七叶丙氨酸α -和β - amyrin异构体混合物的镇痛和抗炎活性3月

G. Aragão, M. C. Pinheiro, P. Bandeira, T. L. Lemos, G. Viana
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引用次数: 30

摘要

在目前的工作中,我们证明了从七叶丙中提取的α -和β -amyrin (AMI)的混合物具有抗伤害活性,这从小鼠的扭体和福尔马林试验中得到了明显的证明。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%。在卡拉胶诱导的足跖水肿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dex- trann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。吲哚美辛和沙利胺均能增强抗炎活性,提示可能与前列腺素和tnf - α抑制有关。
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Analgesic and Anti-Inflammatory Activities of the Isomeric Mixture of Alpha- and Beta-Amyrin from Protium heptaphyllum(Aubl.) March
In the present work, we demonsteated that the mixture of alpha- and beta-amyrin (AMI) from Protium heptaphyllum has anti-nociceptive 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-in-duced 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 dex-tran-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 anti-inflammatory activity was potentiated by both indomethacin and thalid-omide, suggesting a potential involvement of prostaglandins and TNF-alpha inhibitions.
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