小金胶囊抗炎、镇痛作用药效学试验

目的:考察小金胶囊在抗炎及镇痛方面的药效作用。方法:抗炎作用采用小鼠耳肿胀法、大鼠踝关节肿胀法,镇痛作用采用小鼠甲醛致痛法及醋酸扭体法。结果:小金胶囊对二甲苯所致的小鼠耳炎具有明显的抑制作用,可抑制角叉菜胶所致的大鼠踝关节肿胀,对甲醛所致的小鼠足疼痛具有抑制作用,并可减少醋酸引起的小鼠扭体次数。结论:小金胶囊具有明显的抗炎及镇痛作用。     

复方独活寄生合剂抗炎、镇痛作用观察

目的：观察复方独活寄生合剂抗炎、镇痛作用。方法：分别采用蛋清致大鼠足跖肿胀法、二甲苯致小鼠耳廓肿胀法观察抗炎作用，采用小鼠醋酸扭体法、热板法观察药物的镇痛作用。结果：复方独活寄生合剂对蛋清所致大鼠足跖肿胀及二甲苯引起的小鼠耳廓肿胀均有明显抑制作用，且能显著减少醋酸所引起的小鼠扭体反应次数，延长小鼠热板法引起的痛反应潜伏期。结论：复方独活寄生合剂具有抗炎、镇痛作用。     

胆乐胶囊的抗炎与镇痛作用研究

目的：研究胆乐胶囊的抗炎与镇痛作用。方法：采用蛋清致大鼠足跖肿胀，二甲苯致小鼠耳肿胀，醋酸致小鼠毛细血管通透性增加和扭体进行抗炎镇痛作用研究。结果：胆乐胶囊能明显抑制蛋清致大鼠足跖肿胀和二甲苯致小鼠耳肿胀，并能明显抑制醋酸致小鼠毛细血管通透性增加和扭体数。结论：胆乐胶囊具有较好的抗炎与镇痛作用。     

复方威灵仙合剂抗炎、镇痛作用观察

目的：观察复方威灵仙合剂抗炎、镇痛作用。方法：分别采用小鼠醋酸扭体法、热板法观察药物的镇痛作用,蛋清致大鼠足跖肿胀法、二甲苯致小鼠耳廓肿胀法观察抗炎作用。结果：复方威灵仙合剂能明显减少小鼠醋酸所引起的扭体反应数,延长小鼠热板法引起的痛反应潜伏期．对大鼠蛋清所致足跖肿胀及二甲苯引起的小鼠耳廓肿账均有明显的抑制作用。结论：复方威灵仙合剂具有抗炎,镇痛作用．     

牛黄解毒滴丸解热镇痛和抗炎作用实验

目的：观察牛黄解毒滴丸的解热镇痛和抗炎作用。方法：采用2,4-二硝基酚大鼠致热法观察其解热作用;小鼠扭体法、热板刺激法观察其镇痛作用;小鼠耳部肿胀法、大鼠蛋清足肿胀法观察其抗炎作用。结果：牛黄解毒滴丸显著降低2,4-二硝基酚所致大鼠升高的体温;明显减轻和抑制热板所致的小鼠疼痛及醋酸所致的小鼠扭体反应;抑制二甲苯所致的小鼠耳肿胀和蛋清所致的大鼠足肿胀。结论：牛黄解毒滴丸对实验大鼠、小鼠具有良好的解热、镇痛和抗炎作用。     

骨质增生膏抗炎镇痛实验研究

目的：验证骨质增生膏有显的抗炎镇痛作用。为其临床应用提供了一定的药效学依据。方法：用骨质增生膏水煎液，腹腔注射昆明种小鼠；涂大鼠踝关节处。结果：骨质增生膏显提高小鼠热板法痛阈和抑制醋酸诱发的小鼠扭体反应，明显抑制蛋清所致大鼠踝关节肿胀及抑制巴豆油混合致炎液所致的小鼠耳壳炎症，结论：骨质增生膏有显的抗炎镇痛作用。     

接骨丹胶囊的抗炎镇痛作用

目的：评价接骨丹胶囊的抗炎镇痛作用。方法：用二甲苯致小鼠耳肿胀、鸡蛋清致大鼠足爪肿胀及大鼠肉芽肿炎症模型,考察接骨丹胶囊的抗炎作用;用小鼠醋酸扭体法和热板法,观察接骨丹胶囊的镇痛作用。结果：接骨丹胶囊灌胃给药。可明显减轻小鼠耳肿胀度,降低鸡蛋清致大鼠足爪肿胀,抑制大鼠肉芽肿;对小鼠醋酸扭体和热板反应均呈剂量相关性镇痛作用。结论：接骨丹胶囊对急慢性炎症反应均有明显的抑制作用,对热和化学刺激引起的疼痛反应有明显的镇痛作用。     

愈伤灵膏的抗炎镇痛作用

目的研究愈伤灵膏的抗炎镇痛作用。方法采用血管通透性实验、小鼠耳肿胀实验、大鼠角叉菜胶性足跖肿胀实验、小鼠光热法及醋酸所致小鼠扭体反应等炎症、疼痛模型考察愈伤灵膏的抗炎镇痛作用。结果愈伤灵膏可明显抑制烫伤部位毛细血管通透性 ;对角叉菜胶致大鼠足肿胀和二甲苯致小鼠耳肿胀有明显的抑制作用 ;对光热致小鼠足部疼痛、醋酸致小鼠扭体均有明显的镇痛效果。结论愈伤灵膏具有明显的抗炎、镇痛药效     

胆乐胶囊的抗炎与镇痛作用研究

目的　研究胆乐胶囊的抗炎与镇痛作用。方法　采用蛋清致大鼠足跖肿胀,二甲苯致小鼠耳肿胀,醋酸致小鼠毛细血管通透性增加和扭体进行抗炎镇痛作用研究。结果　胆乐胶囊能明显抑制蛋清致大鼠足跖肿胀和二甲苯致小鼠耳肿胀,并能明显抑制醋酸致小鼠毛细血管通透性增加和扭体数。结论　胆乐胶囊具有较好的抗炎与镇痛作用。     

桑枝虎杖汤抗炎、镇痛作用观察

目的：观察桑枝虎杖汤抗炎、镇痛作用。方法：采用蛋清致大鼠足跖肿胀法、小鼠热板法观察药物的镇痛作用。结果：桑枝虎杖汤对蛋清所致大鼠足跖肿胀有明显抑制作用,能显著减少醋酸所引起的小鼠扭体反应次数,延长小鼠热板法引起的痛反应潜伏期。结论：桑枝虎杖汤具有抗炎、镇痛作用。     

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.     

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.     

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.