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Discaria americana 根皮减轻疼痛:与阿片类系统和 TRP/ASIC 通道相互作用的药理学证据。

Root bark of Discaria americana attenuates pain: A pharmacological evidence of interaction with opioidergic system and TRP/ASIC channels.

机构信息

Laboratório de Neurobiologia da Dor e Inflamação, Departamento de Ciências Fisiológicas, Universidade Federal de Santa Catarina, Florianópolis, SC 88040-900, Brazil; Faculdade Tecnológica Nova Palhoça, FATENP, Palhoça, SC, Brazil.

Laboratório de Neurobiologia da Dor e Inflamação, Departamento de Ciências Fisiológicas, Universidade Federal de Santa Catarina, Florianópolis, SC 88040-900, Brazil.

出版信息

J Ethnopharmacol. 2018 Dec 5;227:258-267. doi: 10.1016/j.jep.2018.09.008. Epub 2018 Sep 7.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Discaria americana (Rhamnaceae) root bark infusion have been used in traditional medicine as antipyretic, tonic, ameliorative of stomach and skin diseases and diabetes. This study was designed to investigate whether the methanolic extract of the root bark of Discaria americana (MEDa) exhibits antinociceptive effects in mice. Furthermore, it was investigated the involvement of the opioidergic system in MEDa mechanism of action as well the interactions with TRP/ASIC channels in its effect.

MATERIALS AND METHODS

The antinociceptive effect of intra-gastric gavage (i.g.) of MEDa (0.3-300 mg/kg) was evaluated in mice subjected to acute chemical (acetic-acid, formalin, glutamate, capsaicin, cinnamaldehyde, and acidified saline) or thermal (hot plate) tests of pain. The involvement of opioid system was evaluated in the formalin test. A nonspecific effect of MEDa was observed by measuring locomotor activity and exploratory behavior in open field test.

RESULTS

MEDa significantly reduced the number of writhing induced by acetic acid and inhibited the nociception in the two phases of formalin. These effects were inhibited by pretreatment with naloxone. The nociception induced by hot plate and intraplantar injection of glutamate, capsaicin, cinnamaldehyde and acidified saline were significantly inhibited by MEDa. Only the dose of 300 mg/kg altered the locomotor activity.

CONCLUSIONS

Our results demonstrated, for the first time, that the methanolic extract of the root bark of Discaria americana presents antinociceptive effect in chemical and thermal stimuli and its analgesic properties can be due activation of the opioidergic system. These results support the use of Discaria americana in traditional medicine and demonstrate that this plant presents a therapeutic potential for the development of phytomedicines with antinociceptive profile.

摘要

民族药理学相关性

Discaria americana(山龙眼科)的根皮浸剂在传统医学中被用作退热剂、滋补剂、改善胃病和皮肤病以及糖尿病。本研究旨在探讨Discaria americana 根皮的甲醇提取物(MEDa)是否对小鼠具有镇痛作用。此外,还研究了 MEDa 作用机制中阿片样物质系统的参与以及其作用与 TRPV/ASIC 通道的相互作用。

材料和方法

通过灌胃(i.g.)给予 MEDa(0.3-300mg/kg),评估其对急性化学(乙酸、甲醛、谷氨酸、辣椒素、肉桂醛和酸化盐水)或热(热板)疼痛测试的小鼠的镇痛作用。通过甲醛测试评估阿片样物质系统的参与。通过在开放场测试中测量运动活动和探索行为来观察 MEDa 的非特异性作用。

结果

MEDa 显著减少了乙酸引起的扭体次数,并抑制了甲醛的两个阶段的疼痛。这些作用被纳洛酮预处理所抑制。MEDa 显著抑制了热板和足底内注射谷氨酸、辣椒素、肉桂醛和酸化盐水引起的疼痛。只有 300mg/kg 的剂量改变了运动活动。

结论

我们的结果首次表明,Discaria americana 的根皮甲醇提取物在化学和热刺激下具有镇痛作用,其镇痛特性可能是由于阿片样物质系统的激活。这些结果支持了 Discaria americana 在传统医学中的应用,并表明该植物具有开发具有镇痛作用的植物药的治疗潜力。

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