牛黄消炎片的镇痛抗炎作用实验研究

用0.05g/ml和0.025g/ml12个剂量进行试验,均能明显抑制二甲苯引起的小鼠耳肿及角叉菜胶引起的大鼠足趾肿胀,对醋酸诱发的小鼠扭体反应也有明显的抑制作用,试验表明牛黄消炎片有明显的镇痛抗炎作用。     

Synthesis and pharmacological activity of 1,2,4-triazolo[4,3-a]quinolines

The synthesis of a series of 1,2,4-triazolo[4,3-a]quinoline derivatives is described; their structures were assigned by 1H NMR and analytical data. The new compounds were tested in vivo for their antiinflammatory and analgesic activities, as well as for their ulcerogenic action. Some of the tested triazoles showed an analgesic activity in the acetic acid writhing test and antiinflammatory properties on carrageenan paw edema assay.     

小儿抗感颗粒的药效学实验研究

目的观察小儿抗感颗粒的解热、镇痛、抗炎作用。方法采用皮下注射干酵母造成大鼠发热模型,观察其解热作用;采用醋酸扭体法观察其镇痛作用;采用二甲苯致小鼠耳廓肿胀观察其抗炎作用。结果小儿抗感颗粒能明显降低大鼠发热模型的体温,提高小鼠痛阈值,抑制二甲苯致小鼠耳廓肿胀。结论小儿抗感颗粒具有显著的解热、镇痛、抗炎作用。     

Analgesic, antiinflammatory and CNS depressant activities of sesquiterpenes and a flavonoid glycoside from Polygonum viscosum

Analgesic, antiinflammatory and CNS depressant activities of four sesquiterpenes, viscosumic acid, viscozulenic acid, viscoazucine and viscoazulone, and a flavonoid glycoside, quercetin-3-O-(6'-feruloyl)-beta-D-galactopyranoside isolated form the aerial parts of Polygonum viscosum (Polygonaceae) have been assessed. All test compounds exhibited CNS depressant activity in open field test, all but viscoazulone showed analgesic activity in Eddy's hot plate test, all sesquiterpenes inhibited acetic acid induced abdominal writhing in mice, and all but viscoazucine and the flavonoid glycoside exhibited mild to moderate antiinflammatory effect on carrageenan induced rat paw edema.     

Design and synthesis of some new thiazolo [3,2-b]-1,2,4-triazole-5(6H)-ones substituted with flurbiprofen as anti-inflammatory and analgesic agents

In the course of our ongoing studies, a series of thiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones substituted with flurbiprofen (CAS 5104-49-4) has been prepared. The compounds were synthesized by the cyclization of the 3-[(2-fluoro-4-biphenyl)ethyl]-5-mercapto-1,2,4-triazole (3) with chloroacetic acid and relevant benzaldehydes in the presence of acetic acid, acetic anhydride and anhydrous sodium acetate in one step. The product of this one-pot synthesis that precipitated on cooling of the reaction mixture was identified undoubtedly by X-ray crystallographic analysis as thiazolo[3,2-b]-1,2,4-triazole. In-vivo anti-inflammatory and analgesic activities of the compounds were assessed by carrageenan-induced hind paw edema and p-benzoquinone-induced abdominal constriction tests in mice, respectively. In addition, the ulcerogenic risks were evaluated. It is worthy of saying that the compounds which maintained analgesic/antiinflammatory activity of the starting compound were found to be safer with regard to gastric lesion risks at 100 mg/kg oral dose when compared with flurbiprofen. Among the synthesized compounds 3d showed the highest analgesic and antiinflammatory activity without inducing any gastric lesion and deserves further attention in order to develop new lead drug candidates.     

山芝麻的抗炎镇痛作用研究

目的研究山芝麻的抗炎镇痛作用。方法山芝麻高剂量31.2 g生药/kg、中剂量15.6 g生药/kg、低剂量7.8 g生药/kg,连续灌胃7 d抗炎实验采用二甲苯致小鼠耳廓肿胀模型和醋酸致小鼠腹腔毛细血管通透性增高模型,镇痛实验采用热板法和扭体法。结果山芝麻能显著抑制二甲苯引起的小鼠耳廓肿胀,抑制醋酸引起的小鼠腹腔毛细血管通透性增高,并降低小鼠热板痛阈值,减少醋酸引起的扭体次数。结论山芝麻具有抗炎镇痛作用。     

壮药红鱼眼三萜类成分镇痛和抗炎活性实验研究

目的研究壮药红鱼眼三萜类成分的镇痛和抗炎活性。方法采用扭体法观察镇痛作用;用二甲苯使小鼠致炎和醋酸致小鼠腹腔毛细血管通透性增加观察抗炎作用。结果红鱼眼三萜类成分对醋酸致痛具有明显的镇痛作用,对二甲苯所致炎性水肿也有显著的抑制作用。结论红鱼眼三萜类成分具有较好的镇痛、抗炎活性。     

去氧乌头碱的抗炎、镇痛和解热作用

本文报告了新近以伏毛铁棒锤中提得的去氧乌头碱(DAC)的抗炎、镇痛和解热作用实验结果,并与已报道过的3-乙酰乌头碱(3AAC)进行比较。DAC0.8mg/kg (ip)显著抑制巴豆油所致小鼠耳廓肿;0.2mg/kg(ip或sc)显著抑制角叉菜胶或甲醛所致大鼠足爪肿、组胺所致大鼠皮肤渗出及醋酸所致小鼠腹腔渗出。于大鼠角叉菜胶足爪肿模型,测得DAC(ip)的抗炎治疗指数(6.38)略高于3AAC(5.92)。醋酸扭体法测得DAC抑制小鼠扭体反应50％的剂量为0.22±0.06mg/kg(sc);热板法测得DAC的小鼠镇痛ED_(50)为0.41±0.10mg/kg(ip),其镇痛治疗指数(6.37)高于3AAC(4.60)。DAC0.24mg/kg(ip)对伤寒副伤寒混合菌苗所致家兔发热有显著解热作用。     

Antiinflammatory and analgesic activities of Thesium chinense Turcz extracts and its major flavonoids, kaempferol and kaempferol-3-O-glucoside

The ethyl acetate, chloroform extracts, and the two flavonoids kaempferol 1 and kaempferol-3-O-glucoside 2 isolated from whole plants of Thesium chinense Turcz were investigated for their antiinflammatory and analgesic activities. For the antiinflammatory activity, carrageenan-induced hind paw edema and xylene-induced mouse ear edema models, and for the analgesic activity, the acetic acid-induced abdominal constriction test was used. The ethyl acetate extract and two flavonoids showed significant (p<0.05 and p<0.01) and dose-dependent antiinflammatory and analgesic activity. The chloroform extract was inactive in the assay.     

Synthesis of some 1,2,4-triazolo[3,2-b]-1,3-thiazine-7-ones with potential analgesic and antiinflammatory activities

Starting from 3-substituted-1,2,4-triazole-5-thiones (la-h), eight new 5-carbomethoxy-2-substituted-7H-1,2,4-triazolo[3,2-b]-1,3-thiazine-7-ones (2a-h) were synthesized and characterized by spectral and elementary analysis. The obtained compounds were submitted to preliminary pharmacological assay to evaluate their antiinflammatory and analgesic activities as well as gastrointestinal irritation liability and acute toxicity. Among the compounds studied, compounds 2c, 2d, 2e and 2h showed most remarkable antiinflammatory activity in the carrageenan and serotonin induced edema and in the inhibition of castor oil-induced diarrhea tests. The analgesic activity of these active compounds correlated with their antiinflammatory activities in the inhibition of acetic acid-induced writhing test. In gastric ulceration studies, the compounds were found safety at low dose levels (10 and 20 mg/kg).     

布洛芬川芎嗪酯的抗炎镇痛作用

目的观察布洛芬川芎嗪酯的抗炎镇痛作用及其胃肠刺激性。方法采用醋酸扭体法、甲醛致痛法、二甲苯致耳肿胀法、角叉菜胶致足肿胀法及醋酸致腹腔毛细血管通透性增加法等实验方法。结果布洛芬川芎嗪酯灌胃给药对冰醋酸、甲醛所致小鼠炎症性疼痛有显著抑制作用 ,能够显著抑制二甲苯所致小鼠耳肿胀和角叉菜胶致足肿胀 ,降低醋酸致小鼠腹腔毛细血管通透性的增加 ,作用与布洛芬相似 ,胃刺激性小于布洛芬。结论布洛芬川芎嗪酯具有抗炎镇痛作用 ,而且不良反应小于布洛芬。     

乙醇提取新鲜当归油的抗炎镇痛作用

目的 :研究当归油的镇痛、抗炎作用。方法 :应用二甲苯致小鼠耳廓肿胀、醋酸致小鼠腹腔毛细血管通透性增高、蛋清致大鼠足跖肿胀及大鼠棉球肉芽肿增生4种动物模型进行抗炎药效学实验 ;采用醋酸致小鼠扭体反应 ,进行镇痛实验。结果 :当归油能显著抑制上述各种动物模型的炎症反应及醋酸引起的小鼠扭体反应。结论 :当归油对急、慢性炎症均有明显抑制作用 ,且有一定的镇痛效果。     

Antiinflammatory, Analgesic and Antipyretic Activities of Mimusops elengi Linn

In the present study, 70% ethanol extract of Mimusops elengi Linn. bark was assessed for antiinflammatory, analgesic and antipyretic activities in animals. The antiinflammatory activity of ethanol extract of Mimusops elengi (200 mg/kg, p.o) was evaluated using carrageenan-induced paw edema and cotton pellet-induced granuloma models. Analgesic effect was evaluated using acetic acid-induced writhing and Eddy's hot plate models and antipyretic activity was assessed by Brewer's yeast-induced pyrexia in rats. The ethanol extract of Mimusops elengi (200 mg/kg, p.o) significantly inhibited the carrageenan-induced paw oedema at 3rd and 4th h and in cotton pellet model it reduced the transudative weight and little extent of granuloma weight. In analgesic models the ethanol extract of Mimusops elengi decreases the acetic acid-induced writhing and it also reduces the rectal temperature in Brewer's yeast induced pyrexia. However, Mimusops elengi did not increase the latency time in the hot plate test. These results show that ethanol extract of Mimusops elengi has an antiinflammatory, analgesic and antipyretic activity.     

Analgesic and anti-inflammatory activities of total extract and individual fractions of Chinese medicinal ants Polyrhachis lamellidens

The ethanol extract of Chinese medicinal ants Polyrhachis lamelliden was evaluated for its analgesic and anti-inflammatory activities in mice. It was shown that the extract significantly inhibited acetic acid-induced writhing response and increased hot-plate pain threshold of mice at doses of 1.5 and 3.0 g crude drug/kg. Meanwhile, the extract significantly inhibited the increase in vascular permeability induced by acetic acid and in ear edema induced by xylene in mice. However, it had no obvious effect on leukocyte migration induced by carboxymethylcellulose sodium (CMC-Na). The ethanol extract suspended in water was partitioned with diethyl ether, ethyl acetate and n-butanol successively to yield four fractions including water fraction. Among these fractions, diethyl ether and ethyl acetate fractions were found to increase hot-plate pain threshold and to inhibit acetic acid-induced writhing response in mice. Water fractions markedly inhibited acetic acid-induced writhing response and reduced the dye leakage to the peritoneal cavity induced by acetic acid and ear edema induced by xylene. These results suggest that P. lamellidens presents remarkable analgesic and anti-inflammatory activity, which supported the traditional use of the medicinal ants in the treatment of various diseases associated with inflammation. The diethyl ether fraction has greater contribution to the overall analgesic activity, whereas the water fraction showed the greatest anti-inflammatory and peripheral analgesic activities.     

5,6-二芳基-2,3-二氢-1-吡咯里嗪酮类化合物的合成及抗炎镇痛活性

目的寻找高效低毒、有抗炎镇痛活性的新的吡咯里嗪酮类化合物。方法以二芳基取代杂环类COX-2选择性抑制剂为模板,以吡里酮为母体,设计并合成了5,6-二芳基-2,3-二氢-1-吡咯里嗪酮类化合物。用IR,¹HNMR和MS确定其结构。用二甲苯致小鼠耳肿胀法和小鼠醋酸扭体法测定这些化合物的(po 200mg·kg^-1)抗炎及镇痛活性。结果合成了17个新化合物(1-17)。生物实验结果显示,多数化合物有一定的抗炎和(或)镇痛活性。结论化合物3,8,11,14和15抗炎活性优于对照药布洛芬;化合物9,10和11镇痛活性接近于对照药布洛芬,值得进一步研究。     

Anti-inflammatory and analgesic amides: new developments

A series of substituted N-cycloalkyl benzamides, cinnamamides, and indole-3-carboxamides were synthesized and evaluated for their analgesic, antiinflammatory activities as well as for their gastrointestinal irritation liability. Indomethacin was used as reference drug in both tests. Compounds 1k, 1b, 1h, 1j, and 1g were the most active in the antiinflammatory paw edema inhibition test, with a sharply dose-dependent effect. In terms of the analgesic activity (acetic acid writhing test), the most active compound was 5a followed by 3a, but many other compounds were found to have a non-negligible potency. Even in this case, the effect was dose dependent.     

Analgesic and Anti-inflammatory Activities of the Aqueous Extract of Plantago major L.

This study aimed to validate the pharmacological effects of Plantago major L., a medicinal plant used to decrease pain and inflammation. The aqueous extract (AE) was prepared from the dried ground leaves. Pretreatment with AE (1 g/kg, p.o.) decreased writhing induced by acetic acid in mice, but it did not change the tail flick responses to heat nociceptive stimuli. In rats, AE (1 g/kg, p.o.) reduced the paw edema and pleurisy induced by carrageenin, but it did not alter the paw edema induced by dextran. The effect of AE on the carrageenin inflammatory responses was more intense than that obtained on the ear edema induced by croton oil in mice. In addition, daily treatment with AE (1 g/kg/day during 8 days, p.o.) inhibited the exudative process induced by croton oil injected into the air pouch of rats. The results indicate that the aqueous extract of Plantago major is endowed with effective antiinflammatory and analgesic activities.     

雷公藤茎、叶的抗炎镇痛药理作用研究

雷公藤叶吕提取物４００、２００ｍｇ／ｋｇｉ．ｇ给药,可明显减轻角又菜胶引起大鼠足跖肿胀和二甲苯引起小鼠耳廓的肿胀作用,对醋酸和小鼠扭体反应有明显抑制作用,表明雷公藤叶具有明显的抗炎,镇痛作用。     

赤丹丸抗炎镇痛的药效学研究

目的研究赤丹丸 (CDW )的抗炎、镇痛及对微循环的作用。方法采用冰乙酸致扭体、二甲苯致耳肿胀、塑料管致大鼠子宫炎及显微镜下观察小鼠耳廓微循环等实验方法。结果灌胃给予CDW对冰乙酸所致小鼠炎症性疼痛有明显的抑制作用 ,能显著抑制二甲苯所致小鼠耳肿胀和塑料管所致大鼠子宫肿胀 ,能明显促进小鼠耳廓微循环。结论赤丹丸具有较好的抗炎、镇痛及促进微循环的作用。     

Analgesic and antiinflammatory effects of 2-(10,11-dihydro-10-oxo-dibenzo[b,f]thiepin-2-yl)propionic acid in rat and mouse

Analgesic and antiinflammatory effects of 2-(10,11-dihydro-10-oxo-dibenzo[b,f]thiepin-2-yl)propionic acid (CN-100) have been investigated pharmacologically in rats and mice. With bradykinin-induced pain responses, CN-100 proved to be the most potent of the commercial non-steroidal antiinflammatory drugs which were tested in rats: The potency of CN-100 was 4 times stronger than that of indometacin. The analgesic effect of CN-100 on writhing induced by acetic acid, adjuvant-induced hyperalgesia, and carrageenin-induced hyperalgesia, and the effect on AgNO3-induced arthralgia were equipotent to or a little weaker than those of indometacin, but stronger than that of diclofenac sodium. In mice, CN-100 was found to be as active as indometacin against peritonitis induced by acetic acid and pain responses induced by mechanical stimulus (pressure). Against the peritonitis induced by acetylcholine and phenyl-quinone, CN-100 showed inhibitory actions and its potencies were much stronger than those of aminophenazone (amino-pyrine) in mice. However, all the drugs tested failed to increase pain thresholds induced by thermal stimulus in rats and mice. CN-100 exerted potent inhibitory effects on carrageenin-induced acute inflammatory edema and adjuvant-induced arthritis. The antiinflammatory effect of CN-100 on the former was equal to that of indometacin, but weaker on the latter. The ulcerogenic activity of CN-100 was less potent than that of indometacin. These results indicate that CN-100 may produce its analgesic effects through a peripheral mechanism and be preferable for clinical use, especially for the treatment of inflammatory conditions accompanied by pain.