Guedes M M, Cunha A N, Silveira E R, Rao V S
Planta Med. 2002 Nov;68(11):1044-6. doi: 10.1055/s-2002-35664.
Centipedic acid and 12-acetoxy-hawtriwaic acid lactone, diterpenes isolated from the flower buds of Egletes viscosa (Asteraceae) were assayed for antinociceptive and gastroprotective activities in animal models of nociception and gastric ulcer. In the chemical nociception induced in mice by intraperitoneal acetic acid and subplantar formalin injections, both diterpenes (25 and 50 mg/kg, p. o.) exerted potent antinociception in a manner similar to indomethacin (5 mg/kg, p. o.). In the formalin test, only the late phase nociceptive response (20 - 25 min) and not the early phase response (0 - 5 min) was inhibited by these diterpenes. However, these compounds were found to be ineffective against thermal nociception in the hot-plate test. Further, the diterpenes reduced the severity of absolute ethanol-induced gastric lesions in rats. At the dose of 50 mg/kg, both centipedic acid and 12-acetoxy hawtriwaic acid suppressed the gastric lesions by 53 % and 63 %, respectively. Against the gastric ulceration induced by indomethacin, only centipedic acid (25 and 50 mg/kg) showed significant inhibition by about 47 - 49 %. The data suggested the gastroprotective and peripheral analgesic properties of diterpenes isolated from E. viscosa.
从粘毛蟛蜞菊(菊科)花蕾中分离得到的二萜类化合物蜈蚣草酸和12-乙酰氧基-豪特里韦酸内酯,在伤害感受和胃溃疡动物模型中进行了抗伤害感受和胃保护活性测定。在通过腹腔注射醋酸和足底注射福尔马林诱导的小鼠化学性伤害感受实验中,两种二萜类化合物(25和50毫克/千克,口服)均以类似于吲哚美辛(5毫克/千克,口服)的方式发挥了强效抗伤害感受作用。在福尔马林试验中,这些二萜类化合物仅抑制了晚期伤害感受反应(20 - 25分钟),而未抑制早期反应(0 - 5分钟)。然而,在热板试验中发现这些化合物对热伤害感受无效。此外,二萜类化合物减轻了大鼠绝对乙醇诱导的胃部损伤。在50毫克/千克的剂量下,蜈蚣草酸和12-乙酰氧基豪特里韦酸分别使胃部损伤抑制了53%和63%。对于吲哚美辛诱导的胃溃疡,只有蜈蚣草酸(25和50毫克/千克)表现出约47 - 49%的显著抑制作用。数据表明从粘毛蟛蜞菊中分离得到的二萜类化合物具有胃保护和外周镇痛特性。