安胃丸抗炎镇痛作用的实验研究

目的研究安胃丸的镇痛、抗炎作用。方法采用扭体法和热板法,观察安胃丸的镇痛作用;采用二甲苯致小鼠耳廓肿胀模型和大鼠棉球肉芽肿模型,观察该药的抗炎作用。结果安胃丸各剂量组小鼠扭体次数显著减少;其中安胃丸中剂量可显著延长小鼠扭体潜伏期。安胃丸高剂量可提高热刺激小鼠的痛阈值。安胃丸各组二甲苯引起的小鼠耳肿胀度及大鼠棉球所致肉芽组织的质量显著降低。结论安胃丸具有良好的抗炎、镇痛作用。     

胃疡宁丸抗炎镇痛的药效研究

目的:对胃疡宁丸的抗炎镇痛作用进行全面的药效学评价。方法:采用小鼠扭体实验、甲醛致痛实验、热刺激致痛实验及压足致痛实验评价胃疡宁丸的镇痛作用;采用小鼠毛细管通透性实验、小鼠耳廓肿胀实验、大鼠棉球肉芽肿实验评价胃疡宁丸的抗炎作用。结果:胃疡宁丸各剂量对醋酸所致小鼠的扭体次数无明显影响;胃疡宁丸高剂量能减少小鼠第二时相中的舔左后足累积时间(P0.05);胃疡宁丸各剂量组可分别提高各时间点热刺激及压足刺激所致的痛阈提高百分率(P0.01);胃疡宁丸中、高剂量能显著性降低二甲苯所致小鼠的耳廓肿胀度(P0.05~0.01);各剂量能显著性降低大鼠肉芽肿系数(P0.01)。结论:胃疡宁丸具有良好的抗炎镇痛作用,可供临床选用。     

山桔叶醇提物抗炎镇痛作用的研究

目的 观察山桔叶醇提物(GPE)对小鼠的抗炎镇痛作用.方法 通过二甲苯致小鼠耳廓肿胀、0.6％冰乙酸致小鼠腹腔毛细血管通透性、1％角叉菜胶致小鼠足肿胀及用小鼠棉球肉芽肿法观察GPE的抗炎作用;通过冰乙酸致小鼠扭体反应和热板致小鼠疼痛法观察GPE的镇痛作用.结果 GPE高、中、低剂量均可显著抑制二甲苯致小鼠耳廓肿胀的肿胀度、1％角叉菜胶致小鼠的足肿胀、0.7％冰乙酸致小鼠的扭体反应次数;GPE高、低剂量可显著抑制冰乙酸致小鼠腹腔毛细血管通透性的增高;GPE高、中剂量均可抑制角叉菜胶致小鼠足肿胀中PGE2的渗出及小鼠棉球肉芽肿的重量,可增高热板致小鼠疼痛的痛阈值.结论 GPE对小鼠有抗炎镇痛的作用.     

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.     

椎痛安胶囊抗炎镇痛作用的实验研究

目的:研究椎痛安胶囊的抗炎、镇痛、消肿等药理作用,为该药的临床研究提供基础.方法:采用小鼠耳廓肿胀法、大鼠甲醛致足跖肿胀法、大鼠棉球肉芽肿法、小鼠热板法、小鼠扭体法等多种模型和方法.结果:椎痛安胶囊能较好地抑制二甲苯引起的小鼠耳廓炎性肿胀和大鼠甲醛致足跖肿胀,并减轻大鼠棉球肉芽肿质量,说明椎痛安胶囊有明显的抗炎作用.镇痛实验表明,椎痛安胶囊能显著提高热板试验小鼠的痛阈,有效抑制冰醋酸引起的小鼠扭体反应次数.结论:椎痛安胶囊具有良好的抗炎、镇痛、消肿等作用.     

贯叶连翘提取物抗炎镇痛作用实验研究

目的：探讨贯叶连翘提取物的抗炎镇痛作用。方法：采用二甲苯致小鼠耳廓肿胀、大鼠棉球肉芽肿实验观察贯叶连翘提取物抗炎作用;通过小鼠甲醛致痛实验观察其镇痛作用。结果：贯叶连翘提取物能够明显抑制二甲苯致小鼠耳廓肿胀,抑制大鼠棉球肉芽肿的增重,减少小鼠在注射甲醛后0～5min,15～30min两个时相内舔足时间、减轻甲醛所致小鼠足跖肿胀。结论：贯叶连翘提取物具有明显的抗炎镇痛作用。     

益母草抗炎镇痛作用的实验研究

目的 探讨益母草的抗炎、镇痛的药理作用.方法 采用二甲苯致小鼠耳廓肿胀,角叉菜胶致大鼠足跖肿胀,小鼠棉球肉芽肿实验观察益母草的抗炎作用,采用热刺激和化学刺激致小鼠疼痛,观察其镇痛作用.结果 益母草对小鼠耳肿胀,大鼠足跖肿胀及小鼠棉球性肉芽肿均有显著抑制作用,能显著提高小鼠热板实验中的痛阈,减少扭体次数.结论 益母草具有显著的抗炎、镇痛的药理作用.     

独一味滴丸抗炎镇痛作用研究

目的观察独一味滴丸抗炎、镇痛作用。方法采用二甲苯小鼠耳肿胀模型、大鼠棉球肉芽肿模型研究独一味滴丸的抗炎作用;采用小鼠热板法、扭体法、甲醛致痛法、大鼠尾电刺激法、大鼠尾尖部压痛法观察独一味滴丸的镇痛作用。结果独一味滴丸对二甲苯所致小鼠耳廓肿胀、大鼠棉球肉芽肿等急慢性炎症模型均有明显抑制作用;对热刺激、化学刺激、电刺激、机械刺激所诱发的动物疼痛均有抑制作用。结论独一味滴丸具有显著的抗炎镇痛作用。     

鸭跖草抗炎镇痛有效部位实验研究

目的：研究鸭跖草不同提取物的抗炎镇痛作用。方法取鸭跖草的水提取物和乙醇提取物,采用二甲苯致小鼠耳肿胀、小鼠棉球肉芽肿胀为抗炎筛选方法;以冰醋酸扭体法、热板法为镇痛筛选方法。结果鸭跖草乙醇提取物和水提起物可减轻二苯致小鼠耳廓肿胀程度,减小小鼠棉球肉芽肿胀程度,减少醋酸致小鼠扭体次数,乙醇提物能延长小鼠舔足时间,乙醇提取物作用强于水提取物,其镇痛抗炎效果均表现出明显的剂量依赖关系。结论中药鸭跖草乙醇提取物具有明显的镇痛抗炎作用。     

五鹤续断抗炎镇痛作用的实验研究

目的:探讨五鹤续断的抗炎镇痛作用。方法:抗炎实验采用二甲苯致小鼠耳廓肿胀等常规抗炎模型;镇痛实验采用热板法和醋酸扭体法。结果:五鹤续断提取物可明显抑制二甲苯致小鼠耳廊肿胀及蛋清引起的大鼠足跖肿胀,能显著抑制大鼠棉球肉芽肿的增重及醋酸致小鼠扭体反应,可明显延长热板引起小鼠疼痛反应的痛阈值。结论:富硒五鹤续断有明显的抗炎镇痛作用。     

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.