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从科科瓦多叶下珠中分离出的类固醇对小鼠的镇痛特性。

Antinociceptive properties of steroids isolated from Phyllanthus corcovadensis in mice.

作者信息

Santos A R, Niero R, Filho V C, Yunes R A, Pizzolatti M G, Delle Monache F, Calixto J B

机构信息

Department of Pharmacology, Universidade Federal de Santa Catarina, Florianópolis, Brazil.

出版信息

Planta Med. 1995 Aug;61(4):329-32. doi: 10.1055/s-2006-958093.

DOI:10.1055/s-2006-958093
PMID:7480179
Abstract

The antinociceptive actions of the steroid compounds isolated from the leaves, stems, and roots of P. corcovadensis have been investigated in mice. Stigmasterol, stigmasterol acetate, beta-sitosterol, and aspirin (3-100 mk/kg, i.p.) inhibited, in a dose-related manner, acetic acid-induced abdominal constriction in mice with ID50s of 16, 11, 9, and 24 mg/kg, respectively. In the formalin test, stigmasterol and stigmasterol acetate (10-100 mg/kg, i.p.) caused graded inhibition of both the neurogenic (first phase) and inflammatory phases (second phase) of formalin-induced pain. However, both compounds were more effective in relation of the second phase of the formalin test with ID50 values of 26 and 41 mg/kg, respectively. Furthermore, both steroids failed to affect the edematogenic response of the formalin test. Given orally, stigmasterol and stigmasterol acetate (50-200 mg/kg) also exhibited significant though less potent analgesic action against both acetic acid- and formalin-induced nociception in mice. In addition, stigmasterol (up to 100 mg/kg, i.p.), in contrast to morphine (10 mg/kg, s.c.), had no analgesic effect in either tail-flick or hot-plate models. These findings suggest that stigmasterol and beta-sitosterol may account, at least in part, for the antinociceptive actions reported previously for the hydroalcoholic extract of Phyllanthus corcovadensis.

摘要

已对从科科瓦多叶下珠的叶、茎和根中分离出的甾体化合物在小鼠中的抗伤害感受作用进行了研究。豆甾醇、乙酸豆甾醇酯、β-谷甾醇和阿司匹林(3 - 100毫克/千克,腹腔注射)以剂量相关的方式抑制了乙酸诱导的小鼠腹部收缩,其半数抑制剂量(ID50)分别为16、11、9和24毫克/千克。在福尔马林试验中,豆甾醇和乙酸豆甾醇酯(10 - 100毫克/千克,腹腔注射)对福尔马林诱导疼痛的神经源性(第一阶段)和炎症阶段(第二阶段)均产生了分级抑制作用。然而,这两种化合物在福尔马林试验的第二阶段更有效,其ID50值分别为26和41毫克/千克。此外,这两种甾体均未影响福尔马林试验的致水肿反应。口服时,豆甾醇和乙酸豆甾醇酯(50 - 200毫克/千克)对小鼠乙酸和福尔马林诱导的伤害感受也表现出显著但效力较弱的镇痛作用。此外,与吗啡(10毫克/千克,皮下注射)不同,豆甾醇(高达100毫克/千克,腹腔注射)在甩尾或热板模型中均无镇痛作用。这些发现表明,豆甾醇和β-谷甾醇可能至少部分地解释了先前报道的科科瓦多叶下珠水醇提取物的抗伤害感受作用。

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