The effect of papaverine on acute opiate withdrawal in guinea pig ileum

In the present work the effect of papaverine, a non specific smooth muscle relaxant, was investigated on the naloxone-precipitated withdrawal contracture of the acute morphine-dependent guinea-pig ileum in vitro. Furthermore, the effect of papaverine was also considered on DAGO (highly selective mu -agonist) and U50-488H (highly selective k-agonist) withdrawal to test whether the possible interaction of papaverine on opioid withdrawal involves mu - and/or k-opioid receptors. Following a 4 min in vitro exposure to opioid agonist, the guinea-pig isolated ileum exhibited a strong contracture after the addition of naloxone. Papaverine treatment (1 x 10(-7) - 5 x 10(-7) - 1 x 10(-6) M) before or after the opioid agonists was able of both preventing and reversing the naloxone-induced contracture after exposure to mu (morphine and DAGO) or k (U50-488H) opiate agonists in a concentration-dependent fascion. Both acetylcholine response and electrical stimulation were not affected by papaverine treatment whereas the final opiate withdrawal was still reduced. The results of the present study indicate that papaverine was able to produce significative influence on the opiate withdrawal in vitro and papaverine was able to exert its effect both at mu and k opioid agonists.     

川芎嗪对吗啡依赖离体豚鼠回肠戒断收缩的影响

目的观察中药川芎的主要成分川芎嗪对吗啡依赖离体豚鼠回肠催促戒断反应的影响,评价川芎嗪对吗啡依赖豚鼠回肠的作用。方法采用豚鼠回肠体外孵育方法。催促戒断收缩由1μmol/L纳络酮加入已在含3μmol/L吗啡的37.5℃Krebs液中孵育4 h的离体豚鼠回肠引起。分别在给予纳络酮前、后1 min加入不同浓度的盐酸川芎嗪,观察豚鼠回肠的收缩反应。结果川芎嗪100,200,300μmol/L对正常回肠收缩未见明显影响。当川芎嗪100,200,300μmol/L在加入纳洛酮前1 min给药,纳洛酮催促的回肠戒断性收缩被明显抑制,与吗啡依赖对照组相比较有显著性差异(P<0.05或P<0.01)。川芎嗪200,300μmol/L在加入纳洛酮后1 min给药,对戒断性收缩也有明显抑制作用。结论川芎嗪对纳洛酮催促的吗啡依赖豚鼠离体回肠戒断性收缩的形成有抑制作用,对已出现的戒断收缩也有明显阻断作用。提示川芎嗪具有抑制吗啡戒断症状的作用。     

Relaxant activity of raspberry (Rubus idaeus) leaf extract in guinea-pig ileum in vitro

Tea made from the leaves of Rubus idaeus L. (raspberry) has been used for centuries as a folk medicine to treat wounds, diarrhoea, colic pain and as a uterine relaxant. Extracts of dried raspberry leaves prepared with different solvents, (n-hexane, ethyl acetate, chloroform and methanol) were tested in vitro for relaxant activity on transmurally stimulated guinea-pig ileum. The methanol (MeOH) extract exhibited the largest response and also indicated that the active compounds are of a relatively polar nature. Hence the bulk of the leaves were extracted with methanol and the dried extract fractionated on a silica gel column, eluting with chloroform, mixtures of chloroform and methanol and finally methanol. Each fraction was examined by thin layer chromatography and tested for relaxant activity in an in vitro transmurally stimulated guinea-pig ileum preparation. The fractions eluted with chloroform (CHCl(3)) lacked relaxant activity. Samples eluted with CHCl(3)/MeOH (95:5) had moderate relaxant activity, while a second distinctive peak of activity eluted with a more polar solvent mixture (CHCl(3)/MeOH 50:50) provided strong dose dependent responses. Evidence was obtained that there are at least two components of raspberry leaf extract which exhibit relaxant activity in an in vitro gastrointestinal preparation.     

生姜不同提取方法的比较及其醇提物稳定性研究

目的:探讨生姜的提取方法及其提取物的稳定性。方法:分别采用4种方法制备生姜的提取物,采用HPLC测定提取物中6-姜酚的含量。并考察光照,加热,酸碱以及氧化条件对提取物中成分的影响。结果:微波辅助萃取法,超声法,渗漉法和回流法4种方法比较,各种方法提取得到成分的相对含量有变化,微波辅助提取物各个成分含量相对较高且提取时间最短,提取物不耐热、酸碱并易氧化。结论:微波辅助提取法为较佳的提取方法。     

Bioassay-guided isolation and identification of antifungal compounds from ginger

A bioassay-guided isolation of antifungal compounds from an African land race of ginger, Zingiber officinale Roscoe, led to the identification of [6], [8] and [10]-gingerols and [6]-gingerdiol as the main antifungal principles. The compounds were active against 13 human pathogens at concentrations of <1 mg/mL. The gingerol content of the African land race was at least 3 x higher than that of typical commercial cultivars of ginger. Therefore, ginger extracts standardized on the basis of the identified compounds, could be considered as antifungal agents for practical therapy.     

Spasmolytic activity of Toddalia asiatica Var. floribunda

The spasmolytic activity of the aerial parts of Toddalia asiatica var. floribunda (family Rutaceae) was evaluated. The ethanol extract exhibited significant spasmolytic activity and was then partitioned into five fractions. The activity was found to be concentrated only in the hexane and chloroform fractions. This activity was shown not to be due to the coumarins, toddalolactone and toddanone, as was previously thought.     

Gastrointestinal stimulant effect of Urginea indica Kunth. and involvement of muscarinic receptors

Urginea indica Kunth. (Family; Liliaceae) was studied for its gastrointestinal stimulant effect to rationalize the traditional medicinal uses as a digestive aid, stomachic and laxative. The crude aqueous-methanol extract of Urginea indica bulb (Ui.Cr) was tested on mice and isolated gut preparations. Ui.Cr, which was tested positive for alkaloids, tannins and coumarins, increased faecal output and accelerated charcoal meal transit in mice (6-12 mg/kg, p.o.), similar to that caused by carbachol (10 mg/kg). Ui.Cr (0.01-1 mg/mL) caused a spasmogenic effect in guinea-pig ileum that was reproduced in rabbit jejunum (0.01-0.3 mg/mL) followed by relaxation at a higher concentration. Like carbachol, the stimulant effect of Ui.Cr was blocked by atropine, suggesting the activation of muscarinic receptors mediating the prokinetic effect. Ui.Cr (0.01-5.0 mg/mL) also inhibited K(+) (80 mm)-induced contraction in rabbit jejunum and shifted the Ca(2+) concentration-response curves to the right, similar to verapamil, a standard calcium channel blocker. These data, indicating the presence of a gastrointestinal stimulant effect in Urginea indica possibly mediated through a cholinergic mechanism, provide a rationale for the use of Urginea indica in indigestion and constipation. The presence of a calcium antagonist effect in the plant may help to alleviate untoward effects of the plant that may result from an excessive increase in gut motility.     

丹参滴注液及其组分致豚鼠过敏反应的实验研究

目的:采用豚鼠过敏试验研究丹参滴注液及其组分的致敏性,为改进该药,提高临床用药安全性提供参考。方法:采用全身主动过敏试验方法,豚鼠腹腔注射各组受试药物以致敏,致敏期间每日观察动物状态。在末次致敏后的第11天用致敏量的2倍量进行激发,观察激发前15 min及激发后40 min豚鼠反应,评价动物反应症状。激发后40 min采血制备血清,ELISA检测血清IgE,组胺含量,并结合反应症状结果综合评价药物致敏性。结果:各组豚鼠致敏期间无异常反应,激发后综合判定致敏性,丹参滴注液、丹参精制液为可疑,辅料组为阴性。结论:丹参滴注液在除去大分子成分后,其余成分仍可能导致机体出现过敏反应。     

Coleonema album: studies of the pharmacological action on smooth muscle in vitro and antimicrobial action of its essential oil

The mode of action of the essential oil of Coleonema album, a South African species from the Cape region, was studied on smooth muscle in vitro using field-stimulated guinea-pig ileum. The oil produced an initial spasmogenic activity followed by spasmolysis, both actions being dose-dependent. The spasmolytic action was post-synaptic and not atropine-like and was unaffected by the adrenoceptor blockers phentolamine and propranolol. There was no evidence for the involvement of either cyclic guanosine monophosphate or cyclic adenosine monophosphate in the spasmolytic activity. The oil had some calcium channel blocking activity but this is not the primary explanation for its spasmolytic response. Antimicrobial activity against Pseudomonas aeruginosa, Escherichia coli, Staphyloccocus aureus and Saccharomyces cerevisiae was very low and totally absent against Enterococcus hirae, suggesting that the oil has no worthwhile potential in this area. However, as the oil has a very disagreeable odour in its undiluted form, it could be a powerful insect repellent, as its local usage suggests, and this remains to be investigated.     

Studies on spasmogenic and spasmolytic activities of Calendula officinalis flowers

The aqueous-ethanol extract of Calendula officinalis flowers (Co.Cr) was studied for its possible spasmolytic and spasmogenic effects in isolated gut preparations. In rabbit jejunum, Co.Cr caused a dose-dependent (0.03-3.0 mg/mL) relaxation of spontaneous and K+-induced contractions, suggestive of calcium channel blockade (CCB). In a few preparations, a mild non-reproducible spasmogenic effect was observed at lower doses, followed by relaxation. The CCB effect was confirmed when pretreatment of the jejunum preparations with Co.Cr produced a dose-dependent rightward shift in the Ca(++) dose-response curves, similar to that of verapamil. Activity-directed fractionation revealed that the spasmolytic activity of the plant was concentrated in its organic fractions. The aqueous fraction exhibited a marked atropine sensitive spasmogenic effect but was found to be devoid of any spasmolytic effect. These data indicate that the crude extract of Calendula officinalis flowers contains both spasmolytic and spasmogenic constituents, exhibiting these effects through calcium channel blocking and cholinergic activities and this study provides a scientific base for its traditional use in abdominal cramps and constipation.     

隔姜灸配合针刺治疗寒凝血瘀型原发性痛经的疗效分析

目的:观察隔姜灸配合针刺治疗原发性寒凝血瘀型痛经的临床疗效,并进行总结分析。方法:将符合纳入标准的原发性痛经(Primary Dysmenorrhea,PD)患者,随机分为观察组(50例)与对照组(50例)。观察组进行隔姜灸(关元、神阙、气海、双侧子宫)配合针刺(三阴交、合谷、内关)进行治疗,对照组口服双氯酚酸钠肠溶片(北京诺华制药有限公司生产,国药准字H11021640),25 mg/12 h;观察两组有效率、疼痛视觉模拟评分量表(Visual Analogue Scale,VAS)评分、前列腺素(Prostaglandin,PG)F2a、全血粘度及血浆粘度。结果:两组患者评价即时有效率,差异无统计学意义(P>0.05),VAS评分P>0.05;治疗结束后评价近期有效率,差异具有统计学意义(P<0.05),治疗后PGF2a均下降,变化幅度有差异(P<0.05);全血粘度及血浆粘度治疗后对比,P<0.05;随访结束后评价远期有效率,差异具有显著统计学意义(P<0.05),VAS评分,P<0.05。结论:隔姜灸配合针刺治疗寒凝血瘀型原发性痛经获得良好的临床效果,治疗过程安全,可推广应用。     

中药白疕合剂对豚鼠银屑病模型T细胞活化调节作用的实验研究

目的:探讨中药白疕合剂对豚鼠银屑病模型T细胞活化的调节作用。方法:将豚鼠随机分为空白对照组、阴性对照组、白疕合剂低、中、高剂量组、消银颗粒组、阿维A组,采用ELISA法检测白疕合剂治疗后豚鼠银屑病模型血清中IL-2、INF-γ、IL-4、IL-10的水平,免疫组织化学法检测皮肤淋巴细胞相关抗原(CLA)的表达。结果:表明白疕合剂高、中、低剂量组血清中IL-2及INF-γ水平降低,同时IL-4及IL-10在血清中的水平升高,白疕合剂能抑制豚鼠皮损中CLA的表达。结论:中药白疕合剂对豚鼠银屑病模型有较好的治疗作用,其作用机理可能是通过调节T细胞的活化作用来治疗银屑病。     

Modulating effect of ginger extract on rats with ulcerative colitis

ETHNOPHARMACOLOGICAL RELEVANCE: Ginger rhizomes are used traditionally for management of different gastrointestinal disturbances. Several studies proved that the rhizome possesses diverse biological activities such as cytotoxic, antioxidant, and anti-inflammatory effects. Recently, interest in ginger for treatment of chronic inflammatory conditions has been renewed. AIM OF THE STUDY: The purpose of the present study is to evaluate the potential role of ginger extract [GE] in modulating the extent and severity of ulcerative colitis (UC), a chronically recurrent inflammatory bowel disease of unknown origin. MATERIALS AND METHODS: Male Wistar rats received 3 different doses of GE, sulfasalazine, or vehicle for 3 consecutive days before induction of UC by intra-rectal acetic acid administration, and continued further for 7 days after the induction. The colonic mucosal injury was assessed by macroscopic scoring, and histological examination. Furthermore, the mucosal content of malondialdehyde (MDA), protein carbonyl (PCO), and reduced glutathione (GSH) with the catalase (CAT) and superoxide dismutase (SOD) activity, were appraised as parameters of the redox state. Acute inflammatory response was determined by measuring myeloperoxidase (MPO), tumor necrosis factor (TNF-alpha), and prostaglandin E2 (PGE2). RESULTS: All parameters were altered in ulcerated rats, and improved in animals receiving GE, an effect that was comparable to that of the standard sulfasalazine, especially at the highest dose level. Colonic mucosal injury parallels with the histological and biochemical evaluations. CONCLUSIONS: Results showed a valuable effect of ginger extract against acetic acid-induced ulcerative colitis possibly by its antioxidant and anti-inflammatory properties.     

N—去甲基蝙蝠葛碱抗心律失常作用

用哇巴因ｉｖ致豚鼠心律失常、乌头碱ｉｖ致大鼠心律失常、氯化钙－氯化乙酰胆碱ｉｖ致小鼠房颤、电刺激致家兔室颤、大鼠冠脉结扎诱发的心律失常等模型证实Ｎ－去甲基蝙蝠葛碱的具抗房性和室性心律失常作用,其作用剂量依赖性增强。离体试验表明Ｎ－去甲基蝙蝠葛碱浓度依赖性延长豚鼠乳头肌快反应和慢反应动作电位的ＡＰＤ５０、ＡＰＤ９０,降低ＡＰＡ,减慢Ｖｍａｘ。     

不同灸材隔姜灸治疗慢性萎缩性胃炎疗效研究

目的:探讨传统艾条隔姜灸和无烟艾条隔姜灸治疗慢性萎缩性胃炎(CAG)临床疗效及对血清学指标的影响。方法:选取80例CAG患者随机分为试验组和观察组,每组各40例。试验组采用传统艾条隔姜灸,观察组采用无烟灸条隔姜灸。比较两组皮肤温度-时间曲线、中医证候评分、血清学指标。结果:试验组穴位皮肤最高温度低于观察组(P<0.05),试验组最高温度出现时间晚于观察组(P<0.05)。试验组总有效率为75.0%,观察组总有效率为45.0%,试验组总有效率高于观察组(P<0.05)。治疗后,试验组中医证候评分低于观察组(P<0.05)。治疗后,两组GAS水平升高,试验组PGⅠ水平升高(P<0.05)。结论:传统艾条隔姜灸和无烟艾条隔姜灸均可改善CAG患者临床症状及血清学指标,但传统艾条隔姜灸适宜温度刺激时间长于无烟灸条隔姜灸,疗效更好,其机制可能与上调血清胃蛋白酶原及胃泌素水平有关。     

白藜芦醇对豚鼠左心室流出道自律组织电活动的影响

目的:本研究主要通过细胞内微电极技术研究白藜芦醇对豚鼠左心室流出道自律组织的电生理效应。方法:选取体重250～300g豚鼠,应用玻璃微电极技术记录动作电位并观察给药前后动作电位的变化。观察指标:MPD、APA、Vmax、VDD、RPF、APD90。结果:(1)白藜芦醇可抑制左心室流出道自律细胞的电活动,白藜芦醇可显著降低左心室流出道自律细胞的APA、Vmax、VDD、RPF(P<0.01);而对MDP和APD50及APD90无明显作用(30、60μmol/L)。(2)白藜芦醇对L-Ca2 通道的影响,预先应用L-Ca2 开放剂BayK8644灌流标本可取消白藜芦醇对流出道起搏细胞的电生理效应;预先应用L-Ca2 阻断剂Verapamil灌流标本可加强白藜芦醇对流出道起博细胞的电生理效应。结论:白藜芦醇可抑制左心室流出道自律细胞的电活动,这些效应可能与其抑制钙离子内流有关,同时提示白藜芦醇与Verapamil对流出道起搏细胞有相似的抑制Ca2 通道电生理作用。     

“肤敏膏”对湿疹皮炎模型的影响

目的:研究"肤敏膏"对豚鼠湿疹皮炎模型皮肤组织病理学的影响,探讨其治疗作用及机理。方法:以2,4-二硝基氯苯(DNFB)建立豚鼠湿疹皮炎模型,采用HE常规病理及透射电镜超微病理学检测方法,观察"肤敏"膏对实验性豚鼠湿疹皮炎的治疗作用。结果:"肤敏膏"能改善动物湿疹皮炎模型皮肤组织病变,减少炎性细胞浸润。结论:"肤敏膏"对Th1/Th2细胞平衡失调所引起的后续皮肤炎症反应和组织损伤有明显抑制作用,从而间接调节Th1/Th2细胞动态平衡,改善过敏症状。     

基于文献研究的变应性鼻炎豚鼠模型造模评价方法的研讨

目的：对以变应性鼻炎模型豚鼠为研究对象的文献进行分析,总结模型评价方法,寻找最佳的模型评价方法。方法：检索中国医院知识总库（CHKD）,以“变应性鼻炎”和“豚鼠”或“过敏性鼻炎”和“豚鼠”为检索词,检索范围为1979~2013年,对文献中采用的模型评价方法进行分析。结果：检索共得到208篇文献,其中共计51篇文献在造模后描述了模型评价方法,即分别通过行为学积分、鼻黏膜分泌物涂片、被动皮肤过敏试验（PCA）、病理观察等方法评价模型。结论：各种评价方法中,行为学积分评价方法最常用,目前以赵秀杰提出的方法较为可靠,但操作细节无统一标准。在此基础上结合鼻黏膜分泌物涂片、PCA评价模型更肯定,但PCA和病理学观察需增加实验动物数量,不易操作。因此,目前的文献基础尚不能为最佳模型评价方法提供充分支持。     

银屑平颗粒对豚鼠银屑病动物模型的影响

目的:研究银屑平颗粒对豚鼠银屑病模型的影响。方法:采用心得安乳剂涂抹耳造豚鼠银屑病样模型,银屑平高、中、低剂量ig 2周,处死豚鼠,采用ELISA试剂盒检测豚鼠耳匀浆液中肿瘤坏死因子-α(TNF-α)及细胞间黏附因子(ICAM-1)的含量,并观察其对病理形态学的影响。结果:与正常组比较,模型组豚鼠TNF-α及ICAM-1显著升高(P0.05),与模型组比较,银屑平颗粒高、中剂量组、甲氨喋呤组TNF-α及ICAM-1显著降低(P0.01);与模型组比较,银屑平高、中、低剂量组对心得安所致的表皮皮损、红肿,皮肤糜烂,角化不全,毛细血管增生扩张等形态学改变有不同程度的改善。结论:银屑平颗粒对银屑病有良好的治疗作用。     

小儿咳喘宁颗粒对豚鼠过敏性哮喘模型的影响

目的研究小儿咳喘宁颗粒对过敏性哮喘豚鼠的作用。方法用卵蛋白(OVA)复制豚鼠哮喘模型,观察小儿咳喘宁颗粒对模型动物哮喘潜伏期、血清中超氧化物歧化酶(SOD)、丙二醛(MDA)、谷胱甘肽过氧化物酶(GSH-PX)、肺组织病理学的影响。结果小儿咳喘宁颗粒可明显延长哮喘潜伏期(P<0.05,P<0.001)、提高模型豚鼠血清中SOD活性(P<0.05),改善模型动物肺组织病理学改变。结论小儿咳喘宁颗粒对过敏性哮喘模型豚鼠有一定的保护作用。