均匀设计法优选栀子半仿生提取工艺条件

目的:优选栀子半仿生提取工艺条件。方法:以栀子苷得率、总环烯醚萜得率和干浸膏收率为指标,采用均匀设计优选栀子半仿生提取工艺条件。结果:优化条件为三煎用水的p H依次为2.0、6.5、9.0;煎煮时间依次为2.0,1.0,1.0 h。结论:采用均匀设计优选的半仿生提取条件科学、合理。     

均匀设计法优选房陵丹参水溶性成分提取工艺

目的优选丹参水溶性成分半仿生提取的最佳工艺条件。方法以丹酚酸B含量、总酚酸含量、干浸膏得率为指标,采用均匀设计优选其半仿生提取法（简称SBE法）的条件。结果优化条件为三煎用水的pH依次为2.0,7.5,8.0;煎煮时间依次为1.0,0.5,0.5 h。结论优选的半仿生条件科学、合理。     

均匀设计法优选蛇床子半仿生提取工艺

目的:优选半仿生提取蛇床子中总香豆素的工艺条件。方法:以蛇床子素含量、总香豆素含量、干浸膏得率为综合指标,采用均匀设计优选蛇床子半仿生提取法(简称SEB)的条件。结果:通过优化并结合工业生产实际,确定三煎用水的pH值依次为3.2,6.8,8.7;煎煮时间依次为132,66,66min。结论:本法为蛇床子的提取提供了理论依据。     

均匀设计法优选大黄半仿生提取工艺

目的：优选大黄的半仿生提取工艺条件。方法：以芦荟大黄素、大黄酸、大黄素、大黄酚的总含量,总蒽醌含量和干浸膏得率为综合评价指标,采用均匀设计法优选大黄半仿生提取工艺。结果：通过优化并结合工业生产实际,确定三煎用水的pH依次为2.0、6.5、9.0;煎煮时间依次为：2,1,1 h。结论：本法为大黄的优化提取提供了理论依据。     

均匀设计法优选莲子心的半仿生提取工艺

目的:优选半仿生法提取莲子心中总生物碱的工艺条件。方法:采用均匀设计法优选半仿生提取工艺;以总生物碱含量、干 浸膏得率为指标,考察药材的提取时间、溶媒量、pH值等因素对提取工艺的影响。结果:优选工艺为莲子心加8倍量水提取3次,3 煎用水的pH值分别为5．0、6．0、8．0,煎煮总时间为4h。结论:本法为莲子心的提取提供了理论依据。     

均匀设计法优选连翘半仿生提取工艺

目的：优选连翘的半仿生提取工艺条件。方法：以连翘酯苷A、连翘苷的含量和干浸膏得率为综合评价指标,采用均匀设计法优选连翘半仿生提取工艺。结果：通过优化试验并将试验结果经过DPS数据处理,确定最优条件并结合生产实际,确定三煎用水的pH依次为2.0,7.0,10.0;煎煮时间依次为：1,0.5,0.5 h。结论：本法为连翘的优化提取提供了理论依据。     

均匀设计法优选山豆根半仿生提取工艺

目的：优选山豆根半仿生提取（SBE）最佳工艺条件。方法：以氧化苦参碱含量和干浸膏得率为指标,采用均匀设计优选其半仿生提取法条件。结果：优化SBE法工艺条件为,三煎用水的pH依次为4．5、7．5、9．0,煎煮时间依次为1．5、0．75、0．75h。结论：该工艺科学合理,有利于综合考察山豆根药效物质提取效果。     

均匀设计法优选抗感利咽糖浆半仿生法提取的工艺条件

目的:优选抗感利咽糖浆的半仿生提取条件。方法:采用均匀设计法,在处方组成和用量、煎提温度、煎提用水量、过滤方法、离心时间、浓缩倍数等条件相同的情况下,用不同p H的水溶液提取方药,以连翘酯苷A、虎杖苷、黄芩苷、大黄素的含量及干浸膏的得率为指标,经过标准化处理,综合评价,优选该方药半仿生提取的工艺条件。结果:最佳的提取工艺为三煎用水的p H值依次为4.9、7.5、9.0,三煎总时间为2 h。结论:结合生产实际,确定三煎用水的p H值依次为5.0、7.5、9.0,3煎提取时间依次为1.0 h、0.5 h、0.5 h。     

均匀设计法优选金果榄半仿生提取工艺

目的:优选金果榄药材半仿生提取(SBE)法的最佳工艺。方法:以盐酸巴马汀含量、盐酸药根碱含量和干浸膏得率的综合评价为指标,以3次煎煮用水的pH值和煎煮时间为考察因素,采用均匀设计法优选SBE法的最佳工艺。结果:优选的工艺为3次煎煮用水的pH值依次为4.0、6.5、9.0,煎煮时间依次为1.0、0.5、0.5h。结论:该工艺科学、合理,可为金果榄药效物质的提取工艺提供理论依据。     

用均匀设计优选玄参的“半仿生提取法”工艺条件

目的优选玄参半仿生提取法的工艺条件。方法以干浸膏、水溶性浸出物、醇溶性浸出物、哈巴俄苷和肉桂酸含量为指标,采用均匀设计优选玄参半仿生提取法的最佳工艺参数。结果玄参SBE法提取的最佳工艺为:三煎用水的pH值分别为6.0、7.5、8.5;煎煮时间依次为150、75、75min。结论优选了玄参SBE法提取的最佳工艺条件。     

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.