X-5大孔树脂分离纯化5种大黄蒽醌的工艺研究

目的 研究X-5大孔吸附树脂对大黄素、大黄酚、大黄素甲醚、芦荟大黄素、大黄酸的吸附性能及纯化工艺.方法 用HPLC测定5种大黄蒽醌的含量,以总蒽醌为指标,考察X-5大孔吸附树脂对大黄总蒽醌的纯化工艺及参数.结果 X-5型大孔吸附树脂对大黄总蒽醌具有良好的吸附性能,大黄的上样浓度为0.064 g·mL-1,流速1 BV·h-1,洗脱剂为3倍量树脂柱体积的70%乙醇.结论 通过X-5型大孔吸附树脂富集、纯化后,总蒽醌含量达13%,浸膏收率为11%,表明该树脂分离、纯化大黄总蒽醌的工艺可行.     

H1020大孔树脂分离纯化大黄蒽醌的研究

目的：研究H1020大孔树脂分离纯化大黄蒽醌类成分的工艺条件及技术参数.方法：以大黄素为指标,用高效液相色谱（HPLC）法测定大黄素的含量;用分光光度法测定总蒽醌的含量,考察H1020树脂对大黄蒽醌的吸附及解吸性能.结果：H1020树脂对大黄总蒽醌的的适宜交换吸附条件为：药液质量浓度0.125 g·mL^-1（相当于生药材）,pH 5～6,流速1 BV·h^-1（BV：柱床体积倍数）;洗脱剂用75%乙醇.结论：H1020树脂吸附大黄总蒽醌的纯化方法可行,具有较好的应用前景.     

大孔树脂纯化薤白总皂苷的研究

目的：研究薤白中总皂苷纯化工艺。方法：采用大孔吸附树脂对薤白总皂苷进行吸附纯化,以总皂苷的收率、质量分数为考察指标综合评价。结果：薤白总皂苷纯化工艺为提取液上D101大孔树脂柱,吸附3h,以水和5％乙醇洗至无色,再以60％乙醇洗脱,60％乙醇部分为皂苷部位。结论：确定了薤白中皂苷部位的提取纯化工艺,总皂苷含量达到55％。     

大孔吸附树脂纯化鬼针草总黄酮的工艺优选

目的优选大孔树脂纯化鬼针草总黄酮的工艺条件。方法以鬼针草总黄酮的吸附率和洗脱率为指标,通过静态吸附试验比较不同种大孔树脂对鬼针草总黄酮的吸附能力,筛选出合适的大孔树脂型号;通过单因素试验优选鬼针草总黄酮的纯化工艺参数。结果HPD400型大孔树脂纯化效果最好,其最佳工艺参数为药液中质量浓度0．5mg／mL,pH=4．0,吸附速率2BV／h,用9BV60％乙醇洗脱,洗脱速率3BV／h,经大孔树脂纯化后鬼针草提取液中总黄酮纯度由原来的24．47％提高至58．41％。结论HPD400型大孔树脂适用于鬼针草总黄酮的纯化,优选的纯化工艺稳定可行。     

大孔吸附树脂富集三七总皂苷的工艺研究

目的:建立三七总皂苷的大孔吸附树脂吸附纯化的工艺条件及参数.方法:以三七总皂苷的含量为考察指标,对树脂吸附容量、洗脱溶酶及其用量进行了考察.结果:通过大孔吸附树脂富集与纯化后三七总皂苷洗脱率达80%以上,70%乙醇洗脱液干燥后的总固形物中三七总皂苷纯度可达81.6%.结果:三七提取物上D101大孔吸附树脂,以水洗脱后,以70%乙醇洗脱可以达到理想的结果.     

大孔吸附树脂富集纯化牛膝总皂苷研究

目的应用大孔吸附树脂富集纯化牛膝总皂苷。方法牛膝醇提液上大孔吸附树脂柱,以水及不同浓度乙醇依次洗脱,考察牛膝总皂苷的洗脱率和纯度。结果牛膝总皂苷富集于50%乙醇洗脱液部分,洗脱率在58.42%以上。结论采用大孔吸附树脂方法富集、纯化牛膝总皂苷可行。     

大孔吸附树脂纯化酸枣仁总皂苷工艺研究

目的:研究大孔吸附树脂纯化酸枣仁总皂苷的工艺条件及参数。方法:以酸枣仁总皂苷的洗脱率、精制度等为指标,用蒸馏水、30%乙醇、70%乙醇各3BV(柱床沉降体积)依次洗脱,考察大孔吸附树脂对酸枣仁总皂苷的吸附性能和洗脱参数。结果:12·7ml酸枣仁总皂苷样品液上大孔吸附树脂柱,酸枣仁总皂苷富集于70%乙醇洗脱液部位,洗脱率为85·2%,精制度为208·4%。结论:通过大孔吸附树脂富集与纯化,可较好地纯化酸枣仁总皂苷。     

大孔吸附树脂法对天麻中天麻苷和总苷的分离纯化

目的：研究AB-8大孔吸附树脂分离纯化天麻中天麻苷和天麻总苷的工艺条件及参数。方法：以天麻苷和天麻总苷的吸附量和洗脱率为考察指标，研究大孔吸附树脂分离纯化的吸附性能和洗脱参数。结果：AB-8树脂对天麻苷吸附容量为7．32mg·g^-1、对总苷吸附容量为16．25mg·g^-1，洗脱率分别为天麻苷96．77％、天麻总苷96．25％，终产品中天麻总苷的纯度可达18．96％。结论：采用本法分离纯化天麻中天麻苷和总苷是可行的。     

棘白菌素B母核的分离纯化工艺研究

目的 研究大孔吸附树脂结合亲水性C18硅胶填料分离纯化棘白菌素B母核(ECBN)的工艺,有效去除色素及其他杂质,获得高纯度ECBN.方法 用HPLC检测方法,以ECBN的吸附量和洗脱率为指标,考察大孔吸附树脂和亲水性C18填料分离纯化ECBN的吸附性能和洗脱参数.结果 分离纯化ECBN的最佳吸附剂为大孔吸附树脂XAD-18和亲水性C18填料,洗脱剂分别为8％乙醇和3％甲醇.此工艺路线获得的成品纯度大于95％,总收率为65％.结论 该分离纯化方法为国内首次报道,工艺简单,使用有机溶剂少,分离效果好,适用于工业化生产.     

大孔吸附树脂对地榆中总鞣质的纯化

目的：筛选最佳大孔树脂纯化地榆中总鞣质,研究其最佳工艺条件及参数。方法：以鞣质的吸附量、吸附率和解吸率为考察指标,对8种大孔吸附树脂并进行评价。结果：HPD-400型树脂具有较好的吸附分离性能,最佳工艺条件为：上样液浓度4．54mg·ml^-1,吸附流速为4BV·h^-1,上柱量为4BV,以70％的乙醇洗脱,用量为3BV。通过大孔树脂纯化后,终产品中鞣质的纯度为68．52％。结论：HPD-400型树脂可用于地榆中鞣质的富集纯化。     

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.