Mechanisms of the antinociceptive action of (−) Epicatechin obtained from the hydroalcoholic fraction of <it>Combretum leprosum</it> Mart & Eic in rodents

<p>Abstract</p> <p>Background</p> <p>The mechanisms of the antinociceptive activity of (−) epicatechin (EPI), a compound isolated from the hydroalcoholic fraction of <it>Combreum leprosum</it> Mart & Eicher.</p> <p>Methods</p> <p>...

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Main Authors: Lopes Luciano da, Marques Rosemarie, Fernandes Heliana, Pereira Sergio da, Ayres Mariane CC, Chaves Mariana, Almeida Fernanda RC
Format: Article
Language:English
Published: BMC 2012-07-01
Series:Journal of Biomedical Science
Subjects:
Online Access:http://www.jbiomedsci.com/content/19/1/68
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author Lopes Luciano da
Marques Rosemarie
Fernandes Heliana
Pereira Sergio da
Ayres Mariane CC
Chaves Mariana
Almeida Fernanda RC
author_facet Lopes Luciano da
Marques Rosemarie
Fernandes Heliana
Pereira Sergio da
Ayres Mariane CC
Chaves Mariana
Almeida Fernanda RC
author_sort Lopes Luciano da
collection DOAJ
description <p>Abstract</p> <p>Background</p> <p>The mechanisms of the antinociceptive activity of (−) epicatechin (EPI), a compound isolated from the hydroalcoholic fraction of <it>Combreum leprosum</it> Mart & Eicher.</p> <p>Methods</p> <p>were assessed in the model of chemical nociception induced by glutamate (20 μmol/paw). To evaluate the mechanisms involved, the animals , male Swiss mice (25-30 g), received EPI (50 mg/kg p.o.) after pretreatment with naloxone (2 mg/kg s.c. opioid antagonist), glibenclamide (2 mg/kg s.c. antagonist K + channels sensitive to ATP), ketanserin (0.3 mg/kg s.c. antagonist of receptor 5-HT<sub>2A</sub>), yoimbine (0.15 mg/kg s.c. α2 adrenergic receptor antagonist), pindolol (1 mg/kg s.c. 5-HT1<sub>a</sub>/1<sub>b</sub> receptor antagonist), atropine (0.1 mg/kg s.c. muscarinic antagonist) and caffeine (3 mg/kg s.c. adenosine receptor antagonist), ondansetron (0.5 mg/kg s.c. for 5-HT<sub>3</sub> receptor) and L-arginine (600 mg/kg i.p.).</p> <p>Results</p> <p>The antinociceptive effect of EPI was reversed by pretreatment with naloxone and glibenclamide, ketanserin, yoimbine, atropine and pindolol, which demonstrates the involvement of opioid receptors and potassium channels sensitive to ATP, the serotoninergic (receptor 5HT<sub>1A</sub> and 5HT<sub>2A</sub>), adrenergic (receptor alpha 2) and cholinergic (muscarinic receptor) systems in the activities that were observed. The effects of EPI, however, were not reversed by pretreatment with caffeine, L-arginine or ondansetron, which shows that there is no involvement of 5HT<sub>3</sub> receptors or the purinergic and nitrergic systems in the antinociceptive effect of EPI. In the Open Field and Rotarod test, EPI had no significant effect, which shows that there was no central nervous system depressant or muscle relaxant effect on the results.</p> <p>Conclusions</p> <p>This study demonstrates that the antinociceptive activity of EPI in the glutamate model involves the participation of the opioid system, serotonin, adrenergic and cholinergic.</p>
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spelling doaj.art-3caa1b881798472cbb690dc7889f097a2022-12-21T20:46:30ZengBMCJournal of Biomedical Science1021-77701423-01272012-07-011916810.1186/1423-0127-19-68Mechanisms of the antinociceptive action of (−) Epicatechin obtained from the hydroalcoholic fraction of <it>Combretum leprosum</it> Mart & Eic in rodentsLopes Luciano daMarques RosemarieFernandes HelianaPereira Sergio daAyres Mariane CCChaves MarianaAlmeida Fernanda RC<p>Abstract</p> <p>Background</p> <p>The mechanisms of the antinociceptive activity of (−) epicatechin (EPI), a compound isolated from the hydroalcoholic fraction of <it>Combreum leprosum</it> Mart & Eicher.</p> <p>Methods</p> <p>were assessed in the model of chemical nociception induced by glutamate (20 μmol/paw). To evaluate the mechanisms involved, the animals , male Swiss mice (25-30 g), received EPI (50 mg/kg p.o.) after pretreatment with naloxone (2 mg/kg s.c. opioid antagonist), glibenclamide (2 mg/kg s.c. antagonist K + channels sensitive to ATP), ketanserin (0.3 mg/kg s.c. antagonist of receptor 5-HT<sub>2A</sub>), yoimbine (0.15 mg/kg s.c. α2 adrenergic receptor antagonist), pindolol (1 mg/kg s.c. 5-HT1<sub>a</sub>/1<sub>b</sub> receptor antagonist), atropine (0.1 mg/kg s.c. muscarinic antagonist) and caffeine (3 mg/kg s.c. adenosine receptor antagonist), ondansetron (0.5 mg/kg s.c. for 5-HT<sub>3</sub> receptor) and L-arginine (600 mg/kg i.p.).</p> <p>Results</p> <p>The antinociceptive effect of EPI was reversed by pretreatment with naloxone and glibenclamide, ketanserin, yoimbine, atropine and pindolol, which demonstrates the involvement of opioid receptors and potassium channels sensitive to ATP, the serotoninergic (receptor 5HT<sub>1A</sub> and 5HT<sub>2A</sub>), adrenergic (receptor alpha 2) and cholinergic (muscarinic receptor) systems in the activities that were observed. The effects of EPI, however, were not reversed by pretreatment with caffeine, L-arginine or ondansetron, which shows that there is no involvement of 5HT<sub>3</sub> receptors or the purinergic and nitrergic systems in the antinociceptive effect of EPI. In the Open Field and Rotarod test, EPI had no significant effect, which shows that there was no central nervous system depressant or muscle relaxant effect on the results.</p> <p>Conclusions</p> <p>This study demonstrates that the antinociceptive activity of EPI in the glutamate model involves the participation of the opioid system, serotonin, adrenergic and cholinergic.</p>http://www.jbiomedsci.com/content/19/1/68(−) epicatechinAntinociceptionCombretum leprosumGlutamateSerotonin and opioids
spellingShingle Lopes Luciano da
Marques Rosemarie
Fernandes Heliana
Pereira Sergio da
Ayres Mariane CC
Chaves Mariana
Almeida Fernanda RC
Mechanisms of the antinociceptive action of (−) Epicatechin obtained from the hydroalcoholic fraction of <it>Combretum leprosum</it> Mart & Eic in rodents
Journal of Biomedical Science
(−) epicatechin
Antinociception
Combretum leprosum
Glutamate
Serotonin and opioids
title Mechanisms of the antinociceptive action of (−) Epicatechin obtained from the hydroalcoholic fraction of <it>Combretum leprosum</it> Mart & Eic in rodents
title_full Mechanisms of the antinociceptive action of (−) Epicatechin obtained from the hydroalcoholic fraction of <it>Combretum leprosum</it> Mart & Eic in rodents
title_fullStr Mechanisms of the antinociceptive action of (−) Epicatechin obtained from the hydroalcoholic fraction of <it>Combretum leprosum</it> Mart & Eic in rodents
title_full_unstemmed Mechanisms of the antinociceptive action of (−) Epicatechin obtained from the hydroalcoholic fraction of <it>Combretum leprosum</it> Mart & Eic in rodents
title_short Mechanisms of the antinociceptive action of (−) Epicatechin obtained from the hydroalcoholic fraction of <it>Combretum leprosum</it> Mart & Eic in rodents
title_sort mechanisms of the antinociceptive action of epicatechin obtained from the hydroalcoholic fraction of it combretum leprosum it mart eic in rodents
topic (−) epicatechin
Antinociception
Combretum leprosum
Glutamate
Serotonin and opioids
url http://www.jbiomedsci.com/content/19/1/68
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