HPLC测定脂溶性前列安栓中盐酸小檗碱的含量

目的 建立一种简便的测定脂溶性前列安栓中盐酸小檗碱含量的方法.方法 采用高效液相色谱法(HPLC)测定盐酸小檗碱的含量.色谱条件为Kromasil C18 柱( 4.6 mm × 200 mm,5 μm), 流动相为乙腈-0.1%磷酸溶液(50:50)(每100 ml中加入十二烷基硫酸钠0.1 g ),检测波长350 nm.供试品预处理采用超声溶解法.结果 盐酸小檗碱在20～200 μg·ml-1范围内有良好的线性关系(r=0.9999),平均回收率为98.9%,RSD为0.5%.结论 本方法可用于脂溶性前列安栓中盐酸小檗碱的含量测定,方法简便、快速、灵敏.     

HPLC法测定参茸益气助阳胶囊中盐酸小檗碱的含量

目的 建立测定参茸益气助阳胶囊中盐酸小檗碱含量的高效液相色谱法.方法 采用Zorbax SB-C18(4.6 mm×250 mm,5μm)色谱柱,以乙腈-0.1%磷酸溶液(50∶50)为流动相,检测波长为265 nm.结果 盐酸小檗碱在10～200μg·mL-1范围内线性关系良好(r=0.999 7),平均回收率为97.58%,RSD为1.65%.结论 采用高效液相色谱法测定盐酸小檗碱的方法准确、可靠、简便,可作为参茸益气助阳胶囊的定量分析方法.     

RP-HPLC测定藏药邦贝抗炎栓中的盐酸小檗碱

目的 建立测定藏药邦贝抗炎栓中盐酸小檗碱含量的方法.方法 采用RP-HPLC法,色谱柱为Kromosil C18(200mm x4.6 mm,5 μm),流动相为0.1%磷酸-乙腈(65:35),流速1 ml·min-1,检测波长346 nm.结果 盐酸小檗碱质量浓度0.34～1.68 mg·ml-1与峰面积呈良好的线性关系(r=0.9998),平均回收率为99.7%,RSD=1.25%.结论 所建方法简便、准确、重复性好,适用于藏药邦贝抗炎栓制剂中盐酸小檗碱的含量测定.     

连朴饮传统煎剂与中药配方颗粒中盐酸小檗碱的含量比较

目的:建立连朴饮传统煎剂(合煎剂)与中药配方颗粒(分煎剂)中盐酸小檗碱的含量测定方法并比较二者含量。方法:采用高效液相色谱法。色谱柱为Diamonisl C18(200mm×4.6mm,5μm),流动相为乙腈-0.1%磷酸溶液(50:50,V/V)(每100ml加十二烷基磺酸钠0.1g),流速为1.0ml/min,检测波长为265nm。结果:盐酸小檗碱进样量在2.0～10.0μg范围内与峰面积积分值呈良好线性关系(r=0.9992);平均加样回收率为97.30%,RSD=1.22%(n=6)。结论:与传统煎剂比较,连朴饮中药配方颗粒中盐酸小檗碱的含量更高。     

HPLC法测定前列安通胶囊中盐酸小檗碱的含量

目的建立测定前列安通胶囊中盐酸小檗碱含量的方法。方法采用高效液相色谱法。色谱条件为X–Terra C18色谱柱,流动相为乙腈-0.5‰磷酸水溶液(27∶73),检测波长为265 nm,柱温30℃,流速为1 ml/min,进样量为10μl。结果盐酸小檗碱检测浓度线性范围为17.88～178.8μg/ml(r=0.9998),平均加样回收率为99.74%,RSD为0.96%(n=6)。结论所建立的方法简便、灵敏、快速,结果准确、可靠,可用于前列安通胶囊中盐酸小檗碱的含量测定。     

三妙丸中盐酸小檗碱的含量测定

目的采用高效液相色谱(HPLC)法测定三妙丸的盐酸小檗碱含量。方法采用Diamonsil ODS1 C18色谱柱(250 mm×4.6 mm,5μm),以50∶50的乙腈-0.1%磷酸溶液(每100mL加十二烷基磺酸钠0.1 g)为流动相,流速为1.0 mL/min,检测波长265 nm。结果盐酸小檗碱进样量在0.127～2.54μg范围内与峰面积线性关系良好,回归方程Y=418 567.505-92 087.201X,r=0.999 4。平均加样回收率为99.53%,RSD为0.48%(n=6)。结论该法简便、准确、专属、重复性好,为三妙丸的盐酸小檗碱含量分析提供了科学有效的方法。     

HPLC法测定西羚片中盐酸小檗碱的含量

目的:建iHPLC法测定西羚片中盐酸小檗碱的含量.方法:采用HPLC法测定盐酸小檗碱含量,选用C18色谱柱,以乙腈-0.1%磷酸溶液一十二烷基磺酸钠(50:50:0.1g)为流动相;检测波长为265nm.结果:盐酸小檗碱在20～200μg/ml范围内线性关系良好(r=0.9999),平均回收率为98.93%,RSD=0.973%(n=6).结论:该方法简便、灵敏、准确,可用于西羚片的质量控制.     

反相高效液相色谱法测定复方金黄痔疮软膏中盐酸小檗碱含量

目的测定复方金黄痔疮软膏中盐酸小檗碱的含量。方法采用反相高效液相色谱（RP-HPLC）法,色谱柱为DiamondC18柱（250mm×4.6mm,5μm）,流动相为乙腈-0.1%磷酸（42∶58,每100mL加十二烷基磺酸钠0.1g）,流速1.0mL/min,柱温30℃,检测波长345nm,进样量20μL。结果盐酸小檗碱进样质量浓度在12.8～102.4μg/mL范围内与峰面积线性关系良好（r=0.9999）;软膏中盐酸小檗碱的平均回收率为99.83%,RSD=1.10%（n=6）。结论所用方法操作简便、快速、准确,适用于复方金黄痔疮软膏中盐酸小檗碱的含量测定。     

HPLC法测定康妇膜中盐酸小檗碱的含量

目的:建立测定康妇膜中盐酸小檗碱含量的方法。方法:采用高效液相色谱法。色谱柱为Agilent extend C18(150mm×4.6mm,5μm),流动相为乙腈-0.1%磷酸溶液(50:50,每100mL加十二烷基磺酸钠0.1g),柱温为30℃,流速为1.0mL·min-1,检测波长为265nm,结果:盐酸小檗碱进样量在0.12825～0.76590μg范围内与峰面积积分值呈良好的线性关系(r=0.9999);平均加样回收率为98.04%,RSD=1.20%(n=6)。结论:本方法简便、准确、重复性好,可用于康妇膜的质量控制。     

HPLC法测定前列通片中盐酸小檗碱的含量

目的 建立用高效液相色谱法测定前列通片中盐酸小檗碱的含量.方法 采用Hypersil BDS C18(4.6mm×200mm,5μm)色谱柱:以乙腈-0.1mol·L-1磷酸二氢钾溶液(35∶65)为流动相,流速1.0mL·min-1,紫外检测波长为347nm测定.结果盐酸小檗碱在0.029～3.625 μg·mL-1范围内线性关系良好(r=0.9999),平均回收率为为98.08%,RSD为1.58%(n=6).结论 本方法简便、快速,重现性好,可用于前列通片质量控制.     

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.     

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.     

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.     

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.