荆芥挥发油的提取及包合工艺研究

目的:采用水蒸气蒸馏法提取荆芥挥发油,优选提取工艺及包合工艺。方法:以挥发油的提取量为考察指标,以加水量、浸泡时间、提取时间作为考察的3 个主要因素,通过 L9(34) 正交试验法优化荆芥挥发油最佳提取工艺。以挥发油与β-环糊精的比例、溶剂用量、时间为考察因素,优选挥发油的包合工艺。结果:最佳提取工艺为饮片加水12倍量,浸泡3小时,提取8小时; 最优包合工艺为挥发油与β-环糊精比例为1:10,加入溶剂量为3倍量,胶体磨碾磨时间为15min。结论:优选的提取工艺和包合工艺简便、快速、稳定、可行,可作为荆芥挥发油产业化生产工艺。     

正交试验优选杏香兔耳风总黄酮提取工艺

目的:优选杏香兔耳风总黄酮的提取工艺。方法:以芦丁为对照,以溶剂用量、提取次数、浸泡时间和提取时间为考察因素,以总黄酮转移率为指标,采用正交试验优选最佳提取工艺。结果:最佳提取工艺为用pH8的氨水配制的50%乙醇溶液为提取溶剂,分别以10、10、8、8倍量回流提取4次,每次1h;总黄酮转移率为84.97%。结论:该提取工艺合理、简单,可用于大规模生产。     

黄连提取方法的试验研究

目的通过对黄连提取方法的研究,确定其最佳提取方法的因素及水平。方法比较醇提与水提,选择最佳提取溶剂,以提取次数、提取时间、浸泡时间、溶剂量为考察因素,以浸膏得率和盐酸小檗碱的含量为考察指标,用正交试验法优选黄连提取工艺。结果黄连的最佳提取工艺为分别加12、10、10倍量水,浸泡0.5h,回流提取3次,提取时间分别为1.5、1.5、1.0 h。结论通过对黄连提取工艺的优选,为工业化大生产提供了实验依据。     

正交设计优选心痛舒片的提取工艺

目的：优选心痛舒片提取工艺。方法：以单因素对乙醇浓度进行考察后，采用正交试验设计法考察溶剂量、浸泡时间及提取时间3个因素对丹参酮ⅡA得率的影响。结果：优选出最佳提取工艺为：乙醇浓度90％，提取两次，溶媒量分别为8倍、6倍，浸泡1．5h，分别提取1．5h、1．0h。结论：上述试验结果可为心痛舒片提取工艺提供试验依据。     

正交试验优选葫芦巴总黄酮提取工艺

目的优选葫芦巴总黄酮最佳提取工艺。方法通过L9(34)正交试验设计及单因素试验,以总黄酮含量为考察指标,综合探讨了提取条件对活性物质提取量的影响。结果各实验因素对葫芦巴总黄酮影响均以提取次数、溶剂体积、提取时间、浸泡时间因素顺序降低。结论总黄酮提取最佳条件为用20倍量体积分数70%的乙醇,回流提取3次,每次1.5h,浸泡30min。最佳提取工艺药材中总黄酮的含量为1.5292%。     

正交试验优选板蓝根多肽的提取工艺

目的:优选板蓝根多肽的提取工艺。方法:以溶剂种类、提取时间、溶剂用量为考察因素,以凯氏定氮法和二喹啉甲酸法测定多肽得率,并以此为评价指标,采用正交试验优选提取工艺。结果:在室温下,板蓝根多肽的最佳提取工艺为用15倍量的超纯水浸泡24 h,该条件下,收率可达70%。结论:所选工艺合理、简便,可用于提取板蓝根中多肽。     

正交试验优选四叶参中四叶参皂苷的提取工艺

目的:优选四叶参中四叶参皂苷的提取工艺。方法:采用单因素试验考察提取溶剂、提取时间、溶剂用量对四叶参皂苷溶出的影响;以溶剂用量、提取次数、提取时间为考察因素,以四叶参皂苷提取率为评价指标,采用正交试验优选提取工艺。结果:最佳提取工艺为加30倍量的甲醇,超声提取3次,每次40 min。结论:所选工艺合理、可行,可用于四叶参中四叶参皂苷的提取。     

温胃胶囊提取工艺研究

目的优选出温胃胶囊挥发油提取和醇提工艺的最佳参数。方法采用正交试验法,以浸泡时间、加水量、提取时间3因素3水平,以挥发油提取率为考察指标,优选挥发油提取工艺;以乙醇体积分数、加醇量、提取时间3因素3水平,以醇浸膏得率和总黄酮含量为考察指标,优选醇提工艺。结果与结论温胃胶囊挥发油提取的最佳工艺参数为浸泡2h,加10倍量水,水蒸气蒸馏8h;醇提最佳工艺参数为加6倍量体积分数60%乙醇提取2h。     

正交试验优选枳实中柚皮苷的提取工艺

目的:优选枳实中柚皮苷的提取工艺。方法:采用单因素试验考察提取溶剂及溶剂浓度对枳实中柚皮苷转移率的影响。以溶剂用量、提取次数、提取时间为考察因素,以柚皮苷转移率为评价指标,采用L9(34)正交试验优选提取工艺。结果:最佳提取工艺为6倍量的70%乙醇提取3次,每次30 min。结论:该工艺稳定,提取率高,可供大规模工业化生产参考。     

正交法优选杭黄菊挥发油提取工艺

目的探讨杭黄菊挥发油的最优提取工艺。方法采用L9(33)正交试验法,以挥发油提取率为指标,以浸泡时间、加水量、提取时间为考察因素进行正交试验。结果影响杭黄菊挥发油提取的最主要因素为浸泡时间,其次为提取时间。最佳提取工艺条件为杭黄菊浸泡10 h,加水12倍,提取10 h。结论该提取工艺简便易行,在最佳提取工艺条件下提取率为0.44%。     

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.     

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.     

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.