Valencia E, Feria M, Díaz J G, González A, Bermejo J
Centro de Productos Naturales Orgánicos A. González, IPNAC-CSIC, Tenerife, Spain.
Planta Med. 1994 Oct;60(5):395-9. doi: 10.1055/s-2006-959517.
Lapidin, a bicyclic sesquiterpene from Ferula linkii Webb, has been evaluated for antinociceptive, anti-inflammatory, and antipyretic activities in mice and rats. Lapidin, vehicle, or the appropriate reference analgesic and anti-inflammatory compounds (acetylsalicylic acid [ASA] and indomethacin) were injected i.p. The more conspicuous effects of lapidin were: 1) a significant protective effect (17-62%; 2.5-20 mg/kg) towards writhings and stretchings induced by acetic acid in mice; 2) a significant antinociceptive effect on jumping responses in the hot-plate test (120 seconds at 15 mg/kg vs. 40 and 85 seconds in vehicle and ASA-treated mice, respectively); 3) a significant dose-dependent (5-15 mg/kg) antinociceptive effect against mechanical noxious stimuli; 4) a dose-dependent anti-inflammatory effect in the carrageenan-induced edema which, at the higher dose (20 mg/kg), was comparable (65% inhibition of paw swelling at 3 hours) to that obtained after indomethacin (10 mg/kg); and 5) a moderate antipyretic effect against yeast-induced hyperthermia. Present results demonstrate that lapidin possesses antinociceptive, anti-inflammatory, and less pronounced antipyretic effects comparable to those of classical non-steroid anti-inflammatory drugs, which make it worthy of further investigations as an antinociceptive and anti-inflammatory drug.
拉皮定是从里氏阿魏(Ferula linkii Webb)中提取的一种双环倍半萜,已在小鼠和大鼠中评估了其抗伤害感受、抗炎和解热活性。腹腔注射拉皮定、赋形剂或适当的参考镇痛和抗炎化合物(乙酰水杨酸[ASA]和吲哚美辛)。拉皮定更显著的作用有:1)对小鼠醋酸诱导的扭体和伸展反应有显著的保护作用(17 - 62%;2.5 - 20 mg/kg);2)在热板试验中对跳跃反应有显著的抗伤害感受作用(15 mg/kg时为120秒,而赋形剂处理的小鼠和ASA处理的小鼠分别为40秒和85秒);3)对机械性有害刺激有显著的剂量依赖性(5 - 15 mg/kg)抗伤害感受作用;4)对角叉菜胶诱导的水肿有剂量依赖性抗炎作用,在较高剂量(20 mg/kg)时,与吲哚美辛(10 mg/kg)后的抗炎效果相当(3小时时爪肿胀抑制率为65%);5)对酵母诱导的发热有中等程度的解热作用。目前的结果表明,拉皮定具有与经典非甾体抗炎药相当的抗伤害感受、抗炎和不太明显的解热作用,这使其作为一种抗伤害感受和抗炎药物值得进一步研究。