人参须药材质量标准的研究

目的 建立人参须药材质量标准。方法 采用经验、显微鉴别法对该药材性状、显微特征进行描述;按照中国药典2015年版四部通则相关方法,对药材水分、总灰分进行了测定;采用薄层色谱法,分别以人参对照药材和人参皂苷（Rb₁、Re、Rf和Rg₁）对照品为对照,对该药材的脂溶性成分及皂苷类成分进行定性鉴别;采用HPLC,以人参皂苷Re、Rg₁、Rb₁和Rb₂为对照,采用Sepax BR-C₁₈色谱柱（4.6 mm×250 mm,5 μm）,乙腈-水为流动相,进行梯度洗脱,在203 nm波长下对各皂苷成分进行定量分析,建立该药材中皂苷类成分的含量测定方法。结果 该药材性状、显微、薄层鉴别方法具有较强的专属性,水分平均值为11.0%,总灰分平均值为4.6%,人参皂苷Re与Rg₁总含量平均值为0.86%,Rb₁含量平均值为0.54%,Rb₂含量平均值为0.31%。结论 本研究依据实验结果和传统经验,同时结合了吉林省人参须药材的生产现状及药用企业的应用情况,可以作为人参须药材的质量标准。     

珠子参薄层色谱鉴别方法的研究

目的建立和完善珠子参薄层鉴别方法。方法通过对薄层制样方法及色谱条件的考察,探索珠子参适宜的薄层鉴别条件。结果供试品溶液制备采用甲醇超声提取、水饱和正丁醇萃取,以竹节参皂苷Ⅳa和人参皂苷Ro作为对照品,展开剂为正丁醇-乙酸乙酯-甲醇-甲酸-水(5?10?0.5?0.3?3.5)上层液,10%硫酸乙醇溶液喷雾,105℃加热,紫外光(365nm)下检视。结论该色谱条件下珠子参主要成分分离度好,斑点清晰,专属性强,可用于珠子参药材的鉴别。     

祛风活络丸中5种成分的薄层色谱鉴别

目的：建立祛风活络丸的薄层色谱鉴别方法。方法：采用适当的萃取方法，萃取后用薄层色谱法鉴别祛风活络丸中的马钱子、川乌、川芎、独活、羌活等5种成分。结果：薄层色谱鉴别的5种供试品色谱叶，在与对照品或对照药材色谱相应的位置上，均能显示相同颜色的斑点。结论：利用薄层色谱法可对祛风活络丸中的5种成分进行鉴别。     

对复方丹参片鉴别(2)的商榷

目的：改进原有的薄层鉴别方法，以提高鉴别的专属性。方法：将硅胶G薄层板改为高效板，增加三七对照药材作为对照物，并对所得的薄层色谱进行扫描，λs=530nm;λR=650nm得到相应的扫描轮廓图。结果：所得薄层色谱分离效果好，供试品的薄层色谱及薄层色谱扫描轮廓图与三七对照药材的相一致，而与同三七薄层行为相近的人参不同，从而提高了该项鉴别的专属图与三七对照药材的相一致，而与同三七薄层行为相近的人参不同，从而提高了该项鉴别的专属性。结论：该方法具有可行性，可供修订标准时参考。亦可在制订含三七的成方制剂的薄层鉴别时借鉴。     

白癜风胶囊的薄层色谱鉴别

目的: 建立白癜风胶囊的薄层色谱鉴别方法.方法: 采用适当的提取方法,提取后用薄层色谱法鉴别白癜风胶囊中的补骨脂、蒺藜、川芎、当归、红花、香附6种成分.结果: 薄层色谱法鉴别的6种供试品色谱中,在与对照品或对照药材色谱相应的位置上,均能显示相同颜色的斑点.结论: 利用薄层色谱法可对白癜风胶囊中的6种成分进行鉴别.     

灯盏细辛药材的薄层色谱鉴别

目的 建立灯盏细辛的薄层色谱鉴别方法.方法 采用适当的提取方法,提取后用薄层色谱法鉴别灯盏细辛中的3,5-2-O-咖啡酰奎宁酸、野黄芩苷、1,3-O-二咖啡酰奎宁酸、咖啡酸4种成分.结果供试品溶液色谱中,在与对照品溶液或对照药材溶液色谱相应的位置上,均能显示相同颜色的斑点.结论 薄层色谱方法简单、重复性好、专属行强,可对灯盏细辛药材进行定性鉴别.     

连桂清心片的薄层色谱鉴别

目的：建立连桂清心片中甘草和黄连的薄层色谱鉴别方法,为连桂清心片质量标准提供依据。方法分别采用不同的方法处理样品,分别以甘草酸铵、盐酸小檗碱为对照品,以甘草、黄连为对照药材,在硅胶 G 薄层板上点样,以适宜的展开剂展开,取出,晾干,显色剂显色。结果在薄层色谱中能够检出连桂清心片中的甘草、黄连,连桂清心片供试品溶液色谱中,与对照品或对照药材色谱相对应位置,色谱斑点清晰,荧光斑点显示相同的颜色,分离良好且阴性对照无干扰,均能有效提供连桂清心片的鉴别特征。结论建立的两种薄层色谱鉴别方法简便,专属性强,重现性好,可用于连桂清心片的薄层定性鉴别。     

大蒜药材的薄层鉴别方法研究

目的建立大蒜药材的薄层鉴别系统。方法以蒜氨酸和精氨酸为对照品,采用灭酶处理,对大蒜药材进行薄层鉴别,并考察不同展开系统、不同点样量、不同薄层板、不同检视方式、不同温度、不同湿度对大蒜药材薄层色谱的影响。结果以蒜氨酸和精氨酸为对照品,正丁醇-冰醋酸-水(4︰1︰1)为展开系统,大蒜药材薄层鉴别特征明显,专属性强。结论该方法可行,重复性好,可作为大蒜药材的薄层鉴别方法。     

三七跌打膏的薄层色谱鉴别

目的：建立三七跌打膏的质量控制方法。方法：采用薄层色谱法以人参皂苷Rb1、人参皂苷Rg1及三七皂苷R1、士的宁、马钱子碱、冰片为对照品,鉴别三七、马钱子、冰片。结果：薄层色谱中斑点清晰、分离度好,阴性无干扰。结论：方法简便,准确,重现性好。可用于控制三七跌打膏的质量。     

愈骨胶囊的薄层色谱鉴别

目的建立愈骨胶囊的薄层色谱(TLC)鉴别方法。方法对处方中血竭、大黄、三七、骨碎补的薄层鉴别方法进行改进,新建没药的薄层鉴别方法。结果薄层色谱中均能检出血竭、大黄、三七、没药药材及大黄素、三七皂苷R1、柚皮苷,薄层色谱斑点清晰,阴性对照品溶液均无干扰,且专属性强、重现性好。结论所建立的薄层色谱方法可用于该制剂的质量控制。     

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.     

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.