玉郎伞提取物抗炎作用研究

研究玉郎伞水提物及从玉郎伞中提取纯化的三种活性成份—黄酮、皂苷、多糖的抗炎作用。以巴豆油致炎小鼠耳廓肿胀、角叉菜胶诱发小鼠足跖肿胀及小鼠棉球肉芽肿模型分别观察玉郎伞水提物及三种成份对小鼠耳廓肿胀、足跖肿胀及棉球肉芽肿形成的抑制作用。结果表明,玉郎伞水提物及三种成份可抑制小鼠耳廓炎症、足跖肿胀及棉球肉芽肿的形成。因此,玉郎伞水提物及三种活性成份具有较强的抗炎作用。     

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。     

长春七超临界提取物镇痛、镇静和抗炎作用的研究

研究长春七超临界提取物(SELB)的镇痛、镇静和抗炎作用。镇痛实验采用小鼠热板法和扭体法;镇静实验采用与戊巴比妥钠协同催眠法和小鼠自主活动法;抗炎实验采用大鼠足跖肿胀法和小鼠耳肿胀法。结果显示:SELB高、中、低剂量组均能显著提高热板致痛小鼠的痛阈和醋酸致痛小鼠的扭体抑制率;高、中剂量组与戊巴比妥钠有协同作用,能显著延长小鼠睡眠时间,高、中、低剂量组能显著减少小鼠自主活动次数;高、中剂量组能显著抑制蛋清致大鼠的足跖肿胀率,高、中、低剂量组均能显著抑制二甲苯致小鼠的耳肿胀度。SELB具有的镇痛、镇静和抗炎作用与长春七的功能主治及临床应用相符。     

白花龙胆花抗炎作用研究

为了研究白花龙胆花的抗炎作用,本文对白花龙胆花水提物和70%乙醇提取物的抗炎活性进行了试验,并测定了水提物和70%乙醇提物中龙胆苦苷的含量.试验采用二甲苯所致小鼠急性耳肿胀试验和二甲苯所致小鼠腹部毛细管通透性试验.将昆明种小白鼠分为7组,分别为空白对照组,白花龙胆花水提物高、中、低剂量组和70%乙醇提取物高、中、低剂量组,灌胃(ig)给药14 d后,用二甲苯分别于小鼠右耳及腹部致炎.测定左右耳重量,计算肿胀度及肿胀抑制率,测定吸光值.结果表明:白花龙胆花水提物和乙醇提取物的中、高剂量组对于二甲苯所致的小鼠急性耳肿胀和小鼠腹部毛细管通透性都有显著的抑制作用.从而表明:白花龙胆花具有显著的抗炎疗效.     

CO2超临界萃取金银花挥发油工艺及抗炎活性研究

采用CO2超临界萃取的方法从金银花中提取挥发油,用小鼠耳肿胀模型对其提取物进行抗炎实验。通过正交试验设计CO2超临界萃取得到最佳提取工艺条件是:温度35℃、压力12 MPa,CO2流量4.0 kg/h,时间1.5h,其得率为1.08%,是共水蒸馏法得率的43.2倍。小鼠耳肿胀模型进行抗炎实验表明,无论是局部给药还是灌胃给药CO2-SFE金银花挥发油均有显著抗炎活性。优选得到的工艺简单、稳定、可行且提取物抗炎效果好。     

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。     

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。     

槐角黄酮栓抗炎、止血、抗溃疡作用的实验研究

目的:研究槐角黄酮栓的抗炎、止血、抗溃疡作用。方法:从中药槐角中提取总黄酮,与脂肪酸甘油酯混合后用热融法制成栓剂。采用小鼠耳廓肿胀法、滤纸肉芽肿法、腹腔毛细血管通透性试验和角叉菜胶致大鼠足跖肿胀法观察槐角黄酮栓的抗炎作用;通过玻璃毛细管法和断尾法测定小鼠出、凝血时间,评价槐角黄酮栓的止血效果。复制大鼠直肠损伤模型,直肠给药治疗,观察伤口愈合情况并HE染色,评价槐角黄酮栓的促愈合作用。结果:槐角黄酮栓具有明显的抗炎、抗溃疡作用,并能缩短小鼠出、凝血时间,提高直肠创面愈合率。结论:槐角黄酮栓制备工艺简单,具有较好的抗炎、止血、抗溃疡作用。     

两粤黄檀乙醇提取物化学成分分析及抗炎活性研究

为了研究壮药两粤黄檀的化学成分及其抗炎活性,阐明其药理作用机制,该研究采用小鼠二甲苯致炎耳廓肿胀法、角叉菜胶致炎足肿胀急性炎症模型,观察不同剂量两粤黄檀乙醇提取物对小鼠耳廓肿胀度、肿胀率及足肿胀度的影响,并利用液相色谱-质谱(LC-MS)、热裂解气相色谱-质谱(PY-GC/MS)等技术分析提取物的化学成分,结合网络药理学方法对其抗炎活性成分以及作用机制进行初步研究。结果表明:(1)两粤黄檀乙醇提取物具有良好的抗炎活性,高剂量组(8 g·kg~(-1))可以显著抑制二甲苯致小鼠耳廓肿胀度、角叉菜胶致炎足趾肿胀,其抑制率均高于50%;(2)从两粤黄檀乙醇提取物中共鉴定得到60个化合物,包括毛蕊异黄酮、芒柄花黄素、血根碱、胡椒碱、β-谷甾醇等多种抗炎活性成分;(3)网络药理学分析显示,两粤黄檀发挥抗炎作用的核心靶点为PIK3CA、EGFR、MAPK、SRC、STAT3、CYP19A1、IL2、MAOA等,涉及c GMP-PKG、cAMP、Focal adhesion、Rap1等信号通路。该研究结果为两粤黄檀的进一步开发利用提供了重要参考。     

桔核中柠檬苦素类物质消炎镇痛作用的研究

为探讨柑桔果实中柠檬苦素类物质对实验动物模型的抗炎镇痛作用,本文通过小鼠耳廓肿胀模型和角叉菜胶致大鼠足肿胀模型观察柠檬苦素的抗炎作用;采用小鼠福尔马林实验及扭体实验观察柠檬苦素的镇痛作用。结果表明：柑桔果实中柠檬苦素类物质能显著抑制二甲苯致小鼠耳廓肿胀和角叉菜胶致大鼠足肿胀程度;减少扭体次数;显著提高小鼠福尔马林实验中的痛域。因此,柑桔果实中柠檬苦素类物质对本实验中的动物模型具有显著的抗炎及镇痛作用。     

Design and synthesis of thiourea derivatives containing a benzo[5,6]cyclohepta[1,2-b]pyridine moiety as potential antitumor and anti-inflammatory agents

Thiourea derivatives (6a-e) were developed and screened for antitumor and anti-inflammatory activity. Most of the compounds exhibited growth inhibitory effects comparable to 5-fluorouracil in vitro against mammary (MCF-7 and MDA-MB 231) as well as colon (HT-29) carcinoma cells. They also showed stronger anti-inflammatory activity than ibuprofen in vivo in the xylene-induced ear swelling assay in mice.     

Anti-inflammatory activity of licochalcone A isolated from Glycyrrhiza inflata

Licochalcone A was isolated from the roots of Glycyrrhiza inflata and evaluated for its anti-inflammatory activity in xylene-induced mice ear edema and carrageenan-induced paw edema tests. At the same time, the inhibition of prostaglandin biosynthesis by licochalcone A was also studied in lipopolysaccharide (LPS)-induced mouse macrophage cells. At 5 mg/ ear, licochalcone A showed remarkable effects against acute inflammation induced by xylene, and at the doses of 2.5, 5, 10 mg/kg (p.o.), licochalcone A reduced significantly paw edema induced by carrageenan compared to the control at the fourth hour. Both COX-2 activity and expression were significantly inhibited by licochalcone A at all the test doses. Therefore, licochalcone A could be a useful compound for the development of new anti-inflammatory agents.     

Anti-inflammatory activity of polysaccharide from <Emphasis Type="Italic">Pholiota nameko</Emphasis>

Pholiota nameko polysaccharide (PNPS-1) has been isolated and purified by enzymatic hydrolysis, hot water extraction, ethanol precipitation, and ion-exchange and gel-filtration chromatography. The anti-inflammatory activity of PNPS-1 was evaluated in rodents using xylene-induced ear edema, egg albumin-, carrageenin-, and formaldehyde-induced paw edema, cotton pellet granuloma test, adhesion of peritoneal leukocytes in vitro, and ulcerogenic activity. The results showed that PNPS-1 (5 mg/ear) inhibited topical edema in the mouse ear and at 100, 200, and 400 mg/kg (intraperitoneally) it significantly suppressed the development of egg albumin-, carrageenin-, and formaldehyde-induced paw edema in the animals. PNPS-1 (100, 200, and 400 mg/kg, per oral) significantly inhibited the growth of granuloma tissues induced by subcutaneously implanted cotton pellets in rats by 10.96, 18.07, and 43.75%, respectively. PNPS-1 also inhibited spontaneous and phorbol-12-myristate-13-acetate-activated adhesion of peritoneal leukocytes in vitro. Further, both acute as well as chronic administration of PNPS-1 (100, 200, and 400 mg/kg, per oral) did not produce any gastric lesion in rats. In conclusion, these data indicated that PNPS-1 possesses significant anti-inflammatory activity suggesting its potential as an anti-inflammatory agent for use in the treatment of various inflammatory-related diseases.     

活络效灵丹抗炎镇痛作用的实验研究

目的：研究活络效灵丹的抗炎、镇痛、消肿等药理作用,为该药的临床研究提供基础。方法：用二甲苯致小鼠耳肿胀法和角又莱胶致大鼠足肿胀法研究抗炎作用,用热板法和扭体法研究镇痛作用。结果：活络效灵丹能较好地抑制二甲苯引起的小鼠耳廓炎性肿胀和大鼠甲醛致足跖肿胀,能显著提高热板试验小鼠的痛阈,有效抑制冰醋酸引起的小鼠扭体反应次数。结论：活络效灵丹具有良好的抗炎、镇痛、消肿等作用。     

大血藤醇提物抗炎镇痛和止血活性研究初探

为观察大血藤醇提物抗炎、镇痛、止血活性,该文采用75%乙醇提取制备大血藤醇提物(AESC),利用HPLC法测定其绿原酸含量; KM鼠(或新西兰兔)在测定抗炎、镇痛、止血活性时随机分为空白对照组、阳性对照组(云南白药酊组)、AESC组,依次测定其抑制二甲苯致小鼠耳肿胀度作用、痛阈值和兔肝脏局部创面损伤出血的记分分值,分别考察其抗炎、镇痛、止血作用。结果表明:AESC中绿原酸含量为(0.294±0.013 5)%;与空白组比较,剂量为0.700 g·kg~(-1)的AESC组能显著减轻二甲苯所致的小鼠耳肿胀度(P0.01),抑制率达26.3%;与空白组及给药前比较,剂量为1.40 g·kg~(-1)的AESC组均能显著提高小鼠痛阈值(P0.01);与空白组相比,剂量为1.40 g·kg~(-1)的AESC组能显著提高兔肝脏局部创面损伤出血的记分分值(P0.001)。大血藤醇提取物具有显著的抗炎、镇痛、止血作用,有望将其开发为抗炎、镇痛、止血制剂。该结果也为大血藤的临床应用提供理论依据。     

Synthesis and biological evaluation of novel hydrogen sulfide releasing glycyrrhetic acid derivatives

A series of hybrids, which are composed of glycyrrhetic acid (GA) and slowly hydrogen sulfide-releasing donor ADT-OH, were designed and synthesized to develop anticancer and anti-inflammatory agents. Most of the compounds, whose inhibitory rates were comparable to or higher than those of GA and aspirin, respectively, significantly inhibited xylene-induced ear edema in mice. Especially, compound V₄ exhibited the most potent inhibitory rate of 60.7%. Furthermore, preliminary structure–activity relationship studies demonstrated that 3-substituted GA derivatives had stronger anti-inflammatory activities than the corresponding 3-unsubstituted GA derivatives. In addition, anti-proliferative activities of compounds V_1?9 were evaluated in three different human cancer cell lines. Compound V₄ showed the most high potency against all three tumor cell lines with IC₅₀ values ranging from 10.01?μM in Hep G2 cells to 17.8?μM in MDA-MB-231 cells, which were superior to positive GA.     

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.     

Novel synthesis and anti-inflammatory activities of 2,5-disubstituted-dioxacycloalkanes

A novel stereospecific synthetic route to obtain a series of 2,5-disubstituted-dioxacycloalkanes is reported. Using an in vivo inhibition assay by monitoring xylene-induced ear edema in mice, the structure-activity relationship of the dioxacycloalkane compounds was studied, and compounds possessing high anti-inflammatory activity were identified.     

Toward the development of chemoprevention agents. Part 1: Design, synthesis, and anti-inflammatory activities of a new class of 2,5-disubstituted-dioxacycloalkanes

A new class of 2,5-disubstituted-dioxacycloalkanes were designed and synthesized via stereoselective synthetic method as cancer chemoprevention agents. The anti-inflammatory activities of these compounds were tested using the xylene-induced mouse ear edema model. Some of these compounds exhibited comparable or better anti-inflammatory activities than that of aspirin suggesting that they can be further developed as potential anti-inflammatory drug lead compounds. In addition, treatment of these anti-inflammatory agents did not prolong tail bleeding time in mice. The structure/activity relationships were also analyzed among these compounds.