活血去瘀颗粒的水提取工艺研究

目的 研究活血去瘀颗粒的最佳水提取工艺.方法 用正交试验设计优化最佳提取条件,以浸膏得率和丹参素含量为指标,选用L9(34)进行煎煮条件的选择.结果 最佳水提取工艺为加入8倍量水提取3次,每次煎煮1.5 h.结论 该提取工艺所得浸膏得率和丹参素含量高.并经验证,合理可行.     

正交试验法优选消炎颗粒提取工艺

目的：优选消炎颗粒的提取工艺。方法：利用正交试验法考察加水量、煎煮时间、煎煮次数等因素对提取工艺的影响,以干浸膏得率和秦皮乙素含量为考察指标,烘干法测定干浸膏得率,高效液相色谱法测定秦皮乙素含量。结果：加8倍量水,煎煮1.5 h,煎煮3次为最佳提取工艺。结论：正交试验法筛选消炎颗粒的提取工艺可行、方法简便,制备的颗粒质量合格稳定。     

正交试验法优选乳舒片的提取工艺

目的：优选乳舒片的提取工艺。方法：采用正交试验法，以丹参素的含量和浸膏得率为指标，考察加水量、煎煮时间和煎煮次数对提取率的影响。结果：最佳提取工艺为10倍加水量、煎煮60min、煎煮3次。结论：正交试验法优选乳舒片的提取工艺简便、快速、准确。     

柴芩解热颗粒提取工艺研究

目的优选柴芩解热颗粒的最佳提取工艺。方法乙醇提取工艺以葛根素含量和浸膏得率为指标,水提取工艺以黄苓苷含量、浸膏得率为指标。采用正交试验优选柴芩解热颗粒最佳提取工艺。结果醇提最佳工艺条件为加8倍量70%乙醇,回流提取3次,每次1.5 h;水提最佳工艺条件为加10倍量水,煎煮3次,每次1.5 h。结论优选出的提取工艺稳定、合理、可行。     

祛风胜湿颗粒提取工艺优选

目的 优选祛风胜湿颗粒最佳的提取工艺.方法 采用L9（3）4正交试验设计,以异欧前胡素含量及干浸膏得率为考察指标,筛选祛风胜湿颗粒的醇提最佳工艺条件;以甘草酸单铵盐含量及干浸膏得率为考察指标,筛选祛风胜湿颗粒的水提最佳工艺条件;采用单因素试验,优选防风、川芎、藁本和蔓荆子4味药材的最佳提取工艺.结果 优选的祛风胜湿颗粒醇提最佳工艺条件为加10倍量70％乙醇,回流提取2次,每次2h;挥发油的提取工艺条件为加8倍量水提取4h;水提最佳工艺条件为加10倍量水,煎煮2次,每次1h.结论 优选的生产工艺合理、可靠,适合现代化大生产.     

正交试验法优选金铃子颗粒提取工艺

摘 要 目的：：优选金铃子颗粒的提取工艺。 方法: 用正交试验法考察加水量、煎煮时间、煎煮次数等因素对提取工艺的影响,以干浸膏得率和延胡索乙素含量为考察指标,烘干法测定干浸膏得率,高效液相色谱法测定延胡索乙素含量。 结果: 加10倍量水,煎煮1 h,煎煮 3 次为最佳提取工艺。 结论: 优选的工艺合理可行、重复性良好、提取效率高,适合于工业化生产。     

清热利湿颗粒提取工艺的实验研究

目的优选清热利湿颗粒的最佳提取工艺。方法水提取工艺以黄柏单煎,采用正交设计法以浸膏得率和盐酸小檗碱含量为考察指标;赤芍等8味药材合煎,采用正交设计法以浸膏得率和芍药苷含量为考察指标,优选最佳提取工艺条件。结果清热利湿颗粒最佳工艺条件：黄柏单煎加入10倍量水,煎煮2次,每次1.5 h;赤芍等药材加入10倍量水,煎煮2次,每次2小时。结论优选出的提取条件科学合理,提取工艺经验证,重现性较好,有效成分转移率较高。     

正交法优化咽炎Ⅰ号口服液提取工艺

目的优选咽炎合剂Ⅰ号口服液的提取工艺。方法以黄芩苷含量和浸膏得率为指标，采用L9（3^4）正交试验对提取工艺进行优选。结果最佳提取工艺为10倍量水，煎煮90min，煎煮3次，60％乙醇沉淀。结论所优选的最佳提取工艺可行。     

正交法优化咽炎I号口服液提取工艺

目的优选咽炎合剂I号口服液的提取工艺。方法以黄芩苷含量和浸膏得率为指标，采用L9（34）正交试验对提取工艺进行优选。结果最佳提取工艺为10倍量水，煎煮90 min，煎煮3次，60%乙醇沉淀。结论所优选的最佳提取工艺可行。     

综合评分法优选驱虫斑鸠菊的提取工艺

目的优选驱虫斑鸠菊的最佳提取工艺。方法采用正交试验设计,以紫铆素含量、总黄酮含量及浸膏得率为指标,考察影响提取的因素。结果驱虫斑鸠菊的最佳提取工艺为加入10倍量水,浸泡1 h,煎煮1 h,共3次。结论该工艺可提高驱虫斑鸠菊的提取率。     

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.     

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.

     

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.     

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.