龙胆苦苷镇痛抗炎药理作用研究

本文采用小鼠醋酸扭体法和热板法观察龙胆苦苷(gentiopicroside)的镇痛药理作用,采用二甲苯致小鼠耳廓肿胀、蛋清致大鼠足跖肿胀急性炎症模型及大鼠肉芽肿慢性炎症模型,考察龙胆苦苷的抗炎药理作用.龙胆苦苷经皮下注射给药,在小鼠醋酸扭体和热板法实验中,减少了扭体次数,提高了小鼠痛域阈值,呈良好的量效关系.明显减轻了二甲苯致小鼠耳廓肿胀,降低蛋清致大鼠足趾肿胀,抑制了大鼠肉芽肿.结果表明龙胆苦苷对热和化学刺激引起的疼痛反应有明显的镇痛作用,对急、慢性炎症反应均有一定的抑制作用.     

姜延胶囊抗炎镇痛作用实验研究

目的:观察姜延胶囊的抗炎镇痛作用.方法:采用醋酸致小鼠腹腔毛细管通透法、二甲苯致小鼠耳廓肿胀法、滤纸性肉芽肿法及小鼠热板法、扭体法镇痛实验等动物模型,考察姜延胶囊的抗炎镇痛效果.结果:姜延胶囊能明显减轻小鼠腹腔毛细血管通透性,对小鼠耳肿胀及肉芽肿均有抑制作用;并能减少热板及醋酸所致的小鼠疼痛反应,提高小鼠痛阈值.结论:姜延胶囊具有良好的抗炎镇痛作用,该实验为其临床应用提供了药理学依据.     

丁香苷抗炎镇痛作用及部分机制研究

研究丁香苷抗炎镇痛作用及部分机制。以阿司匹林作阳性对照药,观察丁香苷对二甲苯致小鼠耳廓肿胀、醋酸致小鼠毛细血管通透性增加、角叉菜胶致大鼠足趾肿胀、棉球致大鼠肉芽肿的抗炎作用;对小鼠热板试验、醋酸扭体试验的镇痛作用;同时测定角叉菜胶致大鼠炎足炎性渗出物中的PGE2、MDA和血清中的NO、SOD,初步探讨丁香苷抗炎镇痛的部分机制。结果表明,丁香苷对急慢性炎症反应有明显抑制作用,能明显降低角叉菜胶致炎足炎性渗出物中PGE2、MDA和血清中NO含量,明显增加血清中SOD的活性。因此,丁香苷具有较强的抗炎镇痛作用,其机制可能与抑制PGE2、NO等炎症介质生成、增强自由基清除能力有关。     

前列腺Ⅰ号抗炎镇痛作用以及抗前列腺炎的实验研究

采用热板法和扭体法观察前列腺Ⅰ号抗炎、镇痛以及抗大鼠实验性前列腺炎的作用。采用小鼠耳廓二甲苯制炎法观察抗炎作用,前列腺炎模型采用向大鼠前列腺组织内注入角叉菜胶的方法。结果显示前列腺Ⅰ号能减少小鼠扭体反应数,延长小鼠热板法引起的痛反应潜伏期,对小鼠耳廓肿胀有明显的抑制作用,前列腺炎模型试验中,前列腺液检查卵磷脂小体明显增加,白细胞数降低。因此前列腺Ⅰ号具有明显的抗炎、镇痛以及抗前列腺炎的作用。     

粗根荨麻水提取物的抗炎、镇痛作用实验研究

采用角叉菜胶大鼠致炎模型,醋酸扭体法、福尔马林致痛试验对粗根荨麻水提取物的抗炎、镇痛作用进行了研究。结果显示粗根荨麻水提取物可抑制角又菜胶所致大鼠足肿胀;并能明显抑制醋酸所致的小鼠扭体数,显著减少福尔马林致痛试验后期小鼠舔足行为。表明粗根荨麻水提取物具有一定的抗炎、镇痛作用。     

合萌水提物抗炎镇痛作用的实验研究

目的:观察合萌水提物的抗炎、镇痛作用。方法:采用二甲苯致小鼠耳肿胀、角叉菜胶致小鼠足跖肿胀、醋酸致小鼠腹腔毛细血管通透性增加及醋酸致小鼠扭体实验、热板实验模型,观察合萌水提物的抗炎镇痛作用,并测定丙二醛(MDA)、一氧化氮(NO)的含量及超氧化物歧化酶(SOD)活性。结果:合萌水提物可抑制二甲苯致小鼠耳肿胀,减轻小鼠足跖肿胀,降低小鼠毛细血管通透性,减少醋酸致小鼠扭体次数,增加热板小鼠痛阈值,降低血清MDA、NO含量,提高血清SOD活性。结论:合萌水提物具有抗炎镇痛作用,作用机制可能与降低血管通透性、抑制NO等炎症介质产生及增强清除自由基、抗脂质过氧化能力有关。     

小茴香挥发油的抗炎镇痛作用

目的：研究小茴香挥发油的抗炎、镇痛作用,为指导临床合理用药提供科学依据。方法：应用二甲苯致小鼠耳廓肿胀、蛋清致大鼠足肿胀2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：小茴香挥发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：小茴香挥发油具有抗炎和镇痛作用。     

小茴香挥发油的抗炎镇痛作用

目的:研究小茴香挥发油的抗炎、镇痛作用,为指导临床合理用药提供科学依据。方法:应用二甲苯致小鼠耳廓肿胀、蛋清致大鼠足肿胀2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:小茴香挥发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:小茴香挥发油具有抗炎和镇痛作用。     

乌头总生物碱贴片抗炎镇痛药效学研究

本文采用蛋清所致大鼠足跖肿胀和小鼠二甲苯所致耳廓肿胀模型研究乌头总生物碱贴片的抗炎作用及化学刺激法和热板法研究乌头总生物碱贴片对小鼠的镇痛作用进行实验.镇痛抗炎实验表明,乌头总生物碱贴片能提高小鼠热板法所致疼痛的痛阈值并减少醋酸所致小鼠扭体反应次数;对二甲苯所致小鼠耳肿胀有明显的抑制作用,能明显减轻蛋清所致的大鼠足跖肿胀.结果表明乌头总生物碱贴片具有明显的抗炎及镇痛作用.     

臭灵丹水提取物的急性毒性及镇痛作用的实验研究

采用上下移动法,醋酸扭体法、热板法、福尔马林致痛试验对臭灵丹水提取物的急性毒性及镇痛作用进行了研究。结果显示：臭灵丹水提取物LD50（腹腔注射）为1．19g／kg;臭灵丹水提取物明显抑制醋酸所致的小鼠扭体数,显著减少福尔马林致痛试验后期小鼠舔足行为;而对热板法所致疼痛无明显作用。表明臭灵丹水提取物具有一定的外周镇痛作用。     

Analgesic and anti-inflammatory effects and safety profile of Cucurbita maxima and Cucumis sativus seeds

The premise of the pharmacology of natural product is to explore benefits of natural resources for the mankind. Medicines extracted from natural resources are considered as primary source for drug discovery. Thus, the current study was designed to evaluate the safety profile and explore the analgesic and anti-inflammatory activity of ethanol extract of Cucurbita maxima (C. maxima) and Cucumis sativus (C. sativus) seeds. These seeds are edible, good in taste and have been used for several therapeutic purposes. Acute toxicity of the seeds was evaluated by Lorke’s method while Eddy’s hot plate and tail immersion methods were used to assess analgesic activity in mice. Anti-inflammatory activity was evaluated by rat hind paw edema method. The seed extracts of C. maxima and C. sativus were found to be safe and showed significant analgesic and anti-inflammatory activity in comparison with the control group. The therapeutic effects of these extracts were almost comparable to aspirin and brufen. Therefore, the seeds can be used as effective analgesic and anti-inflammatory agents.     

Anti-inflammatory and analgesic activity of ononitol monohydrate isolated from Cassia tora L. in animal models

Ononitol monohydrate (OM) was isolated from Cassia tora L. leaves. The anti-inflammatory and analgesic activities of OM have been examined in male Wistar rats and mice. The efficacy of OM against inflammation was studied by using carrageenan-induced paw oedema, croton oil-induced ear oedema, acetic acid-induced vascular permeability, cotton pellet-induced granuloma and adjuvant-induced arthritis. The analgesic activity of OM was assessed using the acetic acid-induced abdominal constriction response, formalin-induced paw licking response and the hot-plate test. In acute type inflammation models, maximum inhibitions of 50.69 and 61.06% (P < .05) were noted with 20 mg/kg of OM in carrageenan-induced hind paw oedema and croton oil-induced ear oedema, respectively. Treatment of OM (20 mg/kg) meaningfully (P < .05) reduced the granuloma tissue formation by cotton pellet study at a rate of 36.25%. OM (20 mg/kg) inhibited 53.64% of paw thickness in adjuvant-induced arthritis model. OM has also been produced significant (P < .05) analgesic activity in acetic acid-induced abdominal constriction response, formalin-induced paw licking response and in hot-plate test suggesting its peripheral and central analgesic potential. The outcomes of the present study proposed that OM influenced on the anti-inflammatory and analgesic activities.     

Design,synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory,analgesic activities and docking study

A group of novel isoindoline hybrids incorporating oxime, hydrazone, pyrazole, chalcone or aminosulfonyl pharmacophores (9–14) was designed and characterized by spectral data and elemental analyses results. All newly synthesized compounds were evaluated as COX-2 inhibitors, anti-inflammatory and analgesic agents. Six hybrid derivatives (10b, 10c, 11a, 11d, 13, 14) were moderate COX-2 inhibitors (IC₅₀ = 0.11–0.18 µM) close to standard celecoxib (IC₅₀ = 0.09 µM). The most active compounds showed outstanding in vivo anti-inflammatory activity (% edema inhibition = 41.7–50, 1 h; 40.7–67.4, 3 h; 20–46.7, 6 h) better than reference drug diclofenac (% edema inhibition = 29.2, 1 h; 22.2, 3 h; 20, 6 h). Most compounds showed significant peripheral and/or central analgesic activity. The moderate selective COX-2 inhibitor; dimethoxychalcone 11d (SI = 103) displayed excellent anti-inflammatory activity (% edema inhibition = 45.8–59.3) and increased thermal pain threshold (50–92.85%) comparable to piroxicam (75%). Molecular docking studies have been established.     

Analgesic and anti-inflammatory studies of cyclopeptide alkaloid fraction of leaves of Ziziyphus nummularia

Ziziyphus nummularia (family: Rhamnaceae) is a thorny small bush, grows in abundance in the grazing lands of the arid areas of Rajasthan, India. It is an important ethnomedicinal plant of the Thar Desert; local inhabitants use every part of the plant as medicine. Kernels are prescribed in pregnancy as soporific, antiemetic and for relieving abdominal pain. The insect gall is powered and given orally with water to cure bone fracture. Crushed root is applied on the paining shoulder of the bullock. The decoction of leaves is used for the treatment of cough and cold; leaves are also regarded as diaphoretic and prescribed in typhoid. Paste of leaves is used for healing of cuts, boils and cutaneous disease. It is widely used in pain and inflammatory conditions.Z. nummularia contains a unique group of alkaloids known as cyclopeptide alkaloids, in continuation of our work carried out on the leaves of Z. nummularia, present study was initiated to explore antiinflammatory and analgesic potential of cyclopeptide alkaloids isolated from the leaves of Z. nummularia (IFZN). Anti-inflammatory activity was tested against rat paw oedema, mouse peritonitis and cotton pellet granuloma. For screening of analgesic activity, acetic acid induced writhing, tail flick and hot plate test were performed.IFZN 30 mg/kg shows the anti-oedematogenic effect against paw oedema induced by carrageenan, dextran, serotonin and histamine; IFZN 20 and 30 mg/kg were found to have highly significant anti-nociceptive effects.Result of pharmacological studies indicated that IFZN is a potent and efficacious analgesic agent. The analgesic activity of IFZN is mediated by the peripheral as well as central pathways.     

蕲蛇提取物抗炎镇痛药理作用的研究

目的 研究蕲蛇提取物的抗炎及镇痛作用,为蕲蛇的临床应用提供科学依据.方法 采用热板法、冰醋酸刺激致痛法研究蕲蛇提取物对小鼠痛阈的影响,利用二甲苯致小鼠耳廓炎症模型和腹腔染料渗出法测定蕲蛇提取物的抗炎作用.结果 蕲蛇提取物醇溶性和水溶性部位对小鼠热板及冰醋酸致痛反应有明显镇痛作用,对二甲苯致小鼠耳廓肿胀、冰醋酸致腹腔毛细血管通透性增高均有明显的抑制作用.结论 蕲蛇提取物醇溶性和水溶性部位有一定的抗炎及镇痛作用,并且水溶性部位较醇溶性部位的药效好,可为蕲蛇的临床应用提供指导作用.     

Synthesis and anti-inflammatory activity of some new 4,5-dihydro-1,5-diaryl-1H-pyrazole-3-substituted-heteroazole derivatives

A series of 4,5-dihydro-1,5-diaryl-1H-pyrazole-3-substituted-heteroazoles were designed and synthesized in order to obtain new compounds with potential anti-inflammatory activity. The title compounds were screened for in vivo anti-inflammatory activity by using Carrageenan induced rat paw edema method. Diclofenac sodium was used as a standard drug for comparison. Out of the 30 compounds tested, compound 19a, 19b, 25a, 25b exhibited significant anti-inflammatory activity. Selected compounds were also screened for in vitro COX-2 inhibition assay and analgesic activity in the acetic acid induced writhing model.     

血脂康胶囊对冠心病患者的抗氧化及抗炎效果研究

目的：探讨血脂康胶囊对冠心病患者的抗氧化及抗炎效果和意义。方法：选取冠心病并且有一定程度的脂代谢紊乱的患者64例,按随机对照原则随机分为A组（32例）及B组（32例）,A组给予血脂康胶囊600mg,日2次;B组予洛伐他汀40mg/d,丙氨酸转氨酶或天冬氨酸转氨酶升高超过正常值3倍以上的患者服用剂量减半,即洛伐他汀20mg/d,经治疗或者观察恢复正常后再加到40mg/d。共比8周,检测实验前后的血浆ALT,AST,CK,OX-LDL,CRP及SOD水平。结果：血脂康胶囊可以明显的降低血浆TG,CHOL,LDL水平,并且与对照组差异有显著性意义（P〈0.05）。血脂康胶囊可以明显的降低血浆OX-LD,CRP水平,与对照组差异有非常显著性意义（P〈0.01）,血脂康胶囊可以提高血浆SOD水平优于对照组（P〈0.01）,而升高ALT,AST,CK的副作用较对照组低（P〈0.05）。结论：血脂康胶囊常规剂量不仅有效调脂而安全,并且有一定的抗氧化及抗炎效果。     

Anti-inflammatory,Antioxidant and Analgesic Amides

The synthesis of some new aryl acetic acids and amides and a pharmacochemical study and quantitative structure-activity relationships (QSAR) on them are described. The compounds were screened for their biological activity using the carrageenin induced rat paw oedema model and a significant inhibition of oedema occurred (44.1–80.1%) at a concentration of 0.01?mmol/1?kg. The analgesic activity, based on the inhibition of acetic acid-induced writhing in rats was also found to be significant. The compounds were found to interact with the stable free radical 1,1-diphenyl-hydrazyl DPPH and with DMSO (for hydroxyl radicals). The compounds were screened for radical scavenging activity with the xanthine/xanthine oxidase system for O₂^-? and for inhibition of soybean lipoxygenase (LOX). The results are discussed in terms of the structural and physicochemical characteristics of the compounds.     

血脂康胶囊对冠心病患者的抗氧化及抗炎效果研究

目的:探讨血脂康胶囊对冠心病患者的抗氧化及抗炎效果和意义。方法:选取冠心病并且有一定程度的脂代谢紊乱的患者64例,按随机对照原则随机分为A组(32例)及B组(32例),A组给予血脂康胶囊600mg,日2次;B组予洛伐他汀40mg/d,丙氨酸转氨酶或天冬氨酸转氨酶升高超过正常值3倍以上的患者服用剂量减半,即洛伐他汀20mg/d,经治疗或者观察恢复正常后再加到40mg/d。共比8周,检测实验前后的血浆ALT,AST,CK,OX-LDL,CRP及SOD水平。结果:血脂康胶囊可以明显的降低血浆TG,CHOL,LDL水平,并且与对照组差异有显著性意义(P<0.05)。血脂康胶囊可以明显的降低血浆OX-LD,CRP水平,与对照组差异有非常显著性意义(P<0.01),血脂康胶囊可以提高血浆SOD水平优于对照组(P<0.01),而升高ALT,AST,CK的副作用较对照组低(P<0.05)。结论:血脂康胶囊常规剂量不仅有效调脂而安全,并且有一定的抗氧化及抗炎效果。