationKahweolCoffeeAntinociceptionCannabinoid systemEndocannabinoidKahweol 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.Associação Brasileira de Divulgação Científica2021-01-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2021001200607Brazilian Journal of Medical and Biological Research v.54 n.12 2021reponame:Brazilian Journal of Medical and Biological Researchinstname:Associação Brasileira de Divulgação Científica (ABDC)instacron:ABDC10.1590/1414-431x2021e11071info:eu-repo/semantics/openAccessGuzzo,L.S.Oliveira,C.C.Ferreira,R.C.M.Machado,D.P.D.Castor,M.G.M.Perez,A.C.Piscitelli,F.Marzo,V. DiRomero,T.R.L.Duarte,I.D.G.eng2021-10-26T00:00:00Zoai:scielo:S0100-879X2021001200607Revistahttps://www.bjournal.org/https://old.scielo.br/oai/scielo-oai.phpbjournal@terra.com.br||bjournal@terra.com.br1414-431X0100-879Xopendoar:2021-10-26T00:00Brazilian Journal of Medical and Biological Research - Associação Brasileira de Divulgação Científica (ABDC)false
dc.title.none.fl_str_mv Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation
title Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation
spellingShingle Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation
Guzzo,L.S.
Kahweol
Coffee
Antinociception
Cannabinoid system
Endocannabinoid
title_short Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation
title_full Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation
title_fullStr Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation
title_full_unstemmed Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation
title_sort Kahweol, a natural diterpene from coffee, induces peripheral antinociception by endocannabinoid system activation
author Guzzo,L.S.
author_facet 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.
author_role author
author2 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.
author2_role author
author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv 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.
dc.subject.por.fl_str_mv Kahweol
Coffee
Antinociception
Cannabinoid system
Endocannabinoid
topic Kahweol
Coffee
Antinociception
Cannabinoid system
Endocannabinoid
description 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.
publishDate 2021
dc.date.none.fl_str_mv 2021-01-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2021001200607
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2021001200607
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/1414-431x2021e11071
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv text/html
dc.publisher.none.fl_str_mv Associação Brasileira de Divulgação Científica
publisher.none.fl_str_mv Associação Brasileira de Divulgação Científica
dc.source.none.fl_str_mv Brazilian Journal of Medical and Biological Research v.54 n.12 2021
reponame:Brazilian Journal of Medical and Biological Research
instname:Associação Brasileira de Divulgação Científica (ABDC)
instacron:ABDC
instname_str Associação Brasileira de Divulgação Científica (ABDC)
instacron_str ABDC
institution ABDC
reponame_str Brazilian Journal of Medical and Biological Research
collection Brazilian Journal of Medical and Biological Research
repository.name.fl_str_mv Brazilian Journal of Medical and Biological Research - Associação Brasileira de Divulgação Científica (ABDC)
repository.mail.fl_str_mv bjournal@terra.com.br||bjournal@terra.com.br
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