栀子黄色素的分离纯化

目的研究栀子黄色素的大孔吸附树脂富集纯化工艺。方法以栀子黄色素的纯度和得率为指标,考察大孔吸附树脂FU02对栀子提取液动态富集纯化最适工艺。结果大孔吸附树脂FU02对栀子黄色素的最适动态吸附条件：料液中栀子黄色素浓度5g/L、栀子苷浓度30~32g/L,料液流速1Bv/h,此条件下大孔吸附树脂FU02对栀子黄色素的吸附率为82.5%,栀子苷去除率可达69.7%。吸附在树脂上的栀子黄色素的最适动态解吸条件：以80%乙醇溶液为解吸液、解吸流速2Bv/h,此条件下栀子黄色素洗脱率可达96.0%,制备的栀子黄色素A238/A440可降至0.35~0.38。结论采用大孔吸附树脂FU02富集纯化,制备高纯度的栀子黄色素,是方便可行的。     

大孔树脂同步分离栀子中栀子苷和栀子黄色素工艺研究

目的研究大孔树脂同步分离纯化栀子药材中的栀子苷和栀子黄色素。方法通过比较不同大孔吸附树脂静态吸附栀子黄色素的能力,并对最佳大孔吸附树脂纯化工艺进行筛选。结果HPD-100型树脂综合性能最佳,其纯化工艺为：上样液浓度A440在60左右,以流样速度1—3mL．min^-1上样;水洗8～10BV;25％乙醇冲洗3～5BV体积;70％乙醇冲洗至洗脱液无色。结论栀子苷得率70％、栀子黄色素（色价100～500、OD小于0．8甚至达到0．3）得率80％（折算至栀子药材含量）,说明此工艺可行。     

大孔树脂同步分离栀子中栀子苷和栀子黄色素工艺研究

目的 研究大孔树脂同步分离纯化栀子药材中的栀子苷和栀子黄色素。方法 通过比较不同大孔吸附树脂静态吸附栀子黄色素的能力,并对最佳大孔吸附树脂纯化工艺进行筛选。结果 HPD-100型树脂综合性能最佳,其纯化工艺为：上样液浓度A440在60左右,以流样速度1～3 mL·min^-1上样;水洗8～10 BV;25%乙醇冲洗3～5 BV体积;70%乙醇冲洗至洗脱液无色。结论 栀子苷得率70%、栀子黄色素(色价100～500、OD小于0.8甚至达到0.3)得率80%(折算至栀子药材含量),说明此工艺可行。     

枸杞多糖提取工艺研究

目的优选枸杞多糖最佳提取工艺条件。方法以枸杞子中枸杞多糖含量和枸杞多糖收得率为指标,用比色法测定其含量,采用3种不同实验方法,用正交实验法L9（34）对实验提取料液比（A）、提取时间（B）、提取温度（或提取火力）（C）和溶液pH值（D）等4个因素进行考察,确定枸杞多糖在3种不同实验方法的最佳提取工艺,并对3种方法最佳工艺进行验证。结果直观分析结果表明,以枸杞多糖含量和收得率为指标,水浴法最佳工艺是A3B3C3D1,超声法的最佳工艺是A3B3C2D1,微波法最佳工艺是A1B2C2D1。结论根据验证实验结果,考虑实验过程节约能源,提取枸杞多糖最佳提取工艺为采用微波波法,提取料液比为1：10,提取时间4 min,提取火力为中火,提取溶液的pH值为8。     

安乳颗粒中丹参的乙醇提取试验研究

目的优选安乳颗粒中丹参的提取工艺。方法以丹参酮ⅡA的含量为考察指标,应用L9（34）正交试验法考察乙醇浓度、液料比、提取时间对提取效果的影响。结果影响因素依次是：乙醇浓度（A）〉液料比（B）〉提取时间（C）,最佳制备工艺为A2B2C2,即加8倍量80%乙醇,加热回流提取2次,每次1.5h。结论该优选制备工艺合理,有效成分提出率高。     

超声波协同半仿生法提取金银花-连翘药对中4种成分的工艺研究

摘要：目的:优选金银花-连翘（1∶1）药对的超声波协同半仿生法提取工艺。方法:采用正交试验设计法,以金银花-连翘（1∶1）药对中绿原酸、连翘脂苷A、木犀草苷及连翘苷的含量为综合评分指标,考察料液比、提取时间、提取温度3个因素对提取效果的影响,进行验证试验。结果:3种因素对有效成分提取率的影响大小顺序为料液比>提取时间>提取温度,其中料液比具有显著性影响;超声波协同半仿生法提取的最优工艺参数为料液比1∶50、提取温度60℃、超声波时间60 min。结论:优选的超声波协同半仿生法提取工艺操作简单、结果稳定可行,可用于金银花-连翘（1∶1）药对的提取。     

正交试验优选山茱萸总环烯醚萜苷的提取、纯化工艺

目的优选山茱萸总环烯醚萜苷的提取、纯化工艺。方法以总苷含量为指标,选择料液比、乙醇浓度和提取温度为考察因素,采用L9(34)正交试验来优选提取工艺;选择洗脱剂浓度及用量为考察因素,采用单因素试验考察SP825型大孔吸附树脂的纯化工艺。结果山茱萸总环烯醚萜最佳提取工艺为料液比1∶25、乙醇浓度10%、提取温度95℃。纯化工艺为10%乙醇洗脱10 BV。结论优选的山茱萸总环烯醚萜苷提取工艺稳定可行,SP825型大孔吸附树脂可富集山茱萸总环烯醚萜苷。     

正丁醇萃取技术制备高纯度栀子苷的工艺研究

目的:优化正丁醇萃取技术制备高纯度栀子苷的工艺。方法:以精制品中栀子苷的含量和栀子苷的转移率为指标,优选正丁醇萃取技术纯化栀子苷的最佳工艺。结果:正丁醇萃取工艺为:取栀子苷粗提物适量,加20倍量的水使之溶解,分别加入正丁醇萃取2次,每次正丁醇用量为栀子苷粗提物质量的20倍,收集正丁醇萃取液,回收正丁醇,干燥,收集白色粉末状样品。结论:此工艺简便易行,效率高,可用于制备纯度高于90%的栀子苷。     

栀子苷的精制工艺研究

目的研究吸附树脂对栀子苷的吸附性能及原液浓度、pH值、流速、洗脱剂的种类对树脂吸附性能的影响.方法采用不同的吸附树脂,用紫外分光光度法测定栀子苷的含量作为观察指标.结果树脂D301对栀子苷的适宜吸附条件为:原液浓度为0.285 g·L-1,pH值为4,流速为3 BV·h-1;洗脱剂用50%乙醇时,解吸效果较好.结论树脂D301可用作栀子苷的精制方法.     

正交试验法优选盐酸对氯苯肼的合成工艺

目的：优选一种盐酸对氯苯肼合成工艺。方法：采用正交设计，以对氯苯肼合成工艺中滴加盐酸时的温度（A），滴加盐酸所用时间（B）还原反应温度（C）和还原反应时间（D）为4个因素，每因素选取3个水平进行试验，测定样品中杂质苯肼的含量。结果：因素A和 C对杂质苯肼的含量均有显著影响，因素B和D影响不显著。优化合成工艺为A2B1C3D1。结论：用正交试验法优选盐酸对氯苯肼合成工艺可行。     

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.