儿咳宁合剂质量标准研究

目的:建立儿咳宁合剂的质量标准。方法:采用薄层色谱(TLC)法对方中莱菔子、浙贝母进行定性鉴别;采用高效液相色谱法测定制剂中黄芩苷的含量。结果:TLC中可清晰检出莱菔子、浙贝母;黄芩苷进样量在0.319~2.640μg范围内与峰面积积分值呈良好线性关系(r=0.9993);平均回收率为99.56%,RSD=0.83%(n=9)。结论:所建标准可用于儿咳宁合剂的质量控制。     

支扩宁合剂质量标准研究

目的:建立支扩宁合剂的质量标准。方法:采用薄层色谱(TLC)法对制剂中黄芩、桑白皮、枳壳、丹参进行定性鉴别;用高效液相色谱法对制剂中黄芩苷进行含量测定。结果:TLC斑点清晰、分离度好,阴性对照无干扰。黄芩苷的检测浓度在15.81～252.96μg.mL-1范围内与峰面积积分值呈良好的线性关系(r=0.9999);平均回收率为101.8%,RSD=1.80%(n=9)。结论:所建标准可用于支扩宁合剂的质量控制。     

利咽灵合剂的质量控制

目的:建立利咽灵合剂的质量标准.方法:采用薄层色谱(TLC)法对利咽灵合剂中的金银花、山豆根、玄参、甘草进行定性鉴别,以高效液相色谱(HPLC)法对其主药金银花中的绿原酸进行含量测定.结果:利咽灵合剂中金银花、山豆根、玄参、甘草的TLC中,在与对照品色谱相应的位置上,显相同颜色的斑点;绿原酸进样量在0.204 0～1.632 μg范围内与峰面积积分值线性关系良好(r=0.999 6),平均回收率为99.04%,RSD为1.04%(n=6).结论:本方法简便、准确、灵敏、重复性好,可用于本品的质量控制.     

栀芩合剂质量控制方法的研究

目的 提高并完善非标准制剂栀芩合剂质量标准.方法 采用薄层色谱法(TLC)对栀芩合剂中栀子、黄柏、黄芩的定性鉴别;采用高效液相色谱法(HPLC)测定栀芩合剂中黄芩苷的含量.色谱柱:Diamonsil C18(250 mm×4.6 mm,5μm),以甲醇-0.1%磷酸溶液(45:55)为流动相,流速为1.0 mL·min-1,检测波长为280 nm.结果 在TLC定性鉴别中,供试品在与对照药材(或对照品)相应位置上出现相对应的特征斑点,阴性对照在相对应位置无干扰,专属性强;HPLC法可以测定黄芩苷的含量,黄芩苷的线性范围为0.0964~0.8676μg(r=1),平均加样回收率为99.08%(n=9,RSD=1.17%).结论 该质量标准确保栀芩合剂快速定性、定量分析,实验方法简单、重复性良好、结果稳定、可靠,能够用于栀芩合剂的质量控制.     

双白片质量标准研究

目的:建立双白片的质量标准。方法:采用薄层色谱(TLC)法鉴别双白片中黄芪、刺五加和芍药;采用高效液相色谱(HPLC)法测定双白片中芍药苷的含量。结果:双白片中黄芪、刺五加及芍药的TLC分别在与对照品色谱对应的位置上显相同颜色的斑点,专属性好。芍药苷进样浓度在3.20～64.00μg·mL-1范围内与峰面积积分值呈良好的线性关系(r=0.9993);平均回收率为99.12%,RSD=1.18%(n=6)。结论:所建标准可用于双白片的质量控制。     

益肾乌发口服液质量标准研究

目的:建立益肾乌发口服液的质量标准。方法:采用薄层色谱(TLC)法对制剂中的制何首乌、补骨脂和枸杞子3味药材进行定性鉴别;用高效液相色谱(HPLC)法对方中制何首乌的有效成分二苯乙烯苷进行含量测定。结果:TLC鉴别方法专属性强,在与对照药材及对照品相应的位置上制何首乌、补骨脂和枸杞子显示相同颜色的斑点,阴性对照无干扰。二苯乙烯苷进样量在0.03～0.60μg范围内与峰面积积分值呈良好线性关系(r=0.9999);平均回收率为102.4%,RSD=1.2%(n=6)。结论:所建标准可用于益肾乌发口服液的质量控制。     

流感合剂的制备与质量标准研究

目的制备流感合剂并建立其质量控制方法。方法采用煎煮和蒸馏法制备流感合剂;以薄层色谱(TLC)法鉴别大黄和姜黄;以高效液相色谱(HPLC)法测定青蒿素的含量。结果TLC能清晰地鉴别大黄、姜黄的特征斑点;青蒿素进样量在0.42~2.10μg范围内线性关系良好(r=0.9993);加样回收率为99.84%(RSD=2.15%)。结论本制剂制备方法简便,稳定性良好。TLC法专属性强,HPLC法简便、准确,可用于流感合剂的质量控制。     

益神颗粒质量标准研究

目的:建立益神颗粒的质量标准。方法:采用薄层色谱(TLC)法对制剂中的制何首乌、灵芝、黄芪、当归进行定性鉴别;用高效液相色谱法对制何首乌中二苯乙烯苷进行含量测定。结果:TLC鉴别方法专属性强,在与对照药材/对照品相应的位置上显相同颜色的斑点,阴性对照无干扰。二苯乙烯苷进样量在0.037 75~0.755μg范围内与峰面积积分值呈良好线性关系(r=0.999 5);平均加样回收率为99.44%,RSD=1.79%(n=6)。结论:所建标准可用于益神颗粒的质量控制。     

排石止痛合剂质量标准的研究

目的制定排石止痛合剂的质量标准.方法用TLC法鉴别制剂中延胡索、木香、大黄;用HPLC法测定芍药苷的含量.结果TLC色谱中能明显地检出延胡索、木香、大黄;HPLC法测定,芍药苷在0.8～26.0 μg·mL-1线性良好,r=0.999 6(n=6),平均回收率为99.64%,RSD为0.29%.结论定性、定量方法简便、准确,专属性强,能有效控制排石合剂的质量.     

乳疾灵合剂的鉴别与含量测定

目的:建立乳疾灵合剂中白芍、淫羊藿和丹参的鉴别与芍药苷的含量测定方法。方法:采用薄层色谱(TLC)法和高效液相色谱(HPLC)法。结果:薄层斑点清晰、重现性好,阴性样品无干扰。芍药苷含量测定的线性范围为80～1280μg/mL,r=0.9997,平均回收率为99.4%,RSD为1.8%(n=5)。结论:该方法简便、准确,可用于乳疾灵合剂的质量控制。     

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.

     

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.     

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.     

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.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.