虎参痛风丸在小鼠的镇痛作用

目的：探讨虎参痛风丸的镇痛效果及急性毒性。方法：分别观察虎参痛风丸高、中、低三个剂量组对小鼠冰醋酸所致的扭体反应、热板法致病的影响。观察最大浓度药液对小鼠的急性毒性反应。结果：虎参痛风丸能显抑制小鼠冰醋酸所致的扭体反应、减轻热板刺激所致的疼痛；虎参痛风丸无明显急性毒性反应。结论：虎参痛风丸有明显的镇痛作用又无明显的急性毒性反应。     

虎参痛风胶囊对大鼠足肿的抗炎作用

目的:研究虎参痛风胶囊的抗炎效果及对足肿胀组织前列腺素E2(PGE2)含量的影响.方法:分别观察虎参痛风胶囊500,250,125 mg·kg-13个剂量组对蛋清所致的大鼠足肿胀的影响.同时测定肿胀的足组织中PGE2的含量.结果:虎参痛风胶囊能显著抑制蛋清所致的大鼠足肿胀程度,减少肿胀的足组织中PGE2的含量.结论:虎参痛风胶囊有明显的抗炎作用.其抗痛风的机制部分是通过减少PGE2的产生和聚集来实现的.     

溃结康胶囊的抗炎作用机制

目的:研究渍结康胶囊的抗炎作用及其可能的机制.方法:通过小鼠耳肿胀、大鼠角叉菜胶足跖肿胀、大鼠棉球肉芽肿等实验观察其抗炎作用,并测定小鼠足爪中前列腺素E2(PGE2)、丙二醛(MDA)的含量.结果:溃结康胶囊能明显抑制二甲苯所致的小鼠耳肿胀,角叉菜胶所致大鼠足跖肿胀以及棉球肉芽肿的增生,并减少PGE2、MDA在炎症组织中的产生;对摘除肾上腺的小鼠亦可抑制二甲苯所致的耳肿胀.结论:溃结康胶囊具有一定的抗炎作用,其作用与抑制PGE2合成及脂质过氧化有关.     

苜蓿提取物抗炎镇痛作用的实验研究

目的研究苜蓿提取物抗炎镇痛的药理作用。方法应用二甲苯引起的小鼠耳肿胀,角叉菜胶致大鼠足趾肿胀、棉球所致大鼠肉芽组织增生、醋酸致小鼠扭体反应,及热水缩尾法疼痛模型观察了苜蓿提取物对炎症及疼痛反应的影响。结果苜蓿提取物可显著抑制二甲苯引起小鼠耳肿胀度,抑制率分别为78.72%、67.70%、46.03%;显著抑制角叉菜胶所致大鼠足肿胀,第6小时高、中、低剂量组的抑制率分别为47.86%、37.40%、34.84%;高、中剂量苜蓿提取物可明显抑制棉球致大鼠肉芽组织增生,其抑制率分别为32.26%、20.80%;对醋酸诱发的小鼠扭体反应有明显的抑制作用,其抑制率分别为65.99%、73.6%、55.84%;高、中剂量苜蓿提取物可延长热水引起疼痛的潜伏期,其延长率分别为51.55%、36.49%。结论苜蓿提取物具有明显的抗炎和镇痛作用。     

NO偶联双氯芬酸衍生物抗炎、镇痛、解热作用实验研究

目的：考察NO偶联双氯芬酸衍生物(澳通，CO-3)的抗炎、镇痛、解热作用。方法：通过小鼠耳二甲苯致炎、角叉菜胶致大鼠足跖肿胀、大鼠棉球肉芽肿及Ⅱ型胶原所致的大鼠关节炎等实验模型，观察CO-3的抗炎作用；通过小鼠醋酸扭体、热板刺激和大鼠甩尾等实验模型，观察CO-3的镇痛作用；通过大鼠啤酒酵母致热实验模型，观察CO-3的解热作用。结果：CO-3可明显抑制二甲苯所致小鼠耳肿胀、角叉菜胶致大鼠足跖肿胀、大鼠棉球肉芽组织增生及Ⅱ型胶原所致的大鼠关节炎；能显著抑制醋酸引起的小鼠扭体反应及提高甩尾及热板刺激的致痛阈值；对啤酒酵母致热大鼠有明显的解热作用。结论：CO-3具有良好的抗炎、镇痛、解热作用。     

感通颗粒抗感冒作用的实验研究

目的：观察感通颗粒对鼠非特异性炎症及免疫性炎症和解热止痛作用影响。方法：采用小鼠耳壳炎症模型、大鼠足肿胀和棉球肉芽组织增生模型观察抗炎作用，另外观察小鼠非特异性免疫功能及解热镇痛作用。结果：感通颗粒能抑制小鼠二甲苯所致小鼠耳壳炎症和角叉菜胶所致的大鼠足肿胀，减轻大鼠棉球肉芽组织的重量，提高小鼠对碳末廓清指数和吞噬指数，并具有解热止痛、增强机体免疫力的功能。结论：感通颗粒具有明显的消炎和抗感冒作用。     

红藤汤提取液抗炎作用初步试验研究

目的初步观察红藤汤提取液的抗炎作用。方法采用小鼠二甲苯耳肿胀实验、大鼠塑料环肉芽组织增生实验观察红藤汤提取液的抗炎作用。结果红藤汤提取液能明显抑制二甲苯所致的小鼠耳肿胀、塑料环引起的肉芽组织增生。结论红藤汤提取液具有明显的抗炎作用,与对照组相比有明显差异。     

祛风活络丸抗炎镇痛作用的实验研究

目的:观察祛风活络丸的抗炎、镇痛作用.方法:采用二甲苯致小鼠耳廓肿胀、大鼠棉球肉芽肿、小鼠热板与醋酸扭体等方法评价祛风活络丸的抗炎、镇痛作用.结果:祛风活络丸对二甲苯致小鼠耳廓肿胀、醋酸诱发的小鼠腹腔毛细血管通透性增加、大鼠棉球致肉芽组织增生均有显著的抑制作用,能显著降低大鼠角叉菜胶性足跖炎症组织内PGE2含量与胸腔渗出液中白细胞计数,并能明显提高小鼠化学刺激和热刺激所致疼痛的痛阈值.结论:祛风活络丸具有较好的抗炎、镇痛作用.     

马钱子总生物碱对实验性关节炎的影响

目的:观察马钱子总生物碱及士的宁对实验性关节炎的影响.方法:从马钱子中提取生物碱并进一步分离出番木鳖碱(士的宁)、总生物碱(除去部分士的宁)、非生物碱3个部分,观察各部分对角叉菜胶引起的大鼠足肿胀及棉球致肉芽组织增生的影响.结果:总生物碱部分能明显抑制大鼠足肿胀,第4,5,6小时抑制率分别为19.76%,30.02%,36.89%;明显抑制大鼠肉芽组织增生,抑制率37.60%,士的宁及非生物碱部分对上述炎症无明显影响.结论:总生物碱具有抗炎作用,强毒性成分士的宁为无效成分.     

齐墩果酸的抗炎作用

OLA对不同致炎剂引起的大鼠足垫肿胀、二甲苯所致小鼠耳廓肿胀及乙酸引起的小鼠腹腔毛细血管通透性增高均有明显抑制作用.OLA使大鼠炎性组织释放的PGE量减少,抑制大鼠棉球肉芽组织增生,同时伴有肾上腺增重及胸腺缩小.     

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.

---

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.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

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.