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长花加里胡椒生物碱提取物和主要生物碱2-苯基喹啉的抗伤害感受作用评估

Evaluation of antinociceptive effects of Galipea longiflora alkaloid extract and major alkaloid 2-phenylquinoline.

作者信息

Campos-Buzzi F, Fracasso M, Clasen B K, Ticona J C, Gimenez A, Cechinel-Filho V

机构信息

Programa de Mestrado em Ciências Farmacêuticas e Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí - UNIVALI, Itajaí, Santa Catarina, Brazil.

出版信息

Methods Find Exp Clin Pharmacol. 2010 Dec;32(10):707-11. doi: 10.1358/mf.2010.32.10.1516692.

DOI:10.1358/mf.2010.32.10.1516692
PMID:21225005
Abstract

The present study evaluated the antinociceptive properties of an alkaloid extract and 2-phenylquinoline obtained from the bark of Galipea longiflora Krause (Rutaceae) against different models of pain in mice. The results demonstrate that the alkaloid extract caused a pronounced antinociceptive effect with the main alkaloid detected, 2-phenylquinoline, exhibiting moderate activity. The alkaloid extract had a calculated ID50 value of 20.3 mg/kg i.p. and less than 50 mg/kg p.o. against the writhing test which proved to be more effective than the reference drugs when administered by both routes. The ID50 of 2-phenylquinoline was 52.8 mg/kg i.p. with an inhibition of 24.5% when administered orally at 100 mg/kg. In the formalin test the alkaloid extract, but not 2-phenylquinoline, significantly inhibited both phases of pain (neurogenic and inflammatory) at 10 mg/kg i.p. with inhibitions of 37.4% and 58.3%, respectively. The alkaloid extract and 2-phenylquinoline caused only a modest effect in the capsaicin and glutamate tests. In the hot plate test, the alkaloid extract increased the latency time by 25.6% at 10 mg/kg i.p. compared to 2-phenylquinoline which was less effective. It appears that the antinociceptive effects of this plant may be attributed, at least in part, to the presence of some antinociceptive alkaloids in minor concentrations.

摘要

本研究评估了从长花加里匹亚(芸香科)树皮中获得的生物碱提取物和2-苯基喹啉对小鼠不同疼痛模型的镇痛特性。结果表明,生物碱提取物产生了显著的镇痛作用,所检测到的主要生物碱2-苯基喹啉表现出中等活性。生物碱提取物腹腔注射的半数抑制剂量(ID50)计算值为20.3mg/kg,口服给药时小于50mg/kg,在扭体试验中,经两种给药途径证明其比参比药物更有效。2-苯基喹啉腹腔注射的ID50为52.8mg/kg,口服100mg/kg时抑制率为24.5%。在福尔马林试验中,生物碱提取物在腹腔注射10mg/kg时可显著抑制疼痛的两个阶段(神经源性和炎症性),抑制率分别为37.4%和58.3%,而2-苯基喹啉则无此作用。生物碱提取物和2-苯基喹啉在辣椒素和谷氨酸试验中仅产生适度的作用。在热板试验中,与效果较差的2-苯基喹啉相比,生物碱提取物腹腔注射10mg/kg时可使潜伏期延长25.6%。看来该植物的镇痛作用至少部分可归因于存在少量的某些镇痛生物碱。

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