大孔吸附树脂动态纯化葛根藤总黄酮的研究

目的研究大孔树脂动态纯化葛根藤总黄酮的最佳工艺参数。方法采用动态吸附、分离的方法,以总黄酮含量为指标进行考察。结果 D-101大孔吸附树脂静态吸附葛根藤总黄酮的最大吸附量为40.25mg·mL-1;树脂的静置时间为12h;D-101树脂最佳上样浓度为38.00mg·mL-1、70%乙醇为最佳洗脱剂;3mL·min-1做为洗脱剂的洗脱流速为最佳洗脱流速。结论经过工艺验证,在这些参数条件下,分离、纯化葛根藤总黄酮具有良好的重现性。     

大孔树脂吸附分离荆芥总黄酮工艺研究

目的 筛选大孔树脂吸附法分离荆芥总黄酮的最佳洗脱工艺条件.方法 采用D-101型大孔树脂对荆芥总黄酮洗脱吸附,观察上样液流速、浓度、洗脱液浓度对荆芥总黄酮含量影响.结果 实验结果表明,D-101型大孔树脂最佳洗脱工艺参数为上样药液流速3 ml/min,浓度10 mg/ml,洗脱液乙醇浓度70%.结论 D-101型大孔树脂洗脱条件可行方便,适合于荆芥总黄酮分离工艺.     

枇杷叶总黄酮的纯化工艺及抗氧化活性研究

目的 优选枇杷叶总黄酮分离纯化的工艺条件,考察枇杷叶总黄酮抗氧化活性。方法 考察不同型号大孔树脂吸附洗脱能力,及大孔树脂、聚酰胺、硅胶对枇杷叶总黄酮的纯化能力,选择最佳分离纯化工艺,并采用ABTS自由基清除试验对黄酮提取物进行抗氧化活性评价。结果 D101树脂对枇杷叶总黄酮的吸附性能最好,最佳纯化工艺为D101树脂每1g上样相当于1.5g原药材样液,水、10%乙醇、40%乙醇、90%乙醇分别洗脱,洗脱流速为80mL？h-1（12BV？h-1）,收集40%乙醇部分经D101大孔树脂同样条件二次洗脱,收集40%乙醇洗脱液得总黄酮提取物。提取物对ABTS自由基有较好的清除作用。结论 D101大孔树脂重复吸附是分离纯化枇杷叶总黄酮的理想方法。枇杷叶总黄酮具有良好的抗氧化活性。     

大孔吸附树脂纯化两色金鸡菊总黄酮的工艺研究

目的研究大孔树脂纯化两色金鸡菊总黄酮的工艺条件及参数。方法采用静态吸附解吸法优选适宜的大孔树脂,以树脂吸附量、总黄酮解吸率为考察指标,对筛选出的树脂进行工艺优化。结果 D-101树脂具有较好的吸附及解吸附性能,其最佳工艺为:上样液质量浓度3.4 mg/mL,树脂的上样量为15 mL/g,上样液pH值为5.0,上样流速1.0 mL/min,6 BV去离子水洗脱除杂后,用pH 5.0的70%乙醇以1.5 mL/min洗脱5 BV;所得两色金鸡菊总黄酮质量分数为73.5%,得率为8.8%。结论 D-101树脂综合性能好,适合于两色金鸡菊总黄酮的分离纯化。     

人参叶提取物的制备工艺研究

目的 优选从人参叶提取纯化人参叶提取物的工艺条件及参数. 方法 采用正交实验法确定人参叶的提取工艺,运用静态吸附法优选树脂. 同时用动态吸附法考察样品液浓度、流速、吸附容量等因素对树脂动态吸附性能的影响,并对D101大孔吸附树脂脱附性能进行考察. 用高效液相色谱法测定人参皂苷Re的含量、用质量法计算人参皂苷得率. 结果提取工艺:取人参叶粗段,加入12倍原药材量的50%乙醇,采用热回流法提取2次,每次提取2 h. 纯化工艺:选择D101大孔吸附树脂(4 cm×16 cm,柱体积140 mL,死体积30 mL)进行树脂动态吸附性能考察,上样浓度为相当于原药材0.4 g•mL^-1,最大上样量为160 mL,吸附流速为1.5 BV•h^-1,上样吸附后,分别用6 BV的水、40%乙醇、95%乙醇洗脱,40%乙醇的洗脱部位合并,减压浓缩、干燥,即得提取物. 结论 该提取工艺简便易行,可用于人参叶中人参皂苷的提取纯化.     

大孔树脂精制杭白菊总黄酮的上样条件研究

目的优选D-101大孔树脂精制杭白菊总黄酮工艺中的最佳上样条件。方法将影响树脂吸附性能的3个因素上样量、流速和pH设计成3因素3水平试验,采用L9(34)表正交试验,以树脂吸附总黄酮含量、乙醇洗脱总黄酮含量和固体总黄酮含量为评价指标,选择最佳条件。结果确定最佳上样条件为上样量20 mL、pH为5、流速2 BV/h。结论该最佳上样条件可应用于大孔树脂精制杭白菊总黄酮的上样条件研究。     

AB-8大孔吸附树脂纯化葛根总黄酮

目的 研究AB-8大孔吸附树脂分离纯化葛根总黄酮的工艺条件.方法 以葛根素、葛根总黄酮为指标,对上样相对质量浓度、流速、上样量、水洗脱用量、乙醇洗脱浓度、乙醇用量及树脂再生前使用次数进行考察.结果 上样相对质量浓度:0.20 g·mL-1,流速:3 BV.h-1,上样量:2.5 BV,水洗脱用量:2.0 BV,乙醇洗脱浓度:70%,乙醇用量:2.5 BV,树脂再生前可使用3次.总黄酮和葛根素的纯度分别可达65%和27%.结论 AB-8大孔吸附树脂分离纯化葛根总黄酮的工艺条件可用于葛根中总黄酮的精制.     

大孔吸附树脂分离纯化葛根素的研究

目的 研究大孔吸附树脂分离纯化葛根素的工艺，为充分合理利用葛根药材资源及葛根素的工业化生产提供实验依据。方法 量取已处理好的AB-8型大孔吸附树脂75 mL，装入层析柱，加入葛根水浸液，每次100 mL，流速为6 mL·min^-1，收集最后20 mL流出液用高效液相色谱法测定葛根素含量。对已吸附饱和的AB-8型大孔吸附树脂柱，用纯化水150 mL以同样流速洗涤，弃去水洗液，再以70%乙醇洗脱，每次75 mL，接取最后1 mL供高效液相色谱法测定葛根素含量，直至无葛根素被检测出为止。结果 AB-8型大孔吸附树脂动态饱和吸附量以干树脂计为31.96 mg·g^-1；以70%乙醇为洗脱剂，洗脱率为90.49%；稳定性试验中第10个周期以70%乙醇为洗脱剂，洗脱率为82.51%。结论 AB-8型大孔吸附树脂性能优越，适合葛根素的分离纯化。     

大孔树脂纯化柽柳总黄酮工艺的研究

目的 研究D-101大孔吸附树脂分离纯化柽柳总黄酮的工艺条件. 方法 以柽柳总黄酮为指标,对上样量、吸附时间、洗脱速度、乙醇浓度和上样药液pH进行考察. 结果大孔树脂分离柽柳总黄酮的最佳工艺条件为上样量15 mL,pH 6～7,吸附30 min,流速3 BV.h^-1,乙醇浓度70%,乙醇用量3 BV. 结论 D-101大孔吸附树脂能有效分离纯化柽柳总黄酮.     

大孔吸附树脂纯化蜘蛛香总黄酮的工艺研究

目的 建立大孔树脂富集纯化蜘蛛香总黄酮工艺方法。方法 对D-101、AB-8、HPD-600、D-301 4种不同极性大孔树脂进行吸附率和解吸率筛选,确定选择HPD-600树脂。考察了HPD-600树脂上样量、pH值、上样体积流量、上样液浓度、洗脱液配比、酸液浓度、乙醇体积分数、洗脱剂用量对蜘蛛香总黄酮的影响,优化大孔树脂纯化工艺参数。结果 HPD-600树脂装柱,上样浓度为3.03 mg/mL,上样容量为24.24 mg/g,先0.1 mol/L HCl的10%乙醇溶液洗脱除杂,直至洗液颜色不再变浅、固形物含量不再增加,后用0.1 mol/L HCl的80%乙醇溶液,洗脱体积流量1 mL/min,洗脱5倍柱体积,收集洗脱液减压浓缩至干得提取物。结论 HPD-600树脂适用于蜘蛛香中总黄酮的纯化,可使蜘蛛香总黄酮质量分数达55.25%,收率可达39.01%。     

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.

---

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.