Analgesic and anti-inflammatory activities of the isomeric mixture of alpha- and beta-amyrin from Protium heptaphyllum (Aubl.) march.

Gislei Frota Aragão, Marta Cristhiany Cunha Pinheiro, Paulo Nogueira Bandeira, Telma Leda Gomes Lemos, Glauce S de Barros Viana
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引用次数: 29

Abstract

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.

七叶丙氨酸α -和β -amyrin异构体混合物的镇痛和抗炎活性。
在目前的工作中,我们证明了-和-amyrin (AMI)的混合物从七脯蛋白具有抗伤性活性,从老鼠的扭体和福尔马林试验是明显的。AMI(10和50 mg/kg, i.p)分别抑制73%和94%的扭体,同时优先抑制第二阶段反应(37和51;1期和2期的抑制率分别为60%和73%)。纳洛酮,一种阿片类拮抗剂,没有逆转抗感觉作用。AMI (50 mg/kg, i.p)在热板实验中也有活性,在30和60 min后对热刺激的反应时间分别增加62%和71%。在卡拉胶诱导足跖水肿的小鼠中观察到一种预防性的抗水肿作用。给药10、25和50 mg/kg后3小时,爪体积分别显著减少39.2%和53%,且呈剂量依赖性。AMI(25和50 mg/kg, i.p)也能逆转卡拉胶诱导的水肿(疗效)。AMI(10和25 mg/kg, i.p)对右旋糖酐诱导的足跖水肿同样有效(预防作用),在给药后第2小时使足跖体积减少50%和60%,在给药后第3小时使足跖体积减少63%和73%。AMI (50mg /kg, ig)使右旋糖酐注射后已形成的水肿恢复(疗效)。综上所述,AMI具有独立于阿片系统的外周和中枢镇痛作用,并具有有效的抗炎活性。吲哚美辛和沙利度胺均能增强抗炎活性,提示可能与前列腺素和TNFalpha抑制有关。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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