Phytochemical constituents,analgesic and anti-inflammatory effects of methanol extract of Triumfetta rhomboidea leaves in animal models

Objective:To investigate the analgesic and anti-inflammatory effects of the methanolic extract of the leaves of Triumfetta rhomboidea on mice and rats respectively.And to screen the phytochemical constituent of the extract. Methods:The analgesic effect was determined by acetic acid-induced writhing test in mice.While the anti-inflammatory activity was determined by egg albumin-induced oedema of the rat paw.Phytochemical screening was done by standard procedures.Results:Triumfetta rhomboidea leaf extract(50 -400 mg/kg) caused a statistically significant inhibition on the egg albumin-induced eodema or inflammation in Wister albino rats with P【0.001(ANOVA).This effect was higher than the observed effect with Piroxicam(0.5 mg/kg) which was used as a standard.The effect was also dose-dependent.Furthermore,Triumfetta rhomboidea extract caused a statistically significant reduction in the number of acetic acid-induced writhing in mice,with P【0.001(ANOVA).These effects were also does-dependent and greater than the analgesic effects by paracetamol which was used as a reference drug.Phytochemical screening revealed the presence of flavonoids,steroids, triterpenoids alkaloids,tannins and saponins in Truimfetta rhomboidea leaf extract.Conclusion:Triumfetta rhomboidea can be recommended for acute inflammatory disorders and diseases associated with pains.This also supports its traditional use as an anti-snake bite and anti-cancer or anti-tumor agent.Further study is on the way to find out the mechanism of its action and also to isolate,identify and characterize the active principle responsible for these effects in this plant.

Anti-inflammatory and analgesic activities with gastroprotective effect of semi-purified fractions and isolation of pure compounds from Mediterranean gorgonian Eunicella singularis

Objective: To explore anti-inflammatory activities of organic extract and its semi-purified fractions(ethanol, acetone, methanol/dichloromethane) from the Mediterranean gorgonian Eunicella singularis. Methods: The anti-inflammatory and analgesic activities were evaluated, using the carrageenan-induced rat paw edema model and the acetic acid writhing test in mice. The gastroprotective activity was determined using HCl/Et OH induced gastric ulcers in rats. The purification and structure elucidation of compound(s) from the more effective fraction were determined by chromatographic and spectroscopic methods and in comparison with data reported in the literature. Results: The fraction F-Et OH showed an important antiinflammatory activity associated with significant analgesic and gastroprotective properties. The purification and structure elucidation of compound(s) from this fraction lead to the identification of one diterpenoid and four sterols. Conclusions: These results suggested that components from the active fraction can be used to treat various anti-inflammatory diseases.

A Preliminary Study on Anti-inflammatory and Analgesic Effects of Millettia speciosa and Tinpspora sinensis and Their Compatibility

[Objectives]To study the anti-inflammatory and analgesic effects of Millettia speciosa and Tinpspora sinensis and their compatibility.[Methods](i)In the glacial acetic acid writhing experiment,60 SPF-grade Kunming mice were adopted,and the mice were randomly divided into 6 groups at male-female ratio of 1∶1,namely,the blank control group,M.speciosa group,T.sinensis group,M.speciosa compatible with T.sinensis group at the ratio of 1∶2(expressed as 1∶2 compatibility group),M.speciosa compatible with T.sinensis group at the ratio of 1∶1(expressed as 1∶1 compatibility group),and M.speciosa compatible with T.sinensis group at the ratio of 2∶1(expressed as 2∶1 compatibility group),12 mice for each group.Mice of the experimental groups were administered at a dose of 20 mL/kg,and the corresponding concentration of the Chinese medicine extract was given at 1 g/mL.The control group was administered with an equal volume of 0.9%physiological saline,and was intragastrically administered once every 24 h for 14 d.After intragastric administration for one hour on day 14,intraperitoneal injection of 0.5%glacial acetic acid solution was performed to induce pain.(ii)In the hot plate experiment,60 Kunming female SPF mice were adopted,grouped,intragastrically administered with the same glacial acetic acid writhing experiment for 14 d.After intragastric administration for one hour on day 14,the mice were placed on a hot plate apparatus at(55±0.5)℃.to measure the time of licking their hind feet.(iii)In the anti-inflammatory experiment,60 Kunming SPF mice were adopted,grouped,intragastrically administered with the same glacial acetic acid writhing experiment for 14 d.After intragastric administration for one hour on day 14,xylylene was administered to the left ears of mice at a dose of 50μL/piece to induce inflammation.[Results](i)In the glacial acetic acid writhing experiment,compared with the blank control group,the experimental group showed analgesic effects.Specifically,M.speciosa group,T.sinensis group,1∶2 compatibility group,1∶1 compatibility group,2∶1 compatibility group showed significant effect(P<0.05),the writhing inhibition rate was 17.65%,20.59%,29.41%,26.47%,and 44.12%,respectively,and 2∶1 compatibility group showed the most significant analgesic effects.(ii)In the hot plate experiment,compared with the control group,all experimental groups showed analgesic effect.Specifically,M.speciosa group,T.sinensis group,1∶2 compatibility group,1∶1 compatibility group,2∶1 compatibility group showed significant effect(P<0.05),the pain threshold improvement rates were 16.13%,14.55%,14.96%,29.95%,and 58.68%,respectively,and 2∶1 compatibility group showed the most significant analgesic effect.(iii)In the anti-inflammatory experiment,the swelling degree of the 1∶2 compatibility group was significantly different from that of the blank control group,M.speciosa group,T.sinensis group(P<0.05).and 1∶2 compatibility group showed the most significant anti-inflammatory effect.[Conclusions]M.speciosa,T.sinensis,and their compatibility had anti-inflammatory and analgesic effects.The 2∶1 compatibility group had the best analgesic effects,and 1∶2 compatibility group had the best anti-inflammatory effects.

Screening of Anti-inflammatory and Analgesic Parts of Ardisia gigantifolia stapf.and Its Toxicological Safety Study

[Objectives] To screen out the anti-inflammatory and analgesic parts of Ardisia gigantifolia stapf.and to explore the toxicological safety of each part.[Methods]The carrageenan-induced toe swelling experiment of mice,acetic acid-induced peritoneal capillary permeability experiment,pain writhing test,and mouse maximum tolerated dose experiment were carried out.Taking mouse toe swelling,capillary permeability,pain writhing reaction times,and animal death number as indicators,anti-inflammatory and analgesic effects were screened and toxicological safety was evaluated for petroleum ether,ethyl acetate,n-butanol and water parts of A.gigantifolia.[Results] The petroleum ether part of A.gigantifolia can significantly reduce the degree of carrageenan-induced toe swelling of(P < 0.05),significantly inhibit the glacial acetic acid induced capillary permeability of mice(P < 0.05) and the times of pain writhing of mice(P < 0.01),no death was observed in each group after 150-fold of clinical equivalent dose administration,and no abnormality was observed in body weight and tissues of mice.[Conclusions]The petroleum ether part of A.gigantifolia is active part of anti-inflammatory and analgesic effect,and each part is low in toxicological safety.

Design, Synthesis and Pharmacological Evaluation of New Nonsteroidal Anti-Inflammatory Derived from 3-Aminobenzothieno[2,3-<i>d</i>]pyrimidines

During the last few years, condensed thienopyrimidine derivatives have received considerable attention. The therapeutic importance of thienopyrimidines prompted us to synthesize some of spiro(benzothieno[2,3-d]pyrimidine-4-one) derivatives. Some of the novel benzothino-pyrimidine derivatives 3a, 9b, 10b, 11a, 11b, and 11c showed considerable potent anti-inflammatory and analgesic activity of superior G.I.T. safety profile in experimental rats in comparing to indomethacin and tramadol as reference drugs.

髋关节囊周围神经阻滞与髂筋膜间隙阻滞对老年股骨粗隆间骨折患者镇痛效果的对比研究

目的 探讨髋关节囊周围神经(pericapsular nerve group, PENG)阻滞与髂筋膜间隙阻滞(fascia iliaca compartment block, FICB)对老年股骨粗隆间骨折(intertrochanteric femur fracture, IFF)患者股骨近端防旋髓内钉(proximal femoral nail anti-rotation, PFNA)内固定术的镇痛效果。方法 选取2022年1—12月首都医科大学附属北京积水潭医院老年IFF患者60例,随机分为P组和F组,每组各30例。P组采用PENG阻滞,F组采用FICB。两组患者均接受椎管内麻醉进行手术,术后均给予患者静脉自控镇痛(patient controlled intravenous analgesia, PCIA)。比较两组患者不同时点(T1,神经阻滞前;T2,神经阻滞后30 min;T3,术后6 h;T4,术后24 h;T5,术后48 h)静息和运动时的视觉模拟评分(visual analogue score, VAS)、术后补救镇痛率、镇痛满意度评分、住院时间、PCIA按压次数及不良反应发生率。结果 60例患者中,男23例,女37例,年龄65~85岁,平均(70.6±6.0)岁。两组T2~T5时点静息和运动时VAS均低于T1时点,差异均有统计学意义(P <0.05);两组静息和运动时所有时点VAS、术后补救镇痛率、镇痛满意度评分、住院时间、PCIA按压次数及不良反应发生率的比较,差异均无统计学意义(P>0.05)。结论 PENG阻滞与FICB均可缓解老年IFF患者PFNA内固定术的镇痛,且镇痛效果相当。

归芪活血胶囊对神经根型颈椎病大鼠炎性损伤和微循环血流的影响

目的:探究归芪活血胶囊(GQ)对神经根型颈椎病(CSR)大鼠的治疗效应及机制。方法:观察CSR大鼠自发痛、热痛阈、步态评分、前肢和颈部体表微循环状态、脊髓病理结构及超微结构变化、脊髓p38磷酸化情况以及血清白细胞介素-1β(IL-1β)、IL-6以及肿瘤坏死因子-α(TNF-α)。结果:GQ高、中剂量在干预第14天时可显著升高CSR模型大鼠的热痛阈(P<0.05),降低其步态评分和自发痛评分(P<0.05,P<0.01);GQ各剂量均可改善CSR大鼠脊髓炎症水肿变化,显著增加尼氏(Nissl)染色阳性细胞数目(P<0.05),恢复髓鞘和线粒体正常形态,且GQ中剂量效果较明显;GQ高、中剂量可显著升高CSR大鼠颈部和前肢皮肤血流灌注量(P<0.05),对前肢远端血流灌注量的改善程度优于芬必得组(P<0.01);与模型组比较,GQ中剂量可降低CSR大鼠脊髓p38磷酸化比率。结论:GQ可以缓解CSR大鼠热痛觉过敏和步态不稳的程度,改善脊髓炎症病理变化,恢复前肢和颈部体表血流灌注量,且GQ中剂量在改善CSR大鼠炎症损伤方面更有优势。

逆乌茜草水煎液抗炎、镇痛和止泻作用研究

为了确证逆乌茜草水煎液的抗炎作用、镇痛作用、止泻作用,按照试验设计将210只昆明小鼠随机分组,逆乌茜草水煎液组分别灌胃低剂量(0.3033 g/kg)、中剂量(0.9100 g/kg)、高剂量(2.7300 g/kg)的逆乌茜草水煎液,同时每个试验设立模型对照组和阳性对照组。分别采用二甲苯致小鼠耳肿胀法、醋酸致小鼠疼痛扭体法、炭末推进测定法和粪便含水量称重法对逆乌茜草水煎液进行抗炎、镇痛、涩肠和止泻作用研究。结果表明,与模型组比较,逆乌茜草水煎液中剂量组二甲苯引起的耳廓肿胀率极显著降低(P<0.01),表明逆乌茜草水煎液具有良好的抗炎作用,并能延长醋酸致小鼠疼痛扭体潜伏期,但作用不显著,中剂量组、高剂量组小鼠疼痛扭体次数显著减少(P<0.05或P<0.01),且随药物剂量增大,小鼠疼痛扭体抑制率明显升高,表明逆乌茜草水煎液具有显著的镇痛作用;低剂量组、中剂量组、高剂量组逆乌茜草水煎液能抑制炭末在小鼠小肠内的推动,说明逆乌茜草水煎液具有一定的涩肠作用;与空白对照组比较,给药3 d,逆乌茜草水煎液低剂量组、中剂量组、高剂量组和阳性对照组小鼠粪便中含水量无显著性差异(P>0.05),表明逆乌茜草水煎液具有良好的止泻作用。综上,逆乌茜草水煎液具有显著的抗炎作用、镇痛作用和止泻作用,且具有一定的涩肠作用,可作为犊牛腹泻潜在的候选治疗药物进行研究开发。

外周神经免疫互作在针刺抗炎镇痛中的作用

炎症是一种常见的生理反应,适度的炎症反应可以保护机体,对维持机体健康具有重要意义,但过度的炎症反应则会引起炎性痛,给患者造成伤害,如何安全有效地减轻炎性痛是当今医学研究的热点。针刺作为传统中医的一种治疗手段,拥有显著的抗炎镇痛疗效,同时兼具安全无副作用的特点。自主神经介导了针刺的抗炎效应,针刺通过调节迷走神经和交感神经的活性,影响儿茶酚胺在内的多种神经递质释放,影响神经递质与免疫细胞上的受体结合,通过调节免疫细胞影响炎症反应;针刺也能够影响镇痛物质的水平及其受体表达,镇痛物质不仅参与疼痛信息的产生及传递过程,也可以调控免疫细胞的活化,影响促炎介质的水平。神经、免疫系统及其相互作用参与了炎性痛的产生过程,针刺通过外周神经免疫互作发挥抗炎镇痛效应,在临床上可作为一种安全有效的减轻炎性痛的方法。

自热型熥敷中药镇痛抗炎作用评价及皮肤用药安全性观察

目的考察自热型熥敷中药的有效性及安全性。方法大鼠醋酸扭体实验:将70只SD大鼠根据体质量分为正常对照组、模型对照组、双氯芬酸二乙胺乳胶剂组(0.125 g/次,0.5 h)、传统熥敷中药组(12.42 g/kg,0.5 h)、自热型熥敷中药A(3.06 g/kg,0.5 h)、B(3.06 g/kg,3 h)、C(3.06 g/kg,6 h)组,通过注射醋酸建立大鼠疼痛模型,记录30 min内大鼠扭体的次数和潜伏期,考察自热型熥敷中药镇痛疗效以及与传统熥敷中药对比的疗效差异性;大鼠炎症模型实验:选取20只SD大鼠作为正常对照组和假手术组,60只大鼠腹股沟植入棉球建立炎症模型按体质量随机分为模型对照组、双氯芬酸二乙胺乳胶剂组、传统熥敷中药、自热型熥敷中药A、B、C组(给药剂量、时长同醋酸扭体实验),考察自热型熥敷中药抗炎疗效以及与传统熥敷中药对比的疗效差异性;实验兔皮肤刺激性实验:将8只实验兔分为皮肤完整组以及皮肤受损组,各4只,在左、右两侧分别贴上自热型熥敷中药包及去除药的自热型熥敷中药包。每次6 h,连续使用7 d,在自然光下肉眼观察并记录去除药物后1、24、48 h和72 h敷贴部位有无红斑和水肿等情况;豚鼠斑贴实验:将40只背部经去毛处理无损伤的豚鼠,分为阴性对照组(去除药的自热型熥敷中药包)、阳性对照组(1-氯-2,4-二硝基苯)、供试品组(自热型熥敷中药)。致敏阶段:在第0 d、第7 d和第14 d,观察豚鼠背部左侧给药6 h后1 h、24 h是否出现皮肤刺激性反应,末次致敏14 d后,观察豚鼠右侧给药6 h后24 h、48 h是否出现皮肤刺激性反应。结果自热型熥敷中药B、C组大鼠扭体次数与模型对照组比较,差异有统计学意义(P=0.016、=0.007);传统熥敷中药组与自热型熥敷中药A组大鼠扭体次数比较,差异有统计学意义(P=0.029);双氯芬酸二乙胺组潜伏期与模型对照组比较,差异有统计学意义(P=0.008);自热型熥敷中药C组肉芽肿重量与模型对照组比较,差异有统计学意义(P=0.016)。自热型熥敷中药对皮肤无刺激、无致敏性。结论自热型熥敷中药是具有明显镇痛抗炎作用且安全性较高的新制剂。

民族药水河剑水提和醇提取物急性毒性试验及抗炎镇痛有效部位筛选

对水河剑(Diplazium lanceum)药材水提物及醇提物的急性毒性进行初步研究,并筛选水河剑药材具有抗炎镇痛效果的极性部位。使用最大给药量测定方法对小鼠灌胃给药,得到水河剑水提物及醇提物的最大耐受量(MTD),考察水河剑用药的安全性;采用小鼠醋酸扭体及热板法考察水河剑不同极性部位的镇痛效果;采用小鼠耳肿胀法考察水河剑药材不同极性部位的抗炎效果;用ELISA法,测乙酸乙酯提取物(高、中、低)对小鼠耳部二甲苯致炎血清中炎症因子含量的影响。结果表明,水河剑水提物及醇提物急性毒性试验中均未能得到半数致死量(LD_(50)),水河剑药材水提物和醇提取物最大耐受量分别为238.0、165.2 g/kg;水河剑药材不同极性部位提取物对小鼠的舔足时间都有所延长;水河剑药材不同极性部位均对小鼠扭体有抑制效果,各组镇痛率为11.14%~40.36%,其中镇痛效果最好的为乙酸乙酯部位,其次为石油醚部位;水河剑药材不同部位均对小鼠耳肿胀有抑制效果,各组耳肿胀抑制率为24.71%~48.47%,乙酸乙酯及石油醚部位抗炎效果最好;乙酸乙酯高、中、低剂量组小鼠血清中肿瘤坏死因子(TNF-α)、白介素-1β(IL-1β)、前列腺素E_(2)(PGE_(2))炎症因子含量与模型对照组相比均有所下降,乙酸乙酯低、中剂量组的IL-1β、PGE_(2)含量及乙酸乙酯低剂量组的TNF-α含量与模型对照组相比具有显著差异。

紫藤根及含紫藤根经验方的初步药效研究

目的:探讨紫藤根及含紫藤根经验方的抗炎、镇痛作用及其药效动力学规律。方法:通过小鼠棉球肉芽肿炎症实验研究紫藤根及含紫藤根经验方的慢性增生性抗炎作用,同时通过小鼠扭体实验探索紫藤根及含紫藤根习用经验方的镇痛作用。结果:紫藤根及含紫藤根经验方3个剂量组均能不同程度地抑制肉芽的生长,对于棉球肉芽肿所引起的慢性炎症有抑制作用;同时,此方各剂量组均有极显著的镇痛作用。结论:验证了紫藤根及含紫藤根经验方的抗炎、镇痛效果,同时诠释了其经验方所占配伍比例偏少会使整个经验方的抗炎、镇痛效果更好,此研究能为紫藤根的质量标准与临床应用提供参考。

地瓜子醇提物镇痛抗炎镇咳活性及急性毒性研究

目的:观察地瓜子醇提物的镇痛、抗炎、镇咳作用及急性毒性研究。方法:采用小鼠醋酸扭体法、小鼠二甲苯耳廓肿胀试验、小鼠氨水致咳试验以及急性毒性试验。结果:地瓜子醇提物能减少醋酸所致的小鼠扭体反应次数,降低二甲苯所致小鼠耳廓肿胀度,能减少浓氨水致小鼠咳嗽次数。地瓜子醇提物24 h内小鼠灌胃给药LD_(50)为0.61 g/kg·bw(相当于生药8.05 g/kg·bw)。结论:地瓜子醇提物具有明显的镇痛、抗炎、镇咳作用但有毒。

8种建昌帮法栀子炮制品解热、抗炎、镇痛、止血药效比较

目的:研究比较8种建昌帮法栀子炮制品解热、抗炎、镇痛、止血药效作用。方法:分别复制家兔内毒素发热模型、小鼠耳廓二甲苯炎症模型、小鼠醋酸扭体疼痛模型。灌胃给予8种建昌帮法栀子炮制品,测定家兔体温、小鼠耳廓肿胀度及抑制率、小鼠扭体反应次数及抑制率;测定小鼠凝血时间。在各组间进行统计比较。结果:8种建昌帮法栀子炮制品对内毒素所致发热模型家兔均有解热作用(P<0.01;P<0.05),生栀子的解热作用强于炒栀子、姜栀子和焦栀子;生栀仁的解热作用强于生栀皮(P<0.05);炒栀仁的解热作用强于炒栀皮(P<0.05)。8种栀子炮制品对二甲苯致小鼠耳廓炎症均有抑制作用(P<0.01),各栀子炮制品组之间未见显著差异。8种栀子炮制品对醋酸致小鼠扭体反应均有抑制作用(P<0.01;P<0.05),炒栀子、姜栀子和焦栀子的镇痛作用强于生栀子(P<0.05)。焦栀子可明显缩短小鼠凝血时间(P<0.01),其他7种栀子炮制品无此作用。结论:8种建昌帮法栀子炮制品的解热、抗炎、镇痛、止血药效作用存在差异,临床应注意选择使用。

产地加工与炮制一体化工艺对玄参质量的影响

目的比较产地加工与炮制一体化加工工艺和传统加工方法对玄参质量的影响。方法用硅胶G薄层板对不同玄参进行定性鉴别;对不同玄参浸出物、灰分、水分以及多糖、哈巴苷、哈巴俄苷、桃叶珊瑚苷、安格洛苷C、毛蕊花糖苷、肉桂酸的含量进行测定;用二甲苯诱导小鼠进行耳廓肿胀和醋酸扭体实验,研究不同玄参的镇痛抗炎作用。结果2种玄参的鉴别项和检查项均符合2020年版《中华人民共和国药典》相关规定;一体化玄参的多糖、桃叶珊瑚苷、肉桂酸含量高于传统玄参;与空白组比较,2种玄参饮片均具有镇痛抗炎的效果,药效间的差异无统计学意义。结论一体化玄参的质量评价和功效均与传统玄参相似,值得推广应用。

栀子苷镇痛和抗炎作用的研究

目的研究栀子苷的镇痛和抗炎作用。方法小鼠热板实验,醋酸诱发小鼠扭体反应实验,栀子苷对二甲苯致小鼠耳肿胀实验,栀子苷对醋酸诱发小鼠毛细血管通透性实验,栀子苷对角叉菜胶致小鼠足肿胀实验等。结果栀子苷25mg/kg剂量(P<0.05)能延长热刺激所致小鼠痛觉反应时间,栀子苷50 mg/kg剂量组和12.5 mg/kg剂量组对醋酸诱发小鼠扭体反应有明显的抑制作用(P<0.05),最大扭体次数减少百分率可达55%,具有一定的镇痛作用;栀子苷12.5mg/kg剂量组(P<0.05)和25 mg/kg剂量组(P<0.01)对二甲苯致小鼠耳肿胀均有明显的抑制作用,栀子苷大剂量(50mg/溶液kg)组能导致腹腔毛细血管渗透液的吸光值显著降低(P<0.01),即对急性炎症渗出有较明显的抑制作用;栀子苷对角叉菜胶致小鼠足肿胀没有明显抗炎作用,炎症渗出液中PGE2的含量与对照组比较无明显差异,其抗炎作用可能与PGE2释放没有关系。结论栀子苷有一定的镇痛和抗炎作用。

冰片抗炎镇痛作用的实验研究

目的研究冰片的镇痛、抗炎作用。方法采用热板刺激、冰醋酸刺激小鼠扭体、冰醋酸致小鼠腹腔毛细血管通透性增加、角叉菜胶致大鼠足肿胀等方法研究冰片的镇痛及抗炎作用。结果冰片能明显抑制大鼠足跖肿胀度,其半数有效量(ED50)=0.3242g·kg-1;延长小鼠疼痛反应时间,ED50=0.3870g·kg-1;减少小鼠扭体次数,ED50=0.5813g·kg-1。同剂量条件下,冰片的镇痛效应比抗炎效应更为明显。结论冰片具有显著的镇痛、抗炎作用。

益母草镇痛抗炎作用的实验研究

目的研究益母草的镇痛、抗炎作用。方法以阿司匹林为阳性对照,采用小鼠热板法和化学刺激法观察益母草的镇痛作用,采用二甲苯致小鼠耳廓肿胀法和角叉菜胶致大鼠足跖肿胀模型观察益母草的抗炎作用。结果益母草(60g和90 g生药.kg-1,ig)及阿司匹林均能延长小鼠对热刺激疼痛反应潜伏期,使小鼠10,20m in内扭体次数减少,并明显减轻二甲苯所致的小鼠耳廓肿胀和角叉菜致大鼠足跖肿胀,与生理盐水组比较有显著性差异(P<0.05),镇痛及抗炎作用强度与阿司匹林相近或稍弱。结论益母草具有明显的镇痛抗炎作用。

苯基呋咱氮氧化物与双氯芬酸偶联化合物的合成及其抗炎镇痛活性

目的 寻找能增强双氯芬酸 (DC)抗炎镇痛活性 ,又能降低其胃肠道副作用的一氧化氮供体型DC(NO DC)。方法 以酯键将NO供体 3 羟甲基 4 苯基 呋咱氮氧化物及其异构体与DC偶联 ,考察偶联物的抗炎镇痛活性及胃肠道毒副反应 ,研究偶联物体内外的NO释放作用。结果 合成了 15个新化合物 ,其中目标物 (II1～ 9) 9个 ,其结构经IR ,1 HNMR ,MS和元素分析确证。II3和II9的抗炎活性与DC相当 ,II2 的抗炎镇痛活性强于DC ,胃肠道副作用小于DC ,并小于文献报道的硝酸酯类NO DC ,体内有明显的NO释放。结论 II2 值得深入研究。

合成鱼腥草素的抗炎镇痛作用

合成鱼腥草素灌胃给药对巴豆油致小鼠耳肿胀、角叉菜胶致大鼠足肿胀、醋酸致小鼠腹腔毛细血管通透性增高均有显著抑制作用．同时灌胃给药可以抑制醋酸所致的小鼠扭体反应，延长热痛反应潜伏期。