枇杷止咳胶囊的药效学研究

目的研究枇杷止咳胶囊的功效。方法氨水引咳、酚红分泌及组胺致喘等有关试验。结果枇杷止咳胶囊可延长小鼠因氨水所致的咳嗽潜伏期及枸橼酸所致豚鼠的咳嗽潜伏期,减少咳嗽次数;增加小鼠呼吸道酚红排痰量;对抗豚鼠由组胺所致哮喘症状,使动物跌倒潜伏期延长;具有抑制醋酸引起小鼠腹腔毛细血管通透性的抗感染消肿作用结论枇杷止咳胶囊具有镇咳、祛痰、平喘及抗感染作用。     

雪梨止咳颗粒(浸膏粉)药效学研究

目的 观察雪梨止咳颗粒(浸膏粉)的止咳、化痰作用.方法 采用小鼠氨水引咳法、豚鼠柠檬酸引咳法观察雪梨止咳颗粒的止咳作用;小鼠呼吸道酚红排泌法观察其化痰作用.结果 雪梨止咳颗粒(浸膏粉)可明显延长氨水喷雾致咳小鼠的咳嗽潜伏期,显著减少其咳嗽次数;延长柠檬酸喷雾致咳豚鼠的咳嗽潜伏期,减少其咳嗽次数;增加小鼠呼吸道酚红排泌量.结论 雪梨止咳颗粒(浸膏粉)对造模小鼠、豚鼠具有止咳作用,对造模小鼠具有化痰作用.     

止咳平喘药浓百合剂的药效学研究

目的 探讨浓百合剂止咳、祛痰、平喘和抗炎的功效.方法 采用小鼠氨水引咳法、豚鼠枸橼酸引咳法、小鼠酚红祛痰法、豚鼠磷酸组胺引喘法、小鼠耳肿胀法和大鼠足跖肿胀法.结果 浓百合剂可延长小鼠因氨水所致及豚鼠因枸橼酸所致的咳嗽潜伏期,减少咳嗽次数;增加小鼠呼吸道酚红排痰量;对抗豚鼠由磷酸组胺所致的哮喘,延长动物跌倒的潜伏期;减轻二甲苯致小鼠的耳肿胀和角叉菜胶致大鼠的足肿胀,抗炎作用明显.结论 浓百合剂具有较好的止咳、祛痰、平喘、抗炎作用.     

速效止咳糖浆镇咳、平喘、祛痰作用的研究

目的研究速效止咳糖浆药理作用.方法采用小鼠氨水引咳法和豚鼠枸橼酸引咳法、豚鼠整体动物引喘法和离体气管螺旋条实验法、小鼠酚红法分别观察速效止咳糖浆镇咳、平喘、祛痰作用.结果速效止咳糖浆可减少氨水引发小鼠咳嗽反应次数及枸橼酸引起豚鼠咳嗽反应次数,并延长咳嗽潜伏期;对组胺-乙酰胆碱诱发的喘息有保护作用,表现为明显抑制哮喘反应,引喘潜伏期明显延长,并可浓度依赖性的拮抗Ach的收缩支气管作用;增加小鼠气管内酚红排出量.结论速效止咳糖浆具有镇咳、平喘、祛痰作用,为临床治疗慢性支气管炎提供药理学依据.     

金黄止咳颗粒的止咳化痰抗炎作用实验研究

目的观察金黄止咳颗粒的止咳、化痰和抗炎作用。方法分别采用小鼠氨水引咳法、豚鼠枸橼酸引咳法观察金黄止咳颗粒止咳作用,气管酚红排泌法观察其化痰作用,及小鼠二甲苯耳肿胀法和大鼠角叉菜胶性足肿胀法观察其抗炎作用。结果金黄止咳颗粒可明显延长小鼠和豚鼠的咳嗽潜伏期和减少咳嗽次数;显著增加小鼠呼吸道黏膜酚红的排出量,对二甲苯和角叉菜胶所致急性炎症反应有很好的抑制作用。结论金黄止咳颗粒具有明显的止咳、化痰和抗炎作用。     

南芪北芪祛痰、镇咳和平喘作用的实验研究

目的:观察南蓖与北芪在祛痰、镇咳及平喘作用中效果的异同,为南芪的广泛运用提供实验依据.方法:通过小鼠气管酚红法、家鸽纤毛运动实验、小鼠浓氨水引咳法、豚鼠枸橼酸引咳法及豚鼠组胺-乙酰胆碱超声雾化法观察两者的祛痰镇咳平喘作用.结果:南芪、北芪均能增加小鼠气管酚红排泌量,促进家鸽气管内墨汁运动,明显减少氨水引发小鼠咳嗽反应的次数和枸橼酸引发豚鼠咳嗽反应的次数,并延长咳嗽潜伏期,对抗组胺-乙酰胆碱引起的豚鼠支气管哮喘.结论:两者均具有良好的祛痰、镇咳及平喘作用,且效果无显著差异.     

速效止咳糖浆镇咳、平喘、祛痰作用的研究

目的　研究速效止咳糖浆药理作用。方法　采用小鼠氨水引咳法和豚鼠枸橼酸引咳法、豚鼠整体动物引喘法和离体气管螺旋条实验法、小鼠酚红法分别观察速效止咳糖浆镇咳、平喘、祛痰作用。结果　速效止咳糖浆可减少氨水引发小鼠咳嗽反应次数及枸橼酸引起豚鼠咳嗽反应次数 ,并延长咳嗽潜伏期 ;对组胺 -乙酰胆碱诱发的喘息有保护作用 ,表现为明显抑制哮喘反应 ,引喘潜伏期明显延长 ,并可浓度依赖性的拮抗Ach的收缩支气管作用 ;增加小鼠气管内酚红排出量。结论　速效止咳糖浆具有镇咳、平喘、祛痰作用 ,为临床治疗慢性支气管炎提供药理学依据     

速效止咳糖浆镇咳、平喘、祛痰作用的研究

目的 研究速效止咳糖药理作用。方法 采用小鼠氨水引咳法和豚鼠枸橼酸引咳法、豚鼠整体动物引喘法和离体气管螺旋条实验法、小鼠酚红法分别观察速效止咳糖浆镇咳、平喘、祛痰作用。结果 速效止咳糖浆可减少氨水引发小鼠咳嗽反应次数及枸橼酸引起豚鼠咳嗽反应次数，并延长咳嗽潜伏期；对组胺－乙酰胆碱诱发的喘息有保护作用，表现为明显抑制哮喘反应，引喘潜伏期明显延长，并可浓度依赖性的拮抗Ach的收缩支气管作用；增加小鼠气管内酚红排出量。结论 速效止咳糖浆具有镇咳、平喘、祛痰作用，为临床治疗慢性支气管炎提供药理学依据。     

化痰降气胶囊化痰、止咳、平喘的实验研究

目的初步探讨化痰降气胶囊化痰止咳平喘的功效。方法化痰降气胶囊按小鼠剂量3.8 g生药.kg-1,7.5 g生药.kg-1,15 g生药.kg-1,大鼠和豚鼠剂量2.9 g生药.kg-1,5.8 g生药.kg-1,11.6 g生药.kg-1ig给药,观察化痰降气胶囊的化痰、止咳、平喘作用。结果化痰降气胶囊能明显促进小鼠酚红分泌量,增加大鼠痰液排出量,显著减少浓氨水致小鼠咳嗽次数,延长咳嗽潜伏期,显著减少枸橼酸喷雾致豚鼠咳嗽次数,延长氯化乙酰胆碱和组胺混合液喷雾引喘豚鼠潜伏期。结论化痰降气胶囊具有化痰止咳平喘的作用。     

固本喘嗽康颗粒的镇咳、祛痰、平喘实验研究

目的观察固本喘嗽康颗粒对哮喘的药效作用。方法通过动物模型引咳、祛痰和引喘实验来观察其镇咳、祛痰、平喘效果。结果高、中、低剂量的固本喘嗽康颗粒均能显著地抑制浓氨水所致小鼠咳嗽潜伏期和咳嗽次数;能增加小鼠呼吸道的酚红排泌量;还能显著地延长豚鼠哮喘潜伏期,对豚鼠离体气管平滑肌痉挛具有明显的松弛作用。结论固本喘嗽康颗粒具有明显的镇咳、祛痰、平喘作用。     

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.