痛风方剂颗粒镇痛抗炎作用的实验研究

目的:观察痛风方剂颗粒的镇痛、抗炎作用。方法:采用小鼠冰醋酸扭体法和热板法,小鼠二甲苯耳廓肿胀法和角叉菜胶大鼠足跖肿胀法观察痛风方剂颗粒的镇痛、抗炎作用。结果:痛风方剂颗粒对热板所致的小鼠疼痛和醋酸所致的小鼠扭体反应均有显著抑制作用;并能对抗二甲苯所致的小鼠耳廓肿胀和角叉菜胶所致的大鼠足跖肿胀。结论:痛风方剂颗粒具有镇痛、抗炎作用。     

丙酰基青藤碱的镇痛抗炎作用研究

目的：考察丙酰基青藤碱的镇痛抗炎作用。方法：采用小鼠扭体法、小鼠热板法、小鼠耳肿胀法和大鼠足跖胀法等实验模型观察。结果：丙酰基青藤碱可抑制冰醋酸致小鼠疼痛的作用,提高小鼠热板痛阈值,抑制由二甲苯引起的小鼠耳肿,对角叉菜所致的足肿胀也有抑制作用。结论：丙酰基青藤碱具有镇痛抗炎作用,且呈量效关系。     

健胃康颗粒剂抗炎镇痛作用的研究

目的观察健胃康颗粒剂的抗炎、镇痛作用。方法采用小鼠耳肿胀、大鼠角叉菜胶足跖肿胀、大鼠棉球肉芽肿等实验模型观察其抗炎作用;以小鼠热板法和扭体法研究其镇痛作用。结果健胃康颗粒剂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;并可提高小鼠的热痛阈值,减少小鼠的扭体次数。结论健胃康颗粒剂具有抗炎、镇痛作用。     

苯甲酰青藤碱的镇痛抗炎作用

目的:考察青藤碱衍生物苯甲酰青藤碱的镇痛、抗炎作用.方法:用小鼠扭体法、小鼠热板法、小鼠耳肿胀法、大鼠足跖肿胀法等试验观察.结果:苯甲酰青藤碱可抑制冰醋酸致小鼠疼痛的作用,提高小鼠热板痛阈值,抑制由二甲苯引起的小鼠耳肿胀,对角叉菜所致的足肿胀有抑制作用.结论:苯甲酰青藤碱具有镇痛、抗炎作用,且呈量效关系.     

偏痛胶囊流浸膏镇痛抗炎作用实验研究

目的:研究偏痛胶囊流浸膏镇痛、抗炎药效学作用.方法:热板法、醋酸扭体法观察偏痛胶囊流浸膏对小鼠的镇痛作用,二甲苯致小鼠耳肿胀、蛋清致大鼠足肿胀的方法研究偏痛胶囊流浸膏的抗炎作用.结果:偏痛胶囊流浸膏能明显减少醋酸致小鼠扭体次数,显著提高小鼠痛阈值(P＜0.01或P＜0.05);明显抑制小鼠耳肿胀,减少耳重差,对大鼠足跖肿胀有显著抑制作用(P＜0.01或P＜0.05).结论:偏痛胶囊流浸膏具有较好的镇痛、抗炎作用.     

乌梅透骨口服液抗炎镇痛活血作用的药效学

目的：观察乌梅透骨口服液（WTOL）的抗炎、镇痛和活血化淤作用。方法：采用二甲苯致耳肿胀实验、腹腔毛细血管通透性实验、角叉菜胶致足跖肿胀实验和棉球肉芽肿实验观察该药的抗炎作用；采用扭体实验和热板实验观察WTOL的镇痛作用；建立血淤模型观察该药的活血作用。结果：WTOL能显著抑制二甲苯所致的耳肿胀、降低腹腔毛细血管通透性、抑制角叉菜胶引起的足跖肿胀和棉球所致的肉芽肿（P〈0．05）；对醋酸引起的扭体反应有显著的抑制作用，并能明显提高小鼠热板痛阈（P〈0．05）；能降低血淤模型大鼠的血液黏度及红细胞压积（P〈0．05）。结论：WTOL对实验动物模型具有明显的抗炎、镇痛及活血作用。     

痹痛宁颗粒抗炎镇痛的实验研究

目的研究痹痛宁颗粒的抗炎镇痛作用。方法小鼠耳廓肿胀、大鼠足跖肿胀等实验观察其抗炎作用;通过热板法和醋酸扭体法观察其镇痛作用。结果痹痛宁颗粒能显者抑制二甲苯所致小鼠耳廓肿胀,蛋清致大鼠足跖肿胀,提高热板法疼痛模型小鼠痛阈值,抑制醋酸所致小鼠扭体痛反应。结论痹痛宁颗粒具有显著的抗炎、镇痛作用,应进—步深入探讨其抗炎、镇痛的作用机制。     

桂皮醛解热镇痛抗炎作用的实验研究

目的：观察桂皮醛解热镇痛抗炎作用。方法：采用酵母发热大鼠模型，观察桂皮醛解热作用；采用小鼠扭体法和热板法，观察桂皮醛镇痛作用；通过小鼠耳肿胀及对腹腔毛细血管通透性的影响观察桂皮醛抗炎作用。结果：桂皮醛能显著减轻酵母所致大鼠发热反应，明显提高热板痛阈和抑制醋酸所致扭体反应，亦能显著抑制腹腔毛细血管通透性的增高及二甲苯所致小鼠耳廓肿胀。结论：桂皮醛具有明显的解热镇痛抗炎作用。     

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．     

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。     

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.     

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.