辛苍鼻舒胶囊抗炎有效部位的初步观察

目的:初步观察辛苍鼻舒胶囊抗炎作用的有效部位.方法:采用蛋清致小鼠足跖肿胀、醋酸致小鼠腹腔毛细血管炎症、棉球肉芽肿实验,观察辛苍鼻舒胶囊的水提物、挥发油、醇提物的抗炎作用.结果:辛苍鼻舒胶囊中的挥发油、水提物、醇提物分别对蛋清所致小鼠足跖肿胀具有消肿作用,对醋酸致小鼠腹腔毛细血管炎症的急性炎症模型有显著抑制作用,且为醇提物＞挥发油＞水提物;对棉球肉芽肿均有抑制作用,且醇提物＞水提物＞挥发油.结论:辛苍鼻舒胶囊醇提物为抗炎最有效部位.     

白蚁菌圃抗炎机制的研究

目的 探讨白蚁菌圃抗炎的作用机制。方法 采用角叉菜胶致正常及切除双侧肾上腺小鼠足肿胀;角叉菜胶致大鼠胸膜炎;蛋清致小鼠足肿胀的炎症模型。分别用酶联免疫吸附法、紫外分光光度法和荧光分光光度法测炎性渗出液中白三烯(LTB4)、前列腺(PGE2)、5-羟色胺(5-HT)及组胺的水平。结果 角叉菜胶致正常组及去肾上腺组小鼠足肿胀炎症组织及血清中PGE2含量与阴性对照组比有显著性差异;在蛋清致足肿胀中的组胺和5-羟色胺的含量与阴性对照组比有显著性差异;在角叉菜胶致胸膜炎大鼠胸腔渗出液中白三烯含量与阴性对照组比有显著性差异。结论 白蚁菌圃的抗炎作用可能与其抑制炎症部位PGE2、LTB4、5-HT及组胺的水平有关,其抗炎作用不依赖下丘脑-垂体-肾上腺皮质系统的调节。     

白蚁菌圃抗炎机制的研究

目的 探讨白蚁菌圃抗炎的作用机制。方法 采用角叉菜胶致正常及切除双侧肾上腺小鼠足肿胀;角叉菜胶致大鼠胸膜炎;蛋清致小鼠足肿胀的炎症模型。分别用酶联免疫吸附法、紫外分光光度法和荧光分光光度法测炎性渗出液中白三烯(LTB4)、前列腺(PGE2)、5-羟色胺(5-HT)及组胺的水平。结果 角叉菜胶致正常组及去肾上腺组小鼠足肿胀炎症组织及血清中PGE2含量与阴性对照组比有显著性差异;在蛋清致足肿胀中的组胺和5-羟色胺的含量与阴性对照组比有显著性差异;在角叉菜胶致胸膜炎大鼠胸腔渗出液中白三烯含量与阴性对照组比有显著性差异。结论 白蚁菌圃的抗炎作用可能与其抑制炎症部位PGE2、LTB4、5-HT及组胺的水平有关,其抗炎作用不依赖下丘脑-垂体-肾上腺皮质系统的调节。     

鹅不食草挥发油抗炎作用及机制研究

目的:研究鹅不食草挥发油的抗炎作用及其可能的机制。方法:采用小鼠棉球肉芽肿、蛋清致大鼠足肿胀模型,结合荧光分光技术,观察鹅不食草挥发油对急、慢性炎症及炎症介质的影响。结果:鹅不食草挥发油对小鼠棉球肉芽肿和蛋清致大鼠足肿胀均有明显的抑制作用,能明显减少大鼠炎症组织中组胺的含量。结论:鹅不食草挥发油对急、慢性炎症有明显的抑制作用,其机理与抑制炎症介质组胺和5-羟色胺的释放有关。     

糯米藤提取物镇痛抗炎作用

目的 探讨糯米藤水提和醇提取物的镇痛抗炎作用。方法 采用电热板和乙酸致扭体疼痛模型,考察糯米藤水提和醇提取物的镇痛作用;采用二甲苯均匀涂抹引发小鼠耳肿胀和蛋清注射足跖引发大鼠足跖肿胀的炎症模型,考察糯米藤水提和醇提取物的抗炎作用。结果 低、高剂量组糯米藤水提和醇提取物给药后,对电热板诱导的小鼠痛阈值显著提高,对乙酸诱发的扭体反应次数明显减少,相较于健康对照组、自身用药前差异有统计学意义（P<0.01）;对二甲苯涂抹引发的小鼠耳肿胀以及蛋清引发的大鼠足跖肿有明显抑制作用,与健康对照组比较差异有统计学意义（P<0.01）;在镇痛及抗炎方面,糯米藤醇提取物作用明显比水提取物强（P<0.05,P<0.01）。结论 糯米藤水提和醇提取物均具镇痛抗炎作用,且醇提取物作用明显较水提取物强。     

马鞭草醇提液的抗炎作用与组胺、5-羟色胺的关系

目的观察马鞭草醇提液的抗炎作用与组胺、5-羟色胺的关系方法用二甲苯致小鼠耳廓肿胀,通过放免法测定耳廓组织中组胺和5-羟色胺的含量。结果马鞭草醇提液能显著降低小鼠耳廓组织中组胺、5-羟色胺的含量。结论马鞭草醇提液的抗炎作用可能与其抑制组胺、5-羟色胺的合成与释放有关。     

律草醇提液的抗炎作用研究

目的　探讨律草醇提液抗急性炎症的作用 ,为临床用药提供依据。方法　采用二甲苯致小鼠耳肿胀法 ,蛋清致小鼠足跖肿胀法及伊文思蓝法等抗炎实验模型考察律草醇提液的抗炎作用。结果　对二甲苯致小鼠耳肿胀、蛋清致小鼠足跖肿胀及醋酸致小鼠腹腔毛细管通透性增加等均有显著的抑制作用。结论　提示律草醇提液有显著的抗炎作用     

半边莲不同提取物镇痛抗炎作用

目的研究半边莲不同溶剂提取物的镇痛抗炎作用。方法制备半边莲水提取物和75%乙醇提取物,采用醋酸扭体实验和热板实验测定半边莲提取物镇痛作用,二甲苯致小鼠耳廓肿胀实验和10%蛋清致小鼠足跖肿胀实验测定半边莲提取物抗炎作用。结果半边莲水提取物可明显抑制醋酸所致小鼠扭体反应（P＜0.01）;给予半边莲水提取物和醇提取物1,2 h,小鼠热板痛阈值明显提高（P＜0.05或P＜0.01）;半边莲提取物能抑制二甲苯所致小鼠耳廓肿胀（P＜0.05或P＜0.01）;半边莲提取物在致炎后0.5,1,2,4 h能显著抑制10%蛋清所致小鼠足跖肿胀（P＜0.05或P＜0.01）。结论半边莲提取物有明显的镇痛和抗炎作用。     

三叶青藤醇提物的镇痛抗炎作用

目的:研究三叶青藤醇提物的镇痛及抗炎作用。方法:采用小鼠热水缩尾法和醋酸扭体法观察镇痛作用;采用二甲苯致小鼠耳肿胀、角叉菜胶诱导大鼠足肿胀的试验模型观察抗炎作用;并测定角叉菜胶诱导大鼠足肿胀炎性渗出液中前列腺素E2(PGE2)的含量。结果:三叶青藤醇提物能明显提高小鼠的痛阈值,但未能减少小鼠的扭体次数。同时,三叶青藤醇提物能显著减轻小鼠耳肿胀和大鼠足爪肿胀反应,能明显减少大鼠角叉菜胶性炎症渗出液中PGE2含量。结论:三叶青藤醇提物没有明确的镇痛作用,但有显著的抗炎作用,其机制可能与抑制PGE2的合成有关。     

复方鱼腥草胶囊抗炎作用及机制实验研究

目的研究复方鱼腥草胶囊 (FYC)的抗炎作用并探讨其作用机制。方法采用组胺致大鼠皮肤渗透性增高模型、蛋清足肿胀模型研究FYC的抗炎作用 ,同时采用去双侧肾上腺小鼠耳肿胀模型 ,测定大鼠肾上腺中Vc含量及小鼠炎性渗出物中PGE2 、MDA含量研究FYC的抗炎机制。结果FYC可显著降低组胺所致的皮肤通透性增高 ,减轻蛋清足肿胀 ,使肾上腺中Vc含量降低 ,对去肾上腺小鼠不拮抗二甲苯所致小鼠耳肿胀 ,降低炎性渗出物中PGE2 和MDA含量。结论FYC具有明显抗炎作用 ,其机制可能与激动下丘脑 垂体 肾上腺轴 ,减少PGE2 和MDA含量增加有关     

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.