北柴胡气相指纹图谱数据的化学计量学分析

目的 对北柴胡挥发性成分的气相指纹图谱进行化学计量学研究,提取出指纹图谱中的特征数据信息。方法 运用Agilent 7890A气相色谱仪,安捷伦HP-5毛细管气相色谱柱(30 m×0.25 mm,0.25 µm),载气为氮气,流速为1.03 mL·min-1,FID检测温度为280 ℃,对不同产地北柴胡样品进行分析。运用指纹图谱处理软件对指纹图谱数据进行相似度分析、聚类分析及主成分分析。结果 建立了北柴胡挥发性成分的指纹图谱共有模式,获得了28个共有峰。依据化学计量学分析,将样品分成了3类。结论 结果表明化学计量学分析方法适用于指纹图谱数据的分析,可为定量研究提供依据,有助于柴胡药材的质量评价研究。     

不同采收期苍耳草的指纹图谱研究

目的:研究不同采收期苍耳草的指纹图谱,建立稳定、可重复的苍耳草质量控制手段。方法:运用HPLC色谱技术建立不同采收期不同产地苍耳草的指纹图谱。结果:通过比较14批苍耳草和2批苍耳子药材样品HPLC图谱,建立其对照指纹图谱,并以共有模式为参照,通过《中药指纹图谱相似度计算软件》计算,得到色谱指纹图谱模拟图谱及相似度计算结果。除1号、15号和16号与其他批次样品相似度不高外,其他批次相似度较大,但是其主要成分在含量方面存在一定的差异,与药材采自不同采收期有关。结论:本文建立了苍耳草的HPLC指纹图谱,为苍耳草质量标准的建立提供了试验依据。     

水曲柳HPLC指纹图谱研究

目的:建立水曲柳药材的高效液相(HPLC)指纹图谱,为水曲柳的鉴别及质量控制提供依据。方法:对不同产地、不同采集时间的水曲柳药材皮中的香豆素成分进行指纹图谱研究。结果:HPLC指纹图谱中峰的分离度均好,共得到10个共有峰;10批样品的相似度较好。结论:所建立的指纹图谱可用于水曲柳药材的鉴定及质量评价。     

白芷挥发油GC指纹图谱研究

目的:建立白芷挥发油成分的 GC 指纹图谱。方法:SE-30毛细管气相色谱柱(30 m×0.25 mm×0.25 μm),FID 检测器,程序升温为70℃(5 min),以2℃·min~(-1)的速度线性升温至220℃(5 min)。结果:依据21批药材的指纹图谱数据进行聚类分析,将样品分为4类,选定其中10批优质样品建立共有模式。相似度分析结果表明,第Ⅰ类和第Ⅱ类样品为优质药材,第Ⅲ类样品质量一般,第Ⅳ类样品为伪品。结论:本测定方法为白芷药材的质量评价提供了科学依据。     

蒙药山川柳的HPLC指纹图谱建立、相似度评价和聚类分析

目的:建立蒙药山川柳的高效液相色谱(HPLC)指纹图谱,并进行相似度评价和聚类分析。方法:采用HPLC法,色谱柱为Agilent ODS C_(18),流速为1.0 m L/min,流动相为甲醇-水(梯度洗脱),检测波长为335 nm,柱温为30℃,进样量为10μL。以槲皮素峰为参照,生成10批药材样品的HPLC指纹图谱;采用《中药色谱指纹图谱相似度评价系统》(2004 A版)进行相似度评价,确定共有峰;采用SPSS 17.0软件对10批药材样品进行聚类分析。结果:10批药材样品的HPLC指纹图谱有13个共有峰,相似度大于0.95,并指认了槲皮素和山柰酚这2个共有峰。聚类分析结果显示,10批药材样品可聚为两类,S8聚为一类,其余批次聚为一类。结论:所建HPLC指纹图谱、相似度评价和聚类分析结果可为山川柳药材的质量控制提供依据。     

乌拉尔甘草的UPLC指纹图谱研究

目的:建立乌拉尔甘草的超高效液相色谱(UPLC)指纹图谱。方法:采用UPLC法。色谱柱为Waters CORTECS UPLC C18,流动相为乙腈-0.1%甲酸溶液(梯度洗脱),流速为0.3 m L/min,检测波长为254 nm,柱温为30℃,进样量为1μL。以甘草酸为参照,测定27批药材样品的UPLC图谱,采用《中药色谱指纹图谱相似度评价系统》(2004 A版)进行相似度评价,确定共有峰,并对27批药材样品进行聚类分析。结果:27批药材样品的UPLC图谱有20个共有峰;除S2、S4、S19、S21、S22、S24药材样品的相似度小于0.90外,其余21批药材样品相似度均大于0.90;经验证,该21批药材样品UPLC图谱与对照图谱具有较好的一致性。27批药材样品可聚为3类,S24为Ⅰ类,S2、S4、S12、S19、S21、S22为Ⅱ类,其余为Ⅲ类。结论:该研究所建指纹图谱可为甘草的质量评价提供参考。     

不同产地多伞阿魏挥发油成分GC-MS指纹图谱研究

目的建立多伞阿魏药材的GC-MS指纹图谱。方法采用水蒸气蒸馏法提取8个产地44份多伞阿魏挥发油,通过GC-MS分析其成分。运用中药色谱指纹图谱相似度建立共有模式,以2种方法计算相似度评价图谱的相似性,同时利用聚类分析法和主成分分析法分析结果。结果建立了多伞阿魏挥发油GC-MS指纹图谱分析方法;对44份多伞阿魏挥发油样品进行了分析,确立了12个共有峰。GC-MS指纹图谱的相似度>0.90的有37个。44份多伞阿魏药材的挥发油可通过系统聚类归为2类,该结果与指纹图谱的相似度分析结果非常相似,不同产地多伞阿魏药材的挥发油相似度较高。主成分分析表明愈创木醇在多伞阿魏挥发油的质量控制中起着比较重要的作用。结论该方法简便、准确、重现性好,可用于多伞阿魏药材的质量综合评价。     

黔产钩藤HPLC指纹图谱的研究

目的收集贵州十个不同产地的钩藤药材为样品,建立钩藤药材高效液相色谱(HPLC)指纹图谱,以便更全面地评价黔产钩藤药材的内在品质,为黔产钩藤药材的质量控制提供客观依据。方法色谱柱为Kamsial C18色谱柱(4.6×250mm,5μm),流动相为甲醇-0.05%氨水的梯度洗脱,流速为1.0mL/min,紫外检测波长为245nm。结果将16个样品色谱峰作为钩藤特征色谱峰,运用中国药典委员会推荐使用的"中药色谱指纹图谱相似度评价软件"对指纹图谱的相似度进行评价,十批样品的相似度在0.880~0.9960之间。结论 90%药材指纹图谱与共有模式相似度在0.9以上,所建立的HPLC指纹图谱共有模式可作为钩藤药材质量综合评价的参考方法。     

竹叶柴胡药材HPLC指纹图谱研究

目的:建立竹叶柴胡药材的高效液相色谱指纹图谱。方法:色谱柱为Agilent C1(8250mm×4.6mm,5μm),流动相为乙腈-0.2%磷酸水溶液(梯度洗脱),流速为1.0mL·min-1,柱温为30℃,检测波长为203nm。结果:建立了竹叶柴胡药材的指纹图谱,确定了22个共有峰,各峰的相似度均>0.800。结论:该指纹图谱建立方法简单、重复性好,可为竹叶柴胡药材的鉴别和质量评价提供参考。     

芫花挥发油成分GC指纹图谱研究

目的建立芫花挥发性成分的GC指纹图谱,为芫花药材的鉴别及品质控制提供依据。方法采用GC色谱法对所采集的不同地区的芫花药材进行指纹图谱研究,建立GC指纹图谱共有模式,并进行聚类分析和相似度比较。结果 GC指纹图谱对芫花中主要成分均得到较好分离,根据聚类分析和相似度分析处理结果,不同地区的芫花药材指纹图谱相似度存在一定差别。结论该法为芫花药材的质量评价提供科学依据。     

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.