牡丹皮HPLC指纹图谱的研究

目的　建立牡丹皮的HPLC指纹图谱,为科学评价与有效控制牡丹皮质量提供新方法。方法　采用HPLC法测定了10个不同产地牡丹皮样品,色谱条件为Shim -packC18(15 0mm×4 .6mm,5 μm),流动相为乙腈-水梯度洗脱,流速0 .8ml·min-1,检测波长2 30nm,柱温为2 5℃。结果　本研究建立的分析方法有较好的重复性,不同产地的牡丹皮药材色谱峰相对保留时间一致。结论　为牡丹皮药材的质量控制提供了科学的依据。     

大蓟小蓟的高效液相色谱指纹图谱研究

目的:建立反相高效液相色谱法研究大蓟、小蓟黄酮类化合物的指纹图谱,并以此作为鉴别两者的依据。方法:色谱柱:Symmetry C_(18)柱(3.9mm×150mm,5μm);以甲醇和水为流动相进行梯度洗脱,流速:1mL·min~(-1);检测波长:330 nm;柱温:30℃;进样量:10 μL。结果:不同产地的大蓟、小蓟药材的指纹图谱具有稳定、特征的指纹图谱。结论:可以利用液相色谱的特征峰控制大蓟、小蓟药材的质量,并准确地鉴别这两味药材。     

HPLC指纹图谱对比研究川芎和当归的化学成分

目的对比川芎、当归药材水溶性和脂溶性成分的HPLC指纹图谱。方法分别收集12批川芎、10批当归药材,采用HPLC建立指纹图谱;色谱条件为LUNA C18色谱柱(150 mm×4.6 mm,5μm),流动相为甲醇-1%冰醋酸,进行梯度洗脱,检测波长280 nm,流速1.0 mL.min-1,柱温35℃。结果分别建立了川芎、当归药材水溶性和脂溶性成分的HPLC指纹图谱共有模式。结论所建立的指纹图谱可作为区分川芎、当归药材的参考依据。     

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。     

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。     

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。     

不同产地桑白皮HPLC的指纹图谱的研究

目的 建立简单可行的桑白皮药材指纹图谱方法.方法 采用高效液相色谱法,Agilent Extend-C18(4.6 mm×250 mm,5μm)色谱柱,流动相:以乙腈-0.2%甲酸进行梯度洗脱,流速:1 mL·min-1,柱温:30℃,检测波长:280 nm,进样量为10μL.结果 用梯度洗脱得到的色谱图中各色谱峰分离较好,达到指纹图谱分析的效果.结论 该方法重复性好、检测方法简便,可为桑白皮指纹图谱的质量控制提供依据.     

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。     

藏药蕨麻高效液相色谱指纹图谱研究

目的建立蕨麻药材HPLC指纹图谱分析方法。方法采用Kromasil C18(4.6 mm×250 mm,5μm)色谱柱,以乙腈-水梯度洗脱,流速:1.0 mL.min-1,检测波长:208 nm,柱温:30℃。结果共有9个共有峰。共有峰的相对保留时间和相对峰面积的RSD均<3%,符合指纹图谱相关要求。结论此方法准确、可靠。该指纹图谱能够用于蕨麻药材的鉴定及质量评价。     

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.     

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.