Mechanisms of the antinociceptive action of (-) epicatechin obtained from the hydroalcoholic fraction of Combretum leprosum Mart & Eic in rodents.
Mechanisms of the antinociceptive action of (-) epicatechin obtained from the hydroalcoholic fraction of Combretum leprosum Mart & Eic in rodents.
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DOI：
10.1186/1423-0127-19-68
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发表时间：
2012-07-25
影响因子：
11
通讯作者：
Almeida FR
中科院分区：
文献类型：
--
作者：
Lopes Lda S;Marques RB;Fernandes HB;Pereira Sda S;Ayres MC;Chaves MH;Almeida FR
（−）表儿茶素（EPI）的抗伤活性机制，从麻风Combreum lesum Mart & Eicher的水醇部分分离的化合物。以谷氨酸（20 μmol/爪）诱导的化学伤害感觉模型进行评价。为了评估其机制，雄性瑞士小鼠（25-30 g）在纳洛酮（2 mg/kg s.c）预处理后接受EPI （50 mg/kg p.o）。阿片类拮抗剂)，格列本脲(2mg /kg s.c。对ATP敏感的K +通道拮抗剂)，酮色林(0.3 mg/kg s.c。受体5-HT2A拮抗剂)，尤因宾(0.15 mg/kg s.c。α2肾上腺素能受体拮抗剂)，品多洛尔(1mg /kg s.c。5-HT1a/1b受体拮抗剂)，阿托品(0.1 mg/kg s.c。毒蕈碱拮抗剂)和咖啡因(3mg /kg s.c。腺苷受体拮抗剂)，昂丹司琼(0.5 mg/kg s.c。（5-HT3受体）和l -精氨酸（600 mg/kg i.p）。经纳洛酮、格列苯脲、酮色林、yoimine、阿托品和品多洛尔预处理后，EPI的抗伤害性被逆转，这表明阿片受体和对ATP敏感的钾通道、5 -羟色胺能（受体5HT1A和5HT2A）、肾上腺素能（受体α 2）和胆碱能（毒碱受体）系统参与了所观察到的活性。然而，经咖啡因、l -精氨酸或昂丹司琼预处理后，EPI的作用并没有逆转，这表明EPI的抗伤害性作用不涉及5HT3受体或嘌呤能系统和氮能系统。在Open Field和Rotarod试验中，EPI没有显著的影响，说明EPI对结果没有中枢神经系统抑制剂和肌肉松弛剂的作用。本研究表明EPI在谷氨酸模型中的抗伤害性活性涉及阿片系统、血清素、肾上腺素能和胆碱能的参与。
The mechanisms of the antinociceptive activity of (−) epicatechin (EPI), a compound isolated from the hydroalcoholic fraction of Combreum leprosum Mart & Eicher. 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-HT2A), yoimbine (0.15 mg/kg s.c. α2 adrenergic receptor antagonist), pindolol (1 mg/kg s.c. 5-HT1a/1b 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-HT3 receptor) and L-arginine (600 mg/kg i.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 5HT1A and 5HT2A), 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 5HT3 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. This study demonstrates that the antinociceptive activity of EPI in the glutamate model involves the participation of the opioid system, serotonin, adrenergic and cholinergic.
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影响因子：
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作者：
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通讯作者：
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DOI：
10.1016/j.jpba.2009.04.007
发表时间：
2010-01-20
影响因子：
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作者：
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通讯作者：
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