超声波辅助提取西藏雪莲总黄酮及其抗氧化性研究

目的研究以西藏雪莲为原料、乙醇为溶剂,超声提取黄酮类化合物工艺过程的最优条件。方法在单因素试验基础上通过响应面试验优化乙醇体积分数、超声时间和温度等工艺条件,并研究了其对DPPH·的清除作用。结果西藏雪莲总黄酮的最优超声提取工艺:乙醇浓度70%,提取温度60℃,液料比13:1(m L/g),提取时间50 min,提取2次,在此条件下,得到的总黄酮提取物含量为4.246%。其具有较好的清除DPPH·效果。结论超声提取西藏雪莲总黄酮工艺具有时间短、提取物含量高等优点,具有进一步开发应用的价值。     

白花蛇舌草总黄酮的超声提取工艺研究

目的：优选白花蛇舌草总黄酮超声提取最佳工艺。方法：选择无毒的有机溶剂乙醇作为提取溶剂,超声波作为提取方法,然后用聚酰胺色谱柱纯化总黄酮成分,采用NaNO2-Al（NO3）3-NaOH显色法,以芦丁为对照品计算总黄酮的含量,并用正交设计法进行提取工艺优化。通过考察不同因素和水平对提取效率的影响,优选出白花蛇舌草中总黄酮的最佳提取工艺。结果：最佳提取工艺是先用石油醚脱脂1次,提取溶剂为70%乙醇,料液比为1：20,超声时间为30 min,提取次数为3次,提取率为2.375 6%。结论：优选出的工艺简单易行,能保证白花蛇舌草中总黄酮提取完全。     

正交试验优化羊蹄总黄酮提取工艺

目的优选羊蹄总黄酮最佳提取工艺。方法采用正交试验优化乙醇提取工艺条件,并利用紫外分光光度法测定其含量。结果正交试验确定总黄酮最优提取条件:70%乙醇提取2次,每次2h,溶剂用量为12倍量。结论该提取工艺简便、安全、可行、重现性好。     

Box-Behnken响应面法优选低共熔溶剂提取马蹄金总黄酮工艺

目的 优选低共熔溶剂提取马蹄金总黄酮的工艺。方法 以低共熔溶剂体系摩尔比、含水量、超声功率、超声时间为单因素变量,以马蹄金中黄酮类成分提取率为评价指标,采用Box-Behnken响应面法优选总黄酮提取工艺,并进行验证试验。结果 优选的提取工艺为低共熔溶剂氯化胆碱-乳酸（摩尔比1∶2）,含水量为70%,超声（功率为180 W）提取30 min。验证试验结果显示,在此条件下的总黄酮提取率与回归模型预测值的相对误差为0.55%。结论 该优选工艺操作简便、重复性好,可用于马蹄金总黄酮的提取。     

复方雪莲风湿凝胶膏提取工艺研究

目的优选复方雪莲风湿凝胶膏提取工艺。方法采用正交试验设计,分别以蛇床子素含量、姜黄素含量和浸膏收率为指标,优化雪莲等7味药材的提取工艺;以没食子酸含量和浸膏收率为指标,优选土元和五倍子2味药的提取工艺。结果 7味药最佳提取工艺为10倍量80%乙醇,提取3次,每次1 h;2味药最佳提取工艺为10倍量水,提取3次,每次2.5 h。结论优选的提取工艺稳定、可行。     

枳椇子中总黄酮的提取工艺优化

目的:优选枳楔子提取物的最佳提取工艺。方法:以提取物得率及提取物中总黄酮含量为检测指标,对提取溶剂进行筛选;通过考察小鼠肝匀浆中的SOD活性、MDA含量,确定最佳提取方法。同时采取正交设计法对最佳提取方法的提取工艺进行了考察。结果:以75%乙醇为提取溶剂,采用热回流提取法,乙醇浓度为75%、提取时间2h、乙醇加入量为8倍量时为最佳提取工艺。结论:该优选提取工艺合理、可行、可控。     

葛根总黄酮提取工艺优化研究

目的优选葛根总黄酮的最佳提取工艺。方法以乙醇为提取溶剂,正交试验L9（3^4）设计对提取溶剂浓度,提取时间和料液比进行考察;选用特征峰图谱方法所测得的特征峰面积总和、葛根素转移率和固体含量作为评价指标,计算综合得分,以最终得分确定葛根总黄酮的最佳工艺条件。结果影响葛根总黄酮提取的主要因素是溶剂浓度,其次是提取时间,再次是料液比,最佳提取工艺为A2B3C2D2,即,乙醇浓度70%,提取时间3 h,提取次数2次,料液比为1∶8。结论验证试验表明最佳工艺下总黄酮提取率稳定,提取率高,提取工艺合理可行。     

用正交设计法优选老鹰茶总黄酮的提取工艺

目的优选老鹰茶总黄酮提取的最佳工艺.方法以芦丁为对照,AlCl3为显色剂,用紫外分光光度法在410 nm处测定总黄酮含量,以总黄酮含量为指标,应用正交实验,优选老鹰茶总黄酮提取的最佳工艺.结果老鹰茶总黄酮的最佳提取工艺为80%乙醇,12倍量,回流提取3次,每次2 h.结论紫外分光光度法方便、快捷,可用于老鹰茶总黄酮提取工艺的优选.     

正交试验优选独一味总黄酮的提取工艺

目的建立独一味黄酮类成分的提取工艺。方法采用L9(34)正交设计法,以独一味总黄酮含量、山栀苷甲酯和8-O-乙酰山栀苷甲酯含量以及出膏率为检测指标进行试验。结果优选的提取工艺为,70%乙醇,提取3次、每次1.5 h,溶剂用量10倍。结论优选的独一味总黄酮类成分提取工艺简便、省时、节约成本,适合工业化生产。     

超声提取白花蛇舌草总黄酮工艺研究

目的研究白花蛇舌草总黄酮的超声提取工艺。方法以超声波法提取总黄酮类物质,采用正交实验优化提取工艺。利用聚酰胺柱色谱法纯化提取的总黄酮,以芦丁为对照品,利用NaNO2 Al（NO3）3 NaOH显色法计算总黄酮含量。结果最佳提取工艺为白花蛇舌草药材以70%乙醇为提取溶剂,料液比1：20,超声提取30 min,提取3次,提取率2.38%。结论优选出的最佳工艺简单易行,能完全提取白花蛇舌草中总黄酮。     

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.