Aragão Gislei Frota, Cunha Pinheiro Marta Cristhiany, Nogueira Bandeira Paulo, Gomes Lemos Telma Leda, de Barros Viana Glauce S
Department of Physiology and Pharmacology, Federal University of Ceará, Rua Cel. Nunes de Melo 1127, Fortaleza, 60431-970, Brazil.
J Herb Pharmacother. 2007;7(2):31-47. doi: 10.1300/j157v07n02_03.
In the present work, we demonstrated that the mixture of alpha- and beta-amyrin (AMI) from Protium heptaphyllum has antinociceptive activity as was evident from the writhing and formalin tests in mice. AMI (10 and 50 mg/kg, i.p.) inhibited writhing in 73 and 94%, respectively, while preferentially inhibiting the 2nd phase of the response (37 and 51; and 60 and 73% inhibitions of the 1st and 2nd phases, respectively) to the formalin test. Naloxone, an opioid antagonist, did not reverse the antinociceptive effect. AMI (50 mg/kg, i.p.) was also active in the hot plate test, increasing the reaction time to thermal stimulus after 30 and 60 min, by 62 and 71%, respectively. A preventive antiedematogenic effect was observed in mice that had a carrageenan-induced paw edema. Paw volume was significantly and dose-dependently decreased by 39, 42 and 53%, three hours after administration of 10, 25 and 50 mg/kg doses, i.p., respectively. AMI (25 and 50 mg/kg, i.p.) was also able to reverse the edema already induced by carrageenan (curative effect). AMI (10 and 25 mg/kg, i.p.) was equally effective in the dextran- induced paw edema (preventive effect), reducing the paw volume by 50 and 60% at the 2nd hour, and by 63 and 73% at the third hour post-dose. AMI (50 mg/kg, i.p.) reverted the edema already formed after the dextran injection (curative effect). In conclusion, AMI demonstrated peripheral and central analgesic effects independent of the opioid system, and also showed a potent anti-inflammatory activity. The antiinflammatory activity was potentiated by both indomethacin and thalidomide, suggesting a potential involvement of prostaglandins and TNFalpha inhibitions.
在本研究中，我们证明了来自七叶柿的α-和β-香树脂醇（AMI）混合物具有抗伤害感受活性，这在小鼠扭体试验和福尔马林试验中很明显。AMI（10和50mg/kg，腹腔注射）分别抑制73%和94%的扭体反应，同时优先抑制福尔马林试验反应的第二阶段（第一阶段和第二阶段的抑制率分别为37%和51%；60%和73%）。阿片类拮抗剂纳洛酮不能逆转抗伤害感受作用。AMI（50mg/kg，腹腔注射）在热板试验中也有活性，30分钟和60分钟后对热刺激的反应时间分别增加62%和71%。在角叉菜胶诱导的小鼠足爪水肿模型中观察到预防性抗水肿作用。腹腔注射10、25和50mg/kg剂量后3小时，足爪体积分别显著且剂量依赖性地减少39%、42%和53%。AMI（25和50mg/kg，腹腔注射）也能够逆转角叉菜胶已经诱导的水肿（治疗作用）。AMI（10和25mg/kg，腹腔注射）在右旋糖酐诱导的足爪水肿模型中同样有效（预防作用），给药后第2小时足爪体积减少50%和60%，第3小时减少63%和73%。AMI（50mg/kg，腹腔注射）逆转了右旋糖酐注射后已经形成的水肿（治疗作用）。总之，AMI表现出不依赖阿片系统的外周和中枢镇痛作用，并且还显示出强大的抗炎活性。吲哚美辛和沙利度胺均增强了抗炎活性，提示可能涉及前列腺素和肿瘤坏死因子α的抑制作用。
