超临界CO_2萃取与水蒸气蒸馏法提取太子参挥发油化学成分气质联用研究

目的:分析比较采用超临界CO2流体萃取法与水蒸气蒸馏法提取的太子参提取物中挥发性化学成分的异同。方法:使用水蒸馏提取法和超临界CO2萃取技术从太子参中提取挥发性成分,用归一化法测定其百分含量。用气相色谱-质谱(GC-MS)计算机联用技术分离鉴定其中的化学组成。结果:太子参超临界CO2流体萃取物中初步鉴定了33种成分,主要成分为:亚油酸乙酯(28.70%)、n-十六酸(23.12%)、3-糠醇(5.51%)等;水蒸气蒸馏法提取挥发油初步鉴定了17种成分,主要成分为2-丙基呋喃(22.45%)、3-糠醇(19.78%)、3-乙基-3-甲基戊烷(19.47%)。结论:2种方法提取的挥发油化学成分差异较大,超临界CO2流体萃取法提取的挥发油能更真实、全面地反映太子参药材中的化学成分。     

不同方法提取的香椿子挥发油的气质联用成分分析

目的:采用超临界 CO_2流体萃取法及水蒸气蒸馏法从香椿籽中提取挥发油,用气相色谱-质谱联用技术对其化学成分进行分析。方法:采用超临界 CO_2流体萃取法与水蒸气蒸馏法从香椿籽中提取挥发油,用归一化法测定其百分含量。用气相色谱-质谱法对化学成分进行鉴定。色谱条件:DB-5毛细管柱(30 m×0.25 mm,0.25μm);程序升温:初始温度60℃,保持5 min,以4℃·min~(-1)升至180℃,保持10 min,再以15℃·min~(-1)升至260℃,保持50 min;分流进样,分流比50:1;进样口温度280℃。结果:超临界 CO_2流体萃取法提取的挥发油共鉴定了63种成分,占挥发油总成分的88%以上;水蒸气蒸馏法提取挥发油共鉴定了50种成分,占挥发油总成分的94%以上。结论:超临界 CO_2流体萃取法提取的挥发油能更真实、全面地反映药材中的化学成分。     

超临界二氧化碳流体萃取法与水蒸气蒸馏法提取广西产五月艾挥发油化学成分

目的分析广西产五月艾挥发油的主要化学成分。方法分别采用超临界二氧化碳（CO2）流体萃取法和水蒸气蒸馏法提取广西产五月艾挥发油,并通过GC MS技术对其进行分析,面积归一化法测定计算各成分的相对百分含量。结果超临界CO2流体萃取法提取的挥发油共鉴定出30种成分,占挥发油总成分的77.69 %;水蒸气蒸馏法提取的挥发油共鉴定出48种成分,占挥发油总成分的86.54 %。结论两种提取方法得到的五月艾挥发油组分与含量差别较大。     

超临界CO2流体萃取法与水蒸气蒸馏法提取黑松松塔挥发油化学成分的研究

目的比较两种不同提取方法所得的黑松松塔挥发油的挥发性化学成分。方法分别采用超临界CO2流体萃取(SFE)和水蒸气蒸馏(SD)提取黑松松塔的挥发油。运用气相色谱-质谱联用法分离和分析两挥发油的挥发性化学成分。结果超临界CO2流体萃取法提取的挥发油共鉴定出43种成分,占挥发油总成分的60.78%;水蒸气蒸馏法提取的挥发油共鉴定出37种成分,占挥发油总成分的86.16%;结论采用两种方法提取黑松松塔挥发油组分与含量差别较大,且SFE法的提取率低于SD法。     

岷当归挥发油提取方法及其化学成分研究

目的分析岷当归挥发油的主要化学成分。方法分别采用超临界CO2流体萃取法(SFE)和水蒸气蒸馏法(SD)提取岷当归的挥发油,并通过GC-MS技术对其进行分析,面积归一化法测定计算各成分的相对百分含量。结果水蒸气蒸馏法提取的挥发油共鉴定出73种成分,占挥发油总成分的58.99%;超临界CO2流体萃取法提取的挥发油共鉴定出25种成分,占挥发油总成分的63.43%,相同成分13种。结论 2种提取方法得到的岷当归挥发油组分与含量差别较大,该实验结果为了解其挥发性成分及进一步开发应用提供依据。     

三种方法提取防风挥发油的气质联用成分分析

目的对3种不同方法提取的防风挥发油化学成分进行分析。方法采用水蒸气蒸馏法（SD）、溶剂提取法（SX）、超临界CO2流体萃取法（SFE-CO2）提取防风挥发油,用气相-质谱（GC-MS）法对化学成分进行鉴定。结果水蒸气蒸馏法提取挥发油共鉴定了13种化学成分;溶剂提取法提取的挥发油共鉴定了18种化学成分;超临界CO2流体萃取法提取的挥发油共鉴定了21种化学成分。结论超临界CO2流体萃取法提取的挥发油更全面地反映药材中的化学成分。     

超临界CO2提取的百合挥发油化学成分的GC-MS分析

目的 研究百合挥发油化学成分。方法 采用超临界CO₂提取方法,GC-MS联用技术鉴定百合挥发油成分,并用峰面积归一化法测定各成分的相对百分含量。结果 超临界CO₂流体萃取法提取的挥发油共鉴定出50种成分,占挥发油总成分的72.96%。结论 超临界提取百合挥发油成分多、效率高,与水蒸气蒸馏提取出的挥发油成分有差异。     

GC-MS分析不同水蒸气蒸馏法提取的莲子心挥发油成分

目的 分析比较不同水蒸气蒸馏法所得莲子心的挥发油成分。方法 分别采用水蒸气蒸馏装置(SDA)和挥发油测定装置(EODA)的水蒸气蒸馏法提取莲子心挥发油,GC-MS分离鉴定挥发油成分,峰面积归一化法计算百分含量。结果 采用SDA法,鉴定出29种成分,占挥发油总量91.56%,主要成分为棕榈酸(28.96%)、9,17-十八碳二烯醛(19.99%)和亚油酸(11.94%)等;采用EODA法,鉴定出18种成分, 占挥发油总量77.96%,主要成分为棕榈酸(18.98%)、肉桂酸龙脑酯(12.58%)、2-甲氧基-4-乙烯苯酚(8.25%)等。结论 两种水蒸气蒸馏法所得挥发油成分存在较大差异,且SDA较EODA更适合于提取挥发油。     

不同方法提取的佛手挥发油气相色谱-质谱分析结果比较

目的：比较分析水蒸气蒸馏法与超临界流体萃取法（SFE）提取佛手挥发油的化学成分和相对含量。方法：运用气相色谱-质谱技术（GC-MS），结合计算机检索对其化学成分进行分离和鉴定，用色谱峰面积归一化法计算各组分的相对含量。结果：水蒸气蒸馏法中鉴定出18种化学成分，SFE中鉴定出16种化学成分，二者的主要成分均含有D-柠檬烯，相对含量前者为57．87％，后者为81．18％；水蒸气蒸馏法提出成分中还含有25．12％的（＋）-2-蒈烯，而SFE法未检测到该成分。结论：两种提取方法成分结果有所不同，但都含有主要成分D-柠檬烯，含量以SFE法为高。     

超临界CO_2流体萃取法和水蒸气蒸馏法对辛夷挥发油萃取率和萃取质量的比较

目的通过对比超临界CO_2流体萃取法和水蒸气蒸馏法两种方法对辛夷挥发油的萃取率和挥发油的质量,对辛夷中挥发油的最佳的提取方法提供理论依据。方法采用水蒸气蒸馏法和超临界CO_2流体萃取技术提取辛夷的挥发油,利用三因素三水平正交实验法来确定辛夷挥发油的最佳提取工艺,以萃取率和挥发油质量作为评价指标。结果水蒸气蒸馏法确定的最佳提取条件为:料液比1:10,浸泡时间1h,提取时间2h,平均提取率为1.376%;超临界CO_2流体萃取技术确定的最佳提取条件为:温度35℃,压力14mPa,提取时间1h,平均萃取率为3.948%。结论从两种提取方法的实验结果分析,超临界CO_2流体萃取法在辛夷挥发油提取率方面要优于水蒸气蒸馏法,在最佳实验条件下的超临界流体的萃取率是水蒸气蒸馏法的3倍。     

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.