超临界CO2萃取三七中挥发油及皂苷的工艺研究

目的研究超临界CO2萃取三七中挥发油和皂苷的工艺。方法通过考察萃取压力、温度、萃取时间、CO2流量、夹带剂对萃取率的影响,确定三七中挥发油和皂苷的较佳萃取条件,采用薄层色谱法（TLC）鉴别挥发油和皂苷成分。结果萃取三七中挥发油较佳条件为：萃取压力30MPa,温度45℃;解析釜I压力为9MPa,温度40℃;解析釜II压力为6MPa,温度35℃;萃取时间2．5h;CO2流量为25kg·h^-1。皂苷的较佳萃取条件为：萃取压力35MPa,温度55℃;解析釜I压力为8MPa,温度45℃;解析釜II压力为5MPa,温度40℃;萃取时间4h;95％乙醇作夹带剂;CO2流量为25kg·h^-1。挥发油中含有人参炔醇,皂苷中含有总皂苷成分。结论超临界CO2萃取挥发油收率高,时间短。加入95％乙醇作夹带剂,升高压力和温度,能萃取出皂苷类成分。     

超临界CO2萃取人参须根中人参炔醇的工艺研究

目的优化超临界CO2萃取人参须根中人参炔醇的工艺。方法以人参炔醇萃取率为指标,用正交试验法进行优化。结果人参炔醇萃取的最佳工艺条件为萃取温度45℃,萃取压力30MPa,萃取时间80 min,夹带剂为95%乙醇。结论采用超临界CO2萃取法提取脂溶性成分具有速度快、效率高和无污染的特点,CO2可循环利用,且该工艺简便易行。     

远志超临界CO2萃取工艺研究

目的研究远志超临界CO2萃取工艺。方法采用正交试验方法,考察影响远志萃取的因素,建立了超临界CO2萃取最佳条件。结果远志超临界CO2萃取最佳工艺为：压力30MPa,温度45℃,流速25kg·h^-1,时间1．5h。结论用超临界CO2萃取远志可以较好的获得其脂溶性成分,提取物可以供进一步深入研究。     

正交设计法优选火麻仁超临界CO2萃取工艺

目的优选火麻仁超临界CO2萃取最佳工艺条件。方法以火麻仁总萃取得率为考察指标,选取萃取压力、萃取温度、分离釜I温度及分离釜Ⅱ温度作为考察指标,采用L9（3^4）正交设计表优选火麻仁超临界CO2萃取最佳工艺条件。结果萃取压力、萃取温度、分离釜I温度及分离釜Ⅱ温度4种因素对火麻仁总萃取得率有极显著性影响（P〈0．001）,而分离釜I压力无显著性影响（P〉0．05）,优选的萃取条件为萃取温度50℃,萃取压力30MPa,分离釜I温度45℃,分离釜Ⅱ温度55℃。结论超临界CO2萃取法操作简单、稳定、提取率高。     

超临界CO_2萃取法提取迷迭香油工艺及其化学组分研究

目的:优化超临界CO2萃取迷迭香油工艺,并分析其主要化学组分。方法:采用正交试验优化超临界CO2萃取迷迭香油工艺的参数,将提取物的化学成分经气相色谱-质谱联用法(GC-MS)进行分离鉴定,并计算各组分的相对百分含量。结果:优化的最佳工艺为萃取压力20MPa,萃取温度45℃,分离压力6MPa,萃取时间120min。迷迭香油中鉴定出21种化学组分,占挥发油总量的97.99%。迷迭香挥发油中含量较高的成分是1,8-桉叶素(27.23%)、α-蒎烯(19.43%)、樟脑(14.26%)、莰烯(11.52%)等。结论:超临界CO2萃取迷迭香油具有提取时间短、提取率高等优点;浙江产迷迭香与西班牙型较为接近。     

正交设计优化超临界CO2萃取姜油工艺

目的：优化超临界CO2萃取生姜工艺参数。方法：建立生姜指标成分6-姜酚的分析方法,以萃取压力、萃取温度、分离釜Ⅰ压力、萃取时间为考察因素,采用L9（3^4）正交试验表,以姜油收率和6-姜酚百分含量为评价指标进行姜油萃取工艺优选。结果：超临界CO2萃取姜油的最佳萃取条件为：萃取压力20MPa;萃取温度40％;萃取时间3h;分离釜Ⅰ压力6MPa;分离釜Ⅱ压力3MPa。此时姜油的收率为2．117％,姜油中6-姜酚的百分含量为23．164％（n=3）。结论：优化后的超临界CO2萃取生姜工艺具有保持药物原有生物活性、提取效率高、提取物纯净无溶剂残留等优点。     

正交试验优选超临界CO_2流体法萃取藿香正气方中挥发油的工艺

目的:优选超临界CO2流体萃取(SFE-CO2)法萃取藿香正气方中挥发油的工艺条件。方法:以萃取压力、萃取温度、解析釜I压力、解析釜I温度为考察因素,以挥发油萃取率为评价指标,采用L9(34)正交试验表进行工艺优选。结果:最佳工艺为萃取压力25MPa、萃取温度30℃、解析釜I压力9MPa、解析釜I温度45℃;此时挥发油的萃取率最高,为2.057%。结论:应用SFE-CO2法萃取藿香正气方中挥发油,萃取率高,稳定性强,操作纯净、安全且能保持生物活性,是具有相当发展潜力的提取分离方法。     

广东紫珠超临界提取物的GC-MS成分分析及体外抗菌活性

采用超临界CO2萃取法提取广东紫珠低极性成分,应用气相色谱-质谱法分析提取物的化学组成,结合计算机检索技术初步鉴定所分离的化合物,应用色谱峰面积归一化法计算各成分的相对百分含量,并考察各分离釜提取物对金黄色葡萄球菌、大肠杆菌和白色念珠菌的体外抗菌活性。结果从超临界CO2流体萃取分离釜Ⅰ提取物中初步鉴定了27个化合物,占总离子流图峰面积的81.12%;超临界CO2流体萃取分离釜Ⅱ提取物初步鉴定了20个化合物,占总离子流图峰面积的74.60%。广东紫珠超临界CO2萃取分离釜Ⅰ、Ⅱ提取物及二者1︰1混合物对金黄色葡萄球菌、大肠杆菌和白色念珠菌显示出抗菌活性。     

超临界CO2萃取川东獐牙菜总员(口山)酮的工艺优化

目的 优化超临界CO2萃取川东獐牙菜总(口山)酮的工艺.方法 以去甲基雏菊叶龙胆酮和总(口山)酮含量为指标,用正交试验法优选.结果 川东獐牙菜总山酮萃取的最佳工艺条件为:萃取温度40 ℃,萃取压力30 MPa,萃取时间80 min,夹带剂为95%乙醇.结论 采用超临界CO2萃取法提取脂溶性成分具有速度快、效率高和无污染的特点,工艺简便易行.     

超临界CO2萃取结合柱层析法提取和纯化丹参中的丹参酮ⅡA

目的:优化用超临界CO2从丹参中萃取丹参酮ⅡA的工艺条件,并建立纯化丹参酮ⅡA的柱层析法。方法:以HPLC法测定丹参酮ⅡA的含量。采用正交试验优化超临界CO2萃取丹参酮的条件,考察夹带剂用量、萃取压力、萃取温度和分离温度对提取效果的影响。用100~200目的中性氧化铝柱层析,以苯进行洗脱,收集相关流份,减压回收溶剂后经无水乙醇重结晶得到丹参酮ⅡA晶体。结果:超临界CO2萃取丹参酮ⅡA的最优条件为:夹带剂用量120 ml,萃取压力20 MPa,萃取温度50℃,分离温度35℃。柱层析后重结晶得到纯度为93.49%的丹参酮ⅡA晶体。结论:超临界CO2萃取丹参酮具有操作简便、方法可靠、切实可行、无有机溶剂残留的优点,结合柱层析法可获得高纯度晶体。     

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.