Planta Med 2016; 82(01/02): 106-112
DOI: 10.1055/s-0035-1558084
Biological and Pharmacological Activitiy
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Natural Diterpenes from Coffee, Cafestol, and Kahweol Induce Peripheral Antinoceception by Adrenergic System Interaction

Luciana Souza Guzzo
Department of Pharmacology, Institute of Biological Sciences, UFMG, Belo Horizonte, Brazil
,
Marina Gomes Miranda e Castor
Department of Pharmacology, Institute of Biological Sciences, UFMG, Belo Horizonte, Brazil
,
Andrea de Castro Perez
Department of Pharmacology, Institute of Biological Sciences, UFMG, Belo Horizonte, Brazil
,
Igor Dimitri Gama Duarte
Department of Pharmacology, Institute of Biological Sciences, UFMG, Belo Horizonte, Brazil
,
Thiago Roberto Lima Romero
Department of Pharmacology, Institute of Biological Sciences, UFMG, Belo Horizonte, Brazil
› Author Affiliations
Further Information

Publication History

received 28 April 2015
revised 01 July 2015

accepted 14 August 2015

Publication Date:
13 October 2015 (eFirst)

Abstract

Cafestol and kahweol are diterpenes found only in the non-saponified lipid fraction of coffee. They are released during boiling and retained in the filtration process. Previous studies have shown peripheral antinociception induced by endogenous opioid peptides released by these diterpenes. Considering that the activation of the opioid system leads to a noradrenaline release, the aim of this study was to verify the participation of the noradrenergic system in the peripheral antinociception induced by cafestol and kahweol. Hyperalgesia was induced by an intraplantar injection of prostaglandin E2 (2 µg). Cafestol or kahweol (80 µg/paw) were administered locally into the right hindpaw alone, and after the agents α 2-adrenoceptor antagonist yohimbine (5, 10 and 20 µg/paw), α 2 A-adrenoceptor antagonist BRL 44 408 (40 µg/paw), α 2B-adrenoceptor antagonist imiloxan (40 µg/paw), α 2 C-adrenoceptor antagonist rauwolscine (10, 15 and 20 µg/paw), α 2D-adrenoceptor antagonist RX 821 002 (40 µg/paw), α 1-adrenoceptor antagonist prazosin (0.5, 1 and 2 µg/paw), or β-adrenoceptor antagonist propranolol (150, 300 and 600 ng/paw), respectively. Noradrenaline reuptake inhibitor reboxetine (30 µg/paw) was administered prior to cafestol or kahweol low dose (40 µg/paw) and guanetidine 3 days prior to the experiment (30 mg/kg, once a day), depleting the noradrenaline storage. Intraplantar injection of cafestol or kahweol (80 µg/paw) induced a peripheral antinociception against hyperalgesia induced by PGE2. This effect was reversed by intraplantar injections of yohimbine, rauwolscine, prazosin and propranolol. Reboxetine injection intensified the antinociceptive effect of cafestol or kahweol low-dose, and guanethidine reversed almost 70 % of the cafestol or kahweol-induced peripheral antinociception. This study gives evidence that the noradrenergic system participates in cafestol and kahweol-induced peripheral antinociception with the release of endogenous noradrenaline.