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.     

Antiinflammatory,Analgesic and Antipyretic Activities of Aerial Parts of Costus speciosus Koen

In the present study, methanol extracts of Costus speciosus Koen. aerial parts were assessed for antiinflammatory, analgesic and antipyretic activities in experimental animals. The antiinflammatory activity of methanol extract of Costus speciosus (400 and 800 mg/kg, p.o.) was evaluated using carrageenan-induced paw oedema test. 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 methanol extract of aerial parts of Costus speciosus in a dose of 400 and 800 mg/kg showed significant antiinflammatory activity (19.36 and 40.05% reduction) at 5 h postmedication. In analgesic models extract treated animals at (400 and 800 mg/kg) inhibited writhing’s caused by acetic acid by 14.24 and 31.90%, respectively, and it also increased the latency period at both high and low doses which showed the mean reaction time at 16.60±0.355 s and 14.12±0.355 s, respectively, when compared to control in hot-plate test. It also reduces the rectal temperature of the animals at low and high doses significantly 37.03±0.108° and 36.63±0.098°, respectively, in Brewer’s yeast induced pyrexia. The obtained results of the present investigation revealed that methanol extract of Costus speciosus has significant antiinflammatory, analgesic and antipyretic activities.     

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。     

我院2004—2008年解热镇痛抗炎药应用情况分析

目的了解解热镇痛抗炎药应用情况,促进合理用药。方法采用回顾性分析方法,对泸州医学院附属医院2004—2008年解热镇痛抗炎药的种类、销售金额、用药频度（DDDs）及日均费用（DDC）等进行统计、分析。结果5年中,解热镇痛抗炎药销售金额所占比例逐年降低;各类解热镇痛抗炎药的销售金额排序每年基本一致,其他类稳居第1位;单品种销售金额排序中,尼美舒利胶囊始终处于首位;尼美舒利胶囊和阿司匹林肠溶片的DDDs排序始终稳居前两位。结论解热镇痛抗炎药的应用渐趋合理、规范。     

肝胆结石片的镇痛,解热及利尿作用

ｉｇ肝胆结石片３．０、１．５ｇ（生药）／ｋｇ对醋酸所致小鼠的扭体反应抑制率分别为４２．８％、３９．２％;ｉｇ药后１５ｍｉｎ对甲醛所致小鼠的舔足反应的抑制率分别为５２．９％、３５．３％;３０ｍｉｎ的舐足抑制率分别为６８．０％、２３．３％均有显著的镇痛作用;对角叉菜胶致大鼠的升温时程曲线有显著的降低作用。且能促进大鼠尿排量的增加,增加率分别为２０７％、１４７％,表现出良好的利湿作用。     

Screening of Alkaloidal Fraction of Conium maculatum L. Aerial Parts for Analgesic and Antiinflammatory Activity

Conium maculatum Linn. (Umbelliferae) has been traditionally used in the treatment of spasmodic disorders, and to relieve nervous excitation, rheumatic pains in the old and feeble, pain in stomach, pain of gastric ulcer, nervousness and restlessness. Alkaloids have long been considered as bioactive group of constituents present in C. maculatum. Despite a long tradition of use, C. maculatum has not been evaluated pharmacologically to validate its traditional claims for analgesic and antiinflammatory activities. Thus, the present investigations were undertaken with an objective to evaluate alkaloidal fraction of C. maculatum aerial parts for analgesic and antiinflammatory activities. Test doses (100 or 200 mg/kg, p.o.) of alkaloidal fraction were evaluated for analgesic activity using tail flick test and antiinflammatory activity using carrageenan-induced paw oedema test in rats. Morphine (5 mg/kg, p.o.) and indomethacin (5 mg/kg, p.o.) were used as standard analgesic and antiinflammatory drugs, respectively. Alkaloidal fraction of the plant exhibited significant analgesic activity at a dose of 200 mg/kg as it showed significant increase in tail flicking reaction time with respect to the control during 2 h intervals of observation. It also exhibited significant antiinflammatory activity at a dose of 200 mg/kg as it inhibited paw oedema in rats to 71% and reduced the paw volume one-fourth to the control during 1^st h of the study. The present investigations suggest that alkaloids are responsible for analgesic and antiinflammatory activities of C. maculatum.     

上海市40有医院解热镇痛、非甾体抗炎药用药分析

为了解解热镇痛、非白体抗炎药在医院的使用情况、发展趋势，本文就1994～1996年上海市40家医院用药分析系统（HPDIS）医院的解热镇痛、非甾体抗炎药的销售量和金额分布作一分析。     

尼美舒利解热镇痛抗炎作用比较研究

目的研究尼美舒利的解热、镇痛、抗炎作用的量效关系,比较尼美舒利3种药理作用的ED50为临床合理使用尼美舒利提供依据。方法分别采用热灭活大肠埃希菌制备家兔发热模型、冰醋酸制备小鼠疼痛模型、角叉菜胶诱发大鼠足跖肿胀模型,观察尼美舒利的解热、镇痛、抗炎作用,并计算ED。结果尼美舒利能显著降低家兔体温,减少小鼠扭体次数,明显减轻大鼠足关节肿胀程度,其解热、镇痛、抗炎作用的ED50分别为0.85～1．95,2.56,3.15～4.05mg·kg^-1,根据体表面积比例换算成人ED50分别为0．50～0.60,2.72,0.26～0.59mg·kg^-1。结论尼美舒利发挥解热、镇痛和抗炎作用的ED,n存在差异,其中解热最低。     

Synthesis, Antiinflammatory and Antibacterial Activity of Novel Indolyl-isoxazoles

Chalcones were synthesized by reacting indole-3-aldehyde, prepared by Vilsemeir Haack reaction with 4-substituted acetophenone in ethanolic KOH solution. These chalcones were immediately reacted with hydroxylamine hydrochloride in presence of glacial acetic acid as reagent to obtain the corresponding isoxazole derivatives. The synthesized heterocycles were characterized on the basis of physical, chemical tests and spectroscopic data. These compounds were tested for the acute antiinflammatory activity and antibacterial activity using carrageenan-induced rat paw edema method and cup-plate method, respectively.     

2-Phenylimidazo[1,2-a]pyridine-3-carboxylic Acid Derivatives: Synthesis and Antiinflammatory Activity

A series of 2-phenylimidazo[1,2-a]pyridine-3-carboxylic esters, acids, and amides were synthesized and pharmacologically tested in order to evaluate their antiinflammatory and analgesic activity and their ulcerogenic action on the gastro-intestinal tract. The most active member of this series of compounds was found to be 6-methyl-2-phenylimidazo[1,2-a]pyridine-3-carboxylic acid ( 5c ).     

Synthesis,Antiinflammatory and Analgesic Activity of 4-Antipyrine Derivatives

Pharmaceutical Chemistry Journal -     

Synthesis and Antiinflammatory Activity of Newer Pyrazolinylbenzidines and Isoxazolinylbenzidines

In an effort to search for more active antiinflammatory agent, a series of pyrazolinylbenzidines and isoxazolylbenzidines was designed, synthesized, and screened for their potential as novel orally inflammation inhibitors. Compounds 4,4’-bis-(1”-acetyl-5”-substitutedaryl-2”-pyrazolin-3”-yl)benzidines (8-13) and 4,4’-bis-(2”-substitutedaryl-isoxazolin-4’-yl)benzidines (14-19) have been synthesized from 4,4’-bis-(substituted benzylidenyl-acetyl)benzidines (2-7). The structures of the products have been delineated by spectral and elemental analysis. Compounds 2-19 evaluated for antiinflammatory activity and acute toxicity and results are reported. The compound 4,4’-bis-[1”-acetyl-5”-(p-methoxyphenyl)-2”-pyrazolin-3’-yl)benzidine (9) showed more potent and dose-dependent antiinflammatory activity in comparison to reference drug.     

金刚藤分散片抗炎镇痛作用的药效学研究

目的:研究金刚藤分散片(JDT)的抗炎镇痛作用。方法:采用小鼠耳廓肿胀模型、大鼠足跖肿胀模型和大鼠棉球肉芽肿模型来进行JDT的抗炎作用研究;采用小鼠扭体反应实验来进行JDT的镇痛作用研究;同时与阳性对照药金刚藤胶囊(JC)进行比较。结果:JDT对二甲苯所致小鼠耳廓肿胀、蛋清所致大鼠足跖肿胀、大鼠棉球所致肉芽肿、醋酸所致小鼠扭体反应均有显著抑制作用,其效果均优于阳性对照药JC(P<0.05)。结论:JDT具有良好的抗炎镇痛作用。     

Lack of Antiinflammatory Activity of Metronidazole

Abstract: Metronidazole was given to rats with experimentally induced inflammation to evaluate whether the drug has any antiinflammatory effect. Inflammation was caused by injection of Freund's complete adjuvant into a paw. The oedema of the paw measured on the 4th day was not influenced after metronidazole 20 mg/kg/day or 160 mg/kg/day, whereas phenylbutazone 80 mg/kg/day significantly decreased the volume of the paw. The concentration of orosomucoid did not differ in the group of rats given metronidazole 20 mg/kg/day as compared to the control group. However, the orosomucoid concentration was lower in the group given metronidazole 160 mg/kg/day, as was the case in the phenylbutazone group. In groups of rats with polyarthritis studied on the 14th and 21st day there was no difference of arthritic index, volume of paw or orosomucoid concentration in neither low nor high dose metronidazole as compared to the control groups. The phenylbutazone groups, however, showed a lower arthritic index, lower volume of paw and lower orosomucoid concentration.     

Anti-Inflammatory,Analgesic, Antipyretic and Antibacterial Activity of Astragalus siculus Biv

Abstract

Astragalus siculus Biv. (endemic to Sicily) is used in popular medicine. Various extracts of Astragalus siculus Biv. showed marked anti-inflammatory, antipyretic and analgesic activities in rats and mice. The extracts also showed antimicrobial effects against Gram-negative and Gram-positive bacteria responsible for urinary tract infections.     

Design and syntheses of diarylisoxazoles: Novel inhibitors of cyclooxygenase‐2 (COX‐2) with analgesic‐antiinflammatory activity

A group of 4,5‐diphenylisoxazoles ( 11a–p ), 3,4‐diphenyl‐5‐trifluoromethylisoxazoles ( 15, 21 ), and 4,5‐diphenyl‐3‐methylsulfonamidoisoxazole ( 23 ) possessing a variety of substituents (H, F, MeS, MeSO, MeSO₂) at the para‐position of one of the phenyl rings were synthesized for evaluation as analgesic, and selective COX‐2 inhibitory antiinflammatory (AI), agents. Although the 4,5‐diphenylisoxazole group of compounds (11a–p) exhibited potent analgesic and AI activities, those compounds evaluated ( 11a, 11b, 11m ) were more selective inhibitors of COX‐1 than COX‐2, with the exception of 4‐(4‐methylsulphonylphenyl)‐5‐phenylisoxazole ( 11n ) that showed a modest COX‐2 selectivity index (SI) of 2.1. In contrast, 3‐(4‐methylsulphonylphenyl)‐4‐phenyl‐5‐trifluoromethylisoxazole ( 15 ), which retained good analgesic and AI activities, was a highly potent and selective COX‐2 inhibitor (COX‐1 IC₅₀ > 500 μM; COX‐2 IC₅₀ < 0.001 μM) with a COX‐2 SI of > 500,000, relative to the reference drug celecoxib (COX‐1 IC₅₀ = 22.9 μM; COX‐2 IC₅₀ = 0.0567 μM) with a COX‐2 SI of 404. The 3‐phenyl‐4‐(4‐methylsulphonylphenyl) regioisomer ( 21 ) was a less potent inhibitor (COX‐1 IC₅₀ = 252 μM; COX‐2 IC₅₀ = 0.2236 μM) with a COX‐2 SI of 1122, relative to the regioisomer ( 15 ). The related compound 4,5‐diphenyl‐3‐methylsulfonamidoisoxazole ( 23 ) exhibited similar (to 21 ) potency and COX‐2 selectivity (COX‐1 IC₅₀ > 200 μM; COX‐2 IC₅₀ = 0.226 μM) with an SI of 752. A molecular modeling (docking) study for the most potent, and selective, COX‐2 inhibitor (15) in the active site of the human COX‐2 enzyme showed the C‐5 CF₃ substituent is positioned 3.37 Å from the phenolic OH of Tyr³⁵⁵, and 6.91 Å from the Ser⁵³⁰ OH. The S‐atom of the MeSO₂ substituent is positioned deep (7.40 Å from the entrance) inside the COX‐2 secondary pocket (Val⁵²³). These studies indicate a C‐5 CF₃ ( 15, 21 ), or C‐3 NHSO₂Me ( 23 ), central isoxazole ring substituent is crucial to selective inhibition of COX‐2 for this class of compounds. Drug Dev. Res. 51:273–286, 2000. © 2001 Wiley‐Liss, Inc.     

2008—2010年解热镇痛抗炎药应用分析

目的:了解川北医学院附属医院解热镇痛药物使用情况及发展趋势,为今后的药物合理使用提供参考。方法:采用WHO推荐的用药频度(DDDs)作为评价药物利用的指标,回顾性分析我院2008—2010年解热镇痛抗炎药的整体、分类和重点单品种应用情况。结果:该类药物的用药品种、销售量、用药频度逐年增多;昔康类抗炎镇痛药在临床应用广泛,已成为一线药物。结论:疗效确切、不良反应少且价格适中的药物才是临床广泛应用、医患广泛认可的药物。     

Synthesis and Evaluation of Antiinflammatory, Analgesic and Ulcerogenic Potential of NSAIDs Bearing 1,3,4-Oxadiazole Scaffold

Synthesis of 1,3,4-oxadiazole derivatives of diclofenac and mefenamic acid are described. The target compounds 5-[2-(2,6-dichloroanilino)benzyl]-2-aryl-1,3,4-oxadiazole (3a-3e) and 5-[2-(2,3-dimethylanilino)phenyl]-2-(aryl)-1,3,4-oxadiazole (6a-6e) were obtained by treating 2 and 5 with various aromatic acids using POCl₃ as dehydrating agent. They were purified and characterized by IR, ¹H-NMR and elemental analysis. These compounds were further subjected to antiinflammatory, analgesic and acute ulcerogenic activity. Compound 3c and 6d exhibited good antiinflammatory activity and compounds 3c, 3e, 6c, 6d, 6e were found to be non ulcerogenic.     

Inhibition of brain cyclooxygenase-2 activity and the antipyretic action of nimesulide

The antipyretic action and the mechanism of action of 4-nitro-2-phenoxymethanesulfonanilide (nimesulide), a new nonsteroidal antiinflammatory drug, were investigated in yeast-induced febrile rats. Yeast-injected rats developed marked fever and exhibited an approximately 7-fold increase in brain levels of prostaglandin E₂ and an approximately 2-fold increase in the expression of cyclooxygenase-2 mRNA despite an almost unchanged expression of cyclooxygenase-1 mRNA. Nimesulide produced a dose dependent antipyretic action, which was stronger than that of indomethacin and ibuprofen, and decreased dose dependently the increased brain prostaglandin E₂ levels, whereas it did not influence the expression of cyclooxygenase-2 mRNA. It inhibited markedly the enhanced brain cyclooxygenase activity, primarily cyclooxygenase-2, in vivo and dose dependently increased brain cyclooxygenase activity in vitro. These results suggest that the marked antipyretic action of nimesulide is primarily mediated through the selective inhibition of the activity of brain cyclooxygenase-2 induced under febrile conditions.