延胡索HPLC指纹图谱研究

目的建立延胡索药材HPLC指纹图谱,为全面评价延胡索质量提供参考依据。方法色谱柱为Agilent ZORBAX Eclise XDB-C18(150mm×4.6mm,5μm);柱温为25℃;流动相为甲醇-0.1mL·L~(-1)磷酸溶液,梯度洗脱;流速为1.0mL·min~(-1);检测波长为280nm。采用《中药色谱指纹图谱相似度评价系统A版》对10批延胡索药材指纹图谱进行分析。结果确定了11个共有峰,精密度、稳定性和重复性实验中各共有峰相对保留时间的RSD值均小于2.0%,相对峰面积的RSD值均小于5.0%,建立了延胡索药材HPLC指纹图谱,通过分析得到10批延胡索药材指纹图谱的相似度均大于0.85。结论该方法简单易行,重复性较好,可作为延胡索药材的质量评价方法。     

穿山龙超高效液相色谱特征指纹图谱的研究

目的建立穿山龙药材的超高效液相色谱(UPLC)特征指纹图谱分析方法。方法采用Agilent Poroshell 120Bonus-RP色谱柱(50 mm×3.0 mm,2.7μm);流动相:乙腈–水,梯度洗脱;体积流量:0.8 m L/min;检测波长:203 nm;柱温:25℃;进样量:10μL。应用相似度分析软件建立穿山龙药材指纹图谱的共有模式,并对色谱峰进行指认。结果建立了穿山龙药材的UPLC特征指纹图谱共有模式,标定了14个共有峰,指认了其中3个共有峰,10批穿山龙药材的相似度为0.9以上。通过聚类分析,将13批穿山龙药材聚为4类。结论该方法快速,可用于评价穿山龙药材质量。     

鸦胆子药材水溶性成分的HPLC指纹图谱检测方法

目的建立鸦胆子药材水溶性成分指纹图谱检测方法。方法采用汉邦BDS-C18色谱柱(250 mm×4.6 mm,5μm),用反相色谱法进行分离,以乙腈-磷酸水溶液(pH 3.0)进行线性梯度洗脱,检测波长:280 nm,柱温:40℃,进样量:10μL。以没食子酸峰作为内参照峰。结果测定20批不同产地的鸦胆子药材,共标定11个共有峰。通过中药色谱指纹图谱相似度评价系统(2009年版)进行评价,20批鸦胆子药材水溶性指纹图谱之间相似度均在0.95以上。易伪品女贞子水溶性成分与鸦胆子水溶性成分共有模式相似度为0.562。结论建立的指纹图谱检测方法可为鉴别鸦胆子药材真伪和药材质量控制提供试验依据。     

川芎高效液相指纹图谱的研究

目的:用高效液相色谱法建立川芎的指纹图谱.方法:采用Zorbax SB-C18柱(250 mm×4.6 mm,5μm)色谱柱,甲醇和水梯度洗脱,检测波长323 nm,使用"计算机辅助相似度评价软件"进行数据处理,对不同批药材指纹图谱的相似度进行比较分析.结果:精密度和重复性试验中各共有峰、相对峰面积的RSD均小于5%,符合有关规定,不同批号川芎药材的指纹图谱相似度较好.结论:方法准确、重复性好,为川芎的质量控制提供了依据.     

山橿药材HPLC指纹图谱研究

目的利用RP-HPLC法对山橿药材进行指纹图谱进行了研究,为科学评价与有效控制山橿药材质量提供新方法。方法采用AgilentHC-C18色谱柱(150mm×4.6mm,5μm),以甲醇-水(60%～100%)线形梯度洗脱,体积流量1.0mL/min,柱温30℃,在296nm波长下进行检测,记录55min的色谱图。测定10批药材的色谱图,建立山橿的指纹图谱。结果山橿药材有11个共有峰,多数峰可以达到较好的分离,方法学考察表明该方法具有较好的精密度、重复性和稳定性,各色谱图相对保留时间RSD小于0.50%,相对峰面积符合指纹图谱要求。结论建立的共有指纹图谱检测标准可以作为山橿质量评价的和品种鉴别的重要依据。     

山楂药材黄酮类成分HPLC指纹图谱的研究

目的:采用高效液相色谱法建立山楂药材黄酮类成分指纹图谱.方法:以Licrospher C18 ODS柱(200mm×4.6mm,5μm)为色谱柱,采用水和乙腈溶液梯度洗脱,流速0.9mL·min-1,检测波长210nm.结果:精密度和重复性试验中,峰面积大于10%的共有峰的相对峰面积的RSD均小于5%,符合<中药注射剂色谱指纹图谱实验研究技术指南(试行)>中相关要求.结论:本方法可作为控制山楂药材内在质量的标准.     

道地药材黔党参的HPLC指纹图谱研究

目的:建立道地药材黔党参的指纹图谱研究方法,为其质量控制提供理论依据。方法:采用高效液相色谱法。色谱柱为依利特-C18(250mm×4.6mm,5μm),流动相为乙腈-0.2%冰醋酸水溶液(梯度洗脱),流速为0.8ml/min,柱温为30℃,检测波长为270nm。结果:所测10批黔党参样品有13个共有峰,共有峰峰面积的RSD为49.67%～100.93%,峰面积比值的RSD为40.86%～127.97%;共有峰相对保留时间为0.441～1.675,相对保留时间的RSD为0.11%～1.50%;该方法具有良好的稳定性和重复性。结论:所建黔党参HPLC指纹图谱分析方法可较全面地反映该药材中化学成分的信息,可为该药材的质量控制提供理论依据。     

鸡骨草药材指纹图谱研究

目的建立鸡骨草药材的指纹图谱。方法采用RP-HPLC高效液相色谱法,Phenomenex-ODS色谱柱(250 mm×4.0 mm,5μm),甲醇-0.5%冰醋酸溶液,梯度洗脱,流速1.0 ml/min,检测波长270 nm。结果建立了鸡骨草药材指纹图谱共有模式,显示5个共有峰,指认了相思子碱1个特征峰。结论 HPLC指纹图谱中各峰分离度较好,方法具有较好的精密度、重现性和稳定性,符合指纹图谱的要求,可用于鸡骨草药材质量控制。     

射干药材的HPLC指纹图谱研究

目的:研究不同产地射干药材的HPLC指纹图谱,为控制射干药材质量提供依据.方法:采用Agilent Zorbax SB-C18色谱柱(4.6 mm×250 mm,5 μm);乙腈-0.4%冰醋酸水溶液为流动相,梯度洗脱;流速1 mL·min-1;检测波长269 nm.结果:15个不同产地射干药材的指纹图谱有14个共有峰,通过与对照品的保留时间比较,确定了其中7个峰.结论:虽然不同产地药材指纹图谱具有一定差异,HPLC指纹图谱仍可以用作射干药材的质量控制.     

黑草药材HPLC指纹图谱的研究

目的:以不同产地的黑草为研究对象,建立黑草药材的HPLC指纹图谱,为科学评价和有效控制黑草药材的质量提供科学依据。方法:以木犀草素成分为参照峰,采用HPLC法建立黑草药材的指纹图谱;色谱柱:Agilent Extend-C18(250 mm×4.6mm,5μm),流动相:乙腈与0.7%冰醋酸,梯度洗脱;流速:1.0 mL·min-1;检测波长:350 nm;柱温:35℃;进样量:10μL。结果:10批次黑草药材中共有12个指纹图谱峰,经相似度计算,整体相似性好。结论:本文建立的指纹图谱有较强的针对性,为黑草药材的研究以及制定黑草药材的质量控制标准提供科学依据。     

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.     

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.