苦参康复搽剂的气相指纹图谱研究

目的建立复方中药苦参康复搽剂的气相(GC)指纹图谱,以对其进行质量控制。方法采用ZHD-2007-1306(OV-1701)(30 m×0.32 mm×0.6μm)为色谱柱,FID检测器,进样口温度为280℃,起始柱温为100℃,程序升温的方法建立苦参康复搽剂GC指纹图谱,采用"中药色谱指纹图谱相似度评价软件"对10批搽剂进行相似度评价,并指认了其中的特征色谱峰。结果所建立的苦参康复搽剂GC指纹图谱的精密度、重复性、专属性和稳定性均符合要求;10批搽剂的指纹图谱的相似度为0.958～0.984;标定共有指纹图谱峰为16个,指认其中一个峰为苍术中的苍术素。结论所得到的GC指纹图谱可为提高苦参康复搽剂整体的质量控制方法提供依据。     

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。     

羌活和独活药材气相色谱指纹图谱的建立及鉴别

目的为羌活和独活药材的鉴别提供科学依据。方法采用气相色谱(GC)-氢火焰离子化检测法。色谱柱:DB-1毛细管柱(30 m×0.25 mm×0.25μm);程序升温:起始柱温50℃,8℃.min-1升至85℃保持12 min,4℃.min-1升至155℃保持18 min,12℃.min-1升至250℃保持5 min;气化室温度:250℃;载气:氮气;流速:1.2 mL.min-1;进样量:1.0μL;分流比:10∶1;检测器温度:270℃。结果建立了羌活和独活药材的GC指纹图谱;对不同产地药材分别进行了相似度计算;指纹图谱和相似度计算结果显示,羌活和独活药材挥发油含量具有明显区别。结论本方法可用于羌活和独活药材的定性鉴别。     

五指毛桃高效液相色谱指纹图谱研究

目的建立五指毛桃药材HPLC指纹图谱,为科学、合理地实现质量控制提供更为可靠的方法。方法采用高效液相色谱法,以Waters Xbridge C18柱(4.6 mm×250 mm,5μm)为色谱柱;甲醇-0.1%磷酸为流动相梯度洗脱;检测波长为250 nm;流速为0.8 m L·min-1;柱温30℃。结果建立了五指毛桃药材的指纹图谱,标示了22个共有峰,并采用中药色谱指纹图谱相似度评价系统(2004A版)对10批五指毛桃药材HPLC指纹图谱进行了相似度评价,各五指毛桃样品指纹图谱与对照指纹图谱相似度均较高。结论所用方法简便、准确、重复性好,为有效地控制与评价五指毛桃的质量提供了科学依据。     

白芍药材主根与根茎的HPLC指纹图谱比较研究

目的:建立白芍药材主根与根茎的高效液相色谱(HPLC)指纹图谱,并比较两者的异同。方法:色谱柱为Phenomenex C18,流动相为乙腈-0.1%磷酸溶液(梯度洗脱),流速为1.0 m L/min,检测波长为230 nm,柱温为30℃,进样量为10μL。以芍药苷为参照,测定白芍药材主根与根茎部分的HPLC图谱,采用《中药色谱指纹图谱相似度评价系统》(2012版)进行共有峰指认和相似度评价。结果:白芍药材主根与根茎的HPLC图谱有9个共有峰;白芍药材主根与根茎之间相似度>0.9。结论:该研究所建指纹图谱可为白芍药材的鉴别和质量评价提供参考,白芍药材主根与根茎有效成分一致,差异性较小。     

双波长HPLC法建立栀子药材的指纹图谱

目的采用双波长HPLC法建立栀子药材指纹图谱。方法采用Waters Symmetry C_(18)(250mm×4.6mm,5"m)色谱柱;乙腈-水梯度洗脱;流速:0.8mL·min~(-1);柱温:30℃。结果以栀子苷为参照物,用HPLC法测定不同产地10批栀子药材的指纹图谱,分离度达到1.5,用中药色谱指纹图谱相似度评价系统,计算出10批栀子指纹图谱的相似度,均在0.940~1.000。结论该方法具有良好的精密度、稳定性和重复性,可更好地控制栀子药材的内在质量。     

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。     

三七药材、三七三醇皂苷及其制剂的特征图谱质量控制研究

目的:建立三七药材、三七三醇皂苷(PTS)及其制剂三七通舒胶囊(肠溶微丸)的HPLC特征图谱,为三七药材、提取液、PTS和制剂的质量控制以及工艺评价提供有效的方法。方法:采用Waters Symetry Shield C18(4.6 mm×250 mm,5μm)色谱柱,以乙腈-水为流动相,梯度洗脱,流速1.0 mL.min-1,检测波长203 nm,柱温40℃;对多批三七药材、PTS、中间体及其制剂进行HPLC测定和方法学考察,采用中药色谱指纹图谱相似度评价系统2004A版对其进行相似度分析。结果:所建立的HPLC特征图谱能分离三七药材、PTS、中间体及制剂的各组分,具有较好的精密度、重复性和稳定性;经相似度评价,确定各组分平均相似度大于0.9。结论:采用HPLC建立的特征图谱方法简单,重复性良好,能充分展示三七药材、PTS、中间体及其制剂的物质组成以及有效物质群的变化,可用于三七药材、PTS及其制剂的质量控制和工艺评价。     

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。     

湘产菝葜高效液相色谱指纹图谱的研究

目的建立湘产菝葜的高效液相色谱指纹图谱。方法采用Ultimate XB-C18(4.6 mm×250 mm,5μm)色谱柱,以乙腈-0.1%磷酸溶液为流动相,进行梯度洗脱,体积流量1 m L·min-1,柱温35℃,检测波长290 nm,运用"中药色谱指纹图谱相似度评价系统2004A版"软件处理图谱。结果 10批菝葜药材HPLC指纹图谱共标定16个特征峰,10批样品的相似度均>0.9。结论本方法操作简便且重现性好,可用于湘产菝葜药材的质量控制。     

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.