The coffee specific diterpene cafestol induces peripheral antinociception mediated by endogenous opioid peptides.
Clin Exp Pharmacol Physiol. 2012 Feb 14. Epub 2012 Feb 14. PMID: 22332877
Ls Guzzo, Ac Perez, Trl Romero, Ao Azevedo, Idg Duarte
Department of Pharmacology, Institute of Biological Sciences, Belo Horizonte, MG, Brazil.
The opioid peptides have been implicated in peripheral antinociception induced by non-opioidergic compounds, including nonsteroidal anti-inflammatories andα(2) -adrenergic drugs. The aims of the present study were to investigate the possible peripheral antinociceptive effect of cafestol, a diterpene present in the oil derived from coffee beans, and to evaluate the involvement of opioid peptides in this effect. The rat paw pressure test was used, andhyperalgesia was induced by intraplantar injection of prostaglandin E(2) (2 μg/paw). All drugs were locally administered into the hind-paws of male Wistar rats. Intraplantar injection of cafestol (20, 40 and 80 μg) induced peripheral antinociception. The antinociceptive effect of cafestol was due to a local action because the higher dose (80 μg/paw) did not produce any effect in the contralateral paw. The opioid receptor antagonist naloxone (25, 50 and 100 μg/paw) prevented action of cafestol (80 μg/paw) and the aminopeptidases inhibitor bestatin (400 μg/paw) potentiated the antinociceptive effect of cafestol (40 μg/paw). The results discussed here provide evidence that cafestol treatment has peripheral antinociceptive effect and suggest that this effect is mediated by the release of endogenous opioids. © 2012 The Authors Clinical and Experimental Pharmacology and Physiology© 2012 Blackwell Publishing Asia Pty Ltd.