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.     

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。     

不同种、不同产地黄芪中黄酮类HPLC指纹图谱研究

目的:对不同种、不同产地的黄芪药材中黄酮类成分建立HPLC指纹图谱.方法:采用HPLC法,乙腈·水二元梯度洗脱;流速0.8 ml·min-1;检测波长260 nm;柱温:35℃.结果:10批黄芪药材有16个共有峰,其HPLC指纹图谱基本一致,各共有峰保留时间的比值基本一致,共有峰面积之和均大于总峰面积的90%,但其共有峰面积的比值有一定差异.结论:该方法重现性好,建立的指纹图谱为黄芪的质量控制及评价提供了依据.     

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。     

怀牛膝药材的HPLC指纹图谱研究

目的:建立怀牛膝药材的高效液相色谱(HPLC)指纹图谱。方法:色谱柱为SHIMADZU shim-pack VP-ODS(250mm×4.6mm,5μm),柱温为30℃,流动相为甲醇-0.1%醋酸水溶液(梯度洗脱),流速为1.0mL·min-1,检测波长为279nm。结果:建立了怀牛膝原药材和经硫磺熏制过的怀牛膝药材的指纹图谱。12批怀牛膝原药材有24个共有峰,其中9批药材的相似度都在0.9以上,另外3批的相似度较低;11批经硫磺熏制过的怀牛膝药材有20个共有峰,其中7批药材的相似度都在0.8以上,相似度较原药材低。结论:该方法简便、准确、专属性强,可用于怀牛膝药材的质量控制。     

黔产苗药对坐叶药材HPLC指纹图谱研究

目的:建立黔产苗药对坐叶药材的高效液相色谱(HPLC)指纹图谱。方法:采用HPLC法。色谱柱为Agilent Eclipse XDB C_(18),流动相为乙腈-0.2%磷酸溶液(梯度洗脱),流速为1.0 mL/min,检测波长为235 nm,柱温为25℃,进样量为15μL。以芦丁为参照,测定10批贵州不同地区对坐叶药材的HPLC图谱,采用《中药色谱指纹图谱相似度评价系统》(2004A版)进行共有峰指认和相似度评价。结果:10批对坐叶药材的HPLC指纹图谱有12个共有峰,相似度均大于0.90。经验证,10批样品HPLC图谱与对照指纹图谱具有较好的一致性。结论:本研究所建HPLC指纹图谱可为对坐叶药材的鉴别和质量评价提供参考。     

牡丹皮药材HPLC指纹图谱研究

目的建立牡丹皮药材的HPLC指纹图谱鉴别方法。方法色谱条件:色谱柱:迪马公司D iam onsil C18色谱柱(4.6mm×250mm,5μm)。流动相:甲醇-水溶液梯度洗脱。流量:1mL.m i-n 1。检测波长:280nm。以丹皮酚为参照物。结果指纹图谱共有色谱峰的稳定性、精密度和重复性试验中的RSD均小于6%,符合有关规定〔1〕。结论本研究可作为鉴定牡丹皮药材质量的方法之一。     

萹蓄高效液相色谱指纹图谱研究

目的 采用HPLC法建立萹蓄药材的指纹图谱.方法 采用CAPCELL PAK C18 MG(250 mm×4.6 mm,5 μm)色谱柱,以乙腈(A)-0.1％磷酸溶液(B)为流动相,线性梯度洗脱;检测波长340 nm;柱温30℃;流速1.0 mL·min-1.结果 构建的指纹图谱有18个共有峰,确认了其中8个峰的成分分别为绿原酸、杨梅苷、金丝桃苷、木犀草苷、扁蓄苷、槲皮苷、胡桃宁、木犀草素.结论 本研究为萹蓄药材的质量控制提供了新方法.     

山茱萸药材HPLC特征图谱研究

目的 建立山茱萸药材的HPLC特征图谱.方法 流动相:乙腈-0.1％磷酸溶液,梯度洗脱;色谱柱:Agilent HC-C18柱;检测波长:240 nm;柱温:30℃;流速:1.0 mL· min-1,分析时间:90 min.结果 测试样品16批,选择马钱苷峰作为参照,确立4个共有峰作为山茱萸药材特征峰.精密度和重复性试验的RSD均小于2.0％.结论 山茱萸特征图谱专属性强,可用于山茱萸药材的鉴定及质量控制.     

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.

     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

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.