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科科瓦多叶下珠水醇提取物的强效抗伤害感受活性。

Potent antinociceptive activity of a hydroalcoholic extract of Phyllanthus corcovadensis.

作者信息

Gorski F, Corrêa C R, Filho V C, Yunes R A, Calixto J B

机构信息

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

出版信息

J Pharm Pharmacol. 1993 Dec;45(12):1046-9. doi: 10.1111/j.2042-7158.1993.tb07178.x.

Abstract

This study analyses the analgesic effect of a hydroalcoholic extract (HE) from Phyllanthus corcovadensis in several models of pain in mice. HE (3-60 mg kg-1, i.p.) or (100-500 mg kg-1, p.o.) caused a graded and potent analgesic effect against the abdominal constriction response caused by acetic acid and acetylcholine with an ID50 of about 3 and 100 mg kg-1, respectively. In the tail-flick model HE (up to 500 mg kg-1, p.o.) was without effect, while morphine (1-10 mg kg-1, s.c.) caused a graded increase in pain latency (ID50, 3 mg kg-1). HE (1-300 mg kg-1) given both intraperitoneally and orally caused a potent and graded inhibition of the second phase of formalin-induced persistent pain in mice with an ID50 of 1 and 80 mg kg-1, respectively. In contrast, morphine (1-5 mg kg-1, s.c.) inhibited both phases of formalin-induced pain with an ID50 of 2.5 mg kg-1. Indomethacin (1-10 mg kg-1, i.p.) only inhibited the second phase of formalin-induced pain with an ID50 of about 3 mg kg-1. The analgesic effect of indomethacin, but not that caused by morphine and HE was accompanied by a graded inhibition of formalin-induced mouse paw oedema. In addition, HE up to 1 g kg-1 failed to prevent carrageenan- and dextran-induced rat hindpaw oedema. It is concluded that HE exhibits a potent antinociceptive profile, either when given intraperitoneally or orally.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

本研究分析了来自科科瓦多叶下珠的水醇提取物(HE)对小鼠多种疼痛模型的镇痛作用。HE(3 - 60毫克/千克,腹腔注射)或(100 - 500毫克/千克,口服)对乙酸和乙酰胆碱引起的腹部收缩反应产生分级且有效的镇痛作用,其半数抑制剂量(ID50)分别约为3和100毫克/千克。在甩尾模型中,HE(高达500毫克/千克,口服)无效,而吗啡(1 - 10毫克/千克,皮下注射)使疼痛潜伏期分级增加(ID50,3毫克/千克)。腹腔注射和口服给予HE(1 - 300毫克/千克)均能有效且分级抑制小鼠福尔马林诱导的持续性疼痛的第二阶段,ID50分别为1和80毫克/千克。相比之下,吗啡(1 - 5毫克/千克,皮下注射)抑制福尔马林诱导疼痛的两个阶段,ID50为2.5毫克/千克。吲哚美辛(1 - 10毫克/千克,腹腔注射)仅抑制福尔马林诱导疼痛的第二阶段,ID50约为3毫克/千克。吲哚美辛的镇痛作用伴有福尔马林诱导的小鼠爪肿胀的分级抑制,而吗啡和HE引起的镇痛作用则不然。此外,高达1克/千克的HE未能预防角叉菜胶和右旋糖酐诱导的大鼠后爪肿胀。结论是,无论腹腔注射还是口服,HE均表现出有效的抗伤害感受作用。(摘要截短于250字)

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