芪防鼻敏颗粒抗炎、抗过敏作用研究

摘 要 目的：初步探讨中药复方芪防鼻敏颗粒的抗炎、抗过敏作用。方法: 采用二甲苯致小鼠耳廓肿胀法和大鼠棉球肉芽组织形成法观察芪防鼻敏颗粒的抗炎作用,采用大鼠同种被动皮肤过敏反应实验和小鼠耳异种被动皮肤过敏反应观察芪防鼻敏感颗粒的抗过敏作用。结果: 与空白组比较,芪防鼻敏颗粒各剂量组可显著降低二甲苯所致小鼠耳廓肿胀度（P<0.01或0.05）,对大鼠棉球肉芽组织增生无明显抑制作用。与空白组比较,芪防鼻敏颗粒各剂量组可明显降低卵蛋白所致大鼠皮肤蓝斑A值（P<0.01或0.05）,芪防鼻敏颗粒高剂量组可显著降低小鼠耳廓蓝染程度（P<0.05）。结论:芪防鼻敏颗粒具有一定抗炎、抗过敏作用。     

活犀角与犀角抗炎作用的比较研究

摘 要 目的：比较活犀角与犀角的抗炎作用有无显著差异,为活犀角替代犀角提供实验依据。 方法: 通过大鼠足跖肿胀法和小鼠棉球肉芽肿法、耳廓肿胀法、腹腔染料通透法研究活犀角和犀角的抗炎作用。 结果: 与模型对照组比较,活犀角的高（440 mg·kg^-1）、中（220 mg·kg^-1）剂量组和犀角3个剂量组各时间点的足跖肿胀度差异有统计学意义（P＜0.05或P＜0.01）;活犀角和犀角的高（700 mg·kg^-1）、中（350 mg·kg^-1）剂量组能显著降低小鼠棉球肉芽肿的重量（P＜0.05）;活犀角和犀角3个剂量组（700,350,175 mg·kg^-1）均能明显降低二甲苯引起的小鼠耳廓肿胀（P＜0.05或P＜0.01）;犀角中（350 mg·kg^-1）剂量组,活犀角高（700 mg·kg^-1）、中（350 mg·kg^-1）剂量组的腹腔清洗液中伊文思兰的吸光度值显著降低（P＜0.05或P＜0.01）。活犀角与犀角相同剂量组间抗炎作用比较无显著差异。 结论: 活犀角与犀角均具有一定抗炎作用,本研究为活犀角在抗炎作用方面作为犀角的替代品进行使用提供了实验依据。     

银蒿解热合剂抗炎镇痛解热及岗梅解热作用研究

摘 要 目的：探讨银蒿解热合剂的抗炎、镇痛、解热作用及其主药岗梅的解热作用。方法: 通过小鼠毛细血管通透性实验、二甲苯致小鼠耳廓肿胀实验及大鼠棉球肉芽肿实验,观察银蒿解热合剂的抗炎作用;采用小鼠扭体实验和热板法观察该合剂的镇痛作用;以干酵母致大鼠发热模型,研究银蒿解热合剂及其主药岗梅的解热作用。结果:银蒿解热合剂能明显抑制小鼠腹腔内炎性物质的渗出(P<0.05),对二甲苯致耳廓肿胀均有明显的抑制作用, 对肉芽组织增生有抑制作用;能明显提高大鼠的痛阈值,尤其是对干酵母所致发热有显著的抑制作用(P<0.05)。在抗炎、镇痛和解热实验中,银蒿解热合剂中、高剂量组与吲哚美辛组比较,无显著差异（P>0.05）。在解热实验中,岗梅高剂量组,自6h起与吲哚美辛组无显著差异（P>0.05）,表明主药岗梅解热作用亦较为显著。结论:以岗梅为主药的银蒿解热合剂具有很好的抗炎、解热、镇痛作用,主药岗梅有一定抗炎、镇痛作用,且其解热作用较为显著。     

柴葛解肌处方抗炎活性部位筛选

摘 要 目的： 筛选柴葛解肌处方的抗炎活性部位。方法: 采用昆明种小鼠,以二甲苯致小鼠耳廓肿胀实验和角叉菜胶致小鼠足趾肿胀实验考察柴葛解肌处方不同部位的抗炎作用以及对PGE₂含量的影响。结果: 柴葛解肌处方乙酸乙酯和正丁醇部位对小鼠耳廓肿胀以及小鼠足趾肿胀有显著抑制作用,正丁醇部位在0.8 ·kg^-1时对小鼠肿胀耳廓抑制率为51.9%,对小鼠足趾肿胀抑制率为37.45%（P<0.01）,且其PGE₂含量显著减少（P<0.01）。结论:柴葛解肌处方正丁醇部位为其主要抗炎部位,能抑制小鼠耳廓和足趾肿胀,减少PGE₂含量。     

草豆蔻挥发油的抗炎作用研究

目的 研究草豆蔻挥发油的抗炎作用.方法 构建二甲苯致小鼠耳肿胀、醋酸致小鼠腹腔毛细血管通透性增加、棉球诱发大鼠肉芽肿及角叉菜胶致大鼠足跖肿胀炎症模型,将草豆蔻挥发油高、中、低剂量组炎症模型鼠的疗效与空白对照组、阳性对照组(地塞米松)相比较,观察草豆蔻挥发油对不同炎症模型的抗炎作用.结果 与空白对照组及阳性对照组相比,高、中剂量草豆蔻挥发油能够降低小鼠毛细血管通透性,并抑制二甲苯致小鼠耳肿胀,减轻大鼠肉芽肿,其中高剂量草豆蔻挥发油(100mg/kg)的抗炎作用与地塞米松组相当.结论 草豆蔻挥发油具有明显的抗炎作用.     

金克痤胶囊的药效学研究

目的:研究金克痤胶囊的药效学。方法:采用角叉菜胶复制小鼠足跖肿胀、大鼠棉球肉芽肿模型,观察金克痤胶囊的抗炎作用;采用组胺诱导法观察金克痤胶囊对皮肤毛细血管通透性的影响;通过复制丙酸杆菌致大鼠耳廓痤疮炎症模型观察金克痤胶囊对丙酸杆菌致痤疮炎症的影响。结果:金克痤胶囊对角叉菜胶致小鼠足趾肿胀有显著的抑制作用(P<0.01);能抑制大鼠棉球肉芽肿,抑制率为34.3%～44.5%;可降低由组胺诱导的皮肤毛细血管通透性;可显著降低丙酸杆菌引起的耳廓炎症痤疮大鼠的耳廓肿胀率(P<0.01)。结论:金克痤胶囊具有较好的抗炎作用,且对丙酸杆菌所致的寻常痤疮有显著的治疗作用。     

毛冬青口服液抗炎作用实验研究

目的 研究毛冬青口服液的抗炎作用.方法 用二甲苯致小鼠耳廓肿胀、蛋清致大鼠足跖肿胀、醋酸至小鼠腹腔毛细血管通透性增加及大鼠棉球肉芽肿等动物实验模型研究其抗炎作用.结果 毛冬青口服液对二甲苯致小鼠耳廓肿胀、蛋清致大鼠足跖肿胀、醋酸致小鼠腹腔毛细血管通透性增加及大鼠棉球肉芽肿等均有显著的抑制作用.结论 毛冬青口服液具有明显的抗炎作用.     

扁桃酸的镇痛抗炎作用研究

摘 要 目的：观察扁桃酸的镇痛、抗炎作用。方法: 50只昆明种SPF级小鼠随机分为5组：空白对照组（生理盐水,0.1 ml/10 g）、扁桃酸高（300 mg·kg^-1）、中（200 mg·kg^-1）、低（140 mg·kg^-1）剂量组、阿司匹林阳性对照组,ig,qd。采用小鼠扭体法和热板法观察扁桃酸的镇痛作用。采用二甲苯涂耳致小鼠急性耳肿胀观察其抗炎作用。结果: 扁桃酸各剂量组均能使小鼠扭体次数明显减少,痛阈延长,与空白对照组比较差异有统计学意义（P＜0.01）。扁桃酸高剂量组的小鼠扭体次数少于阳性对照组,差异无统计学意义（P＞0.05）,扁桃酸中、低剂量组的小鼠扭体次数多于阳性对照组,其中低剂量组差异有统计学意义（P＜0.05）; 扁桃酸各剂量组用药前后小鼠的痛阈提高率均比阳性对照组高,其中高剂量组用药前后痛阈增加明显,与阳性对照组差异有统计学意义（P＜0.05）。扁桃酸各剂量组对小鼠耳肿胀的影响无显著作用,与空白对照组比较差异无统计学意义（P＞0.05）。结论: 扁桃酸具有显著的镇痛作用,抗炎作用不明显。     

柴葛清热颗粒抗炎镇痛解热作用研究

摘 要 目的： 研究柴葛清热颗粒的抗炎、镇痛、解热作用。方法: 采用昆明种小鼠,以二甲苯致小鼠耳廓肿胀法对柴葛清热颗粒进行抗炎作用评价;以醋酸致小鼠扭体法对柴葛清热颗粒进行镇痛作用评价;采用酵母对Wistar大鼠致热法测定柴葛清热颗粒的解热作用。结果: 柴葛清热颗粒对小鼠耳廓肿胀有显著抑制作用,高剂量时其抑制率为46.3%;柴葛清热颗粒中、高剂量组对小鼠疼痛有显著缓解作用,抑制率分别为51.1%,61.8%;大鼠体温上升1 h,柴葛清热颗粒低中高剂量组即对其体温有显著降低作用,高剂量组对发热大鼠降温达0.56℃。结论: 柴葛清热颗粒能抑制小鼠耳廓肿胀,缓解小鼠疼痛,降低高热大鼠体温。     

姜黄素衍生物FM0807体内抗炎作用研究

目的研究姜黄素衍生物FM0807的体内抗炎作用;方法通过建立二甲苯致小鼠耳廓肿胀、角叉菜胶致小鼠足跖肿胀、棉球植人法诱发慢性肉芽肿等炎症模型,探讨姜黄素衍生物FM0807的体内抗炎作用;结果姜黄素衍生物FM0807高、中、低各剂量对二甲苯致小鼠耳廓肿胀、角叉菜胶致小鼠足跖肿胀、棉球植人法诱发慢性肉芽肿均有明显的抑制作用;结论姜黄素衍生物FM0807对急、慢性炎症有明显的效果。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.