HPLC法测定乙肝灵胶囊中芍药苷的含量

目的测定乙肝灵胶囊中芍药苷的含量。方法采用HPLC法,色谱柱采用Beckman C18反相柱。流动相:甲醇-0.05mol.L-1磷酸二氢钾溶液-醋酸-异丙醇(67∶173∶4∶4),流速为0.8ml.min-1,检测波长为240nm。结果本法线性关系良好(r=0.9995),平均加样回收率为98.44%,RSD=0.77%(n=6)。结论本法简便易行,结果准确,重现性好,可用于乙肝灵胶囊的质量控制。     

荧光分光光度法测定何首乌及人参首乌胶囊中总蒽醌的含量

目的:建立测定何首乌及人参首乌胶囊中总蒽醌含量的方法。方法:荧光分光光度法。以最佳 pH 条件的无水乙醇为溶剂,在λ_(EX)=440nm、λ_(EM)=515nm 处测定总蒽醌含量。结果:在0.03～0.15μg·mL~(-1)范围内,大黄素浓度和荧光强度有良好的线性关系,回归方程为 F=194.36C 2.9642,r=0.9996。平均回收率何首乌为98.1%,RSD 为1.9%;人参首乌胶囊为98.6%,RSD 为2.0%。测得总蒽醌含量何首乌中为0.522 mg·g~(-1),人参首乌胶囊中为0.443mg·g~(-1)。结论:本法简便快捷,准确灵敏,重复性好,可用于何首乌及人参首乌胶囊的质量控制。     

RP-HPLC法测定复方首乌合剂中大黄素的含量

目的:建立以反相高效液相色谱法测定复方首乌合剂中大黄素含量的方法。方法:色谱柱为Diamonsil C_(18)(150 mm×4.6 mm,5μm),流动相为甲醇-0.1%磷酸溶液(68:32),检测波长为220 nm。结果:大黄素的检测浓度在7.8～78.0μg·mL~(-1)范围内与峰面积积分值呈良好线性关系(r=0.9998);平均回收率为98.25%,RSD=1.09%(n=9)。结论:本法准确、灵敏、重现性好,可用于复方首乌合剂的质量控制。     

HPLC法测定复方五仁醇胶囊中五味子醇甲的含量

建立测定复方五仁醇胶囊中五味子醇甲含量的HPLC分析方法。采用DiamonsilTMC18色谱柱,甲醇-水(70∶30)为流动相,检测波长250nm。五味子醇甲在16.16～113.12μg·mL-1之间与峰面积呈良好的线性关系(r=0.9996,n=6),平均回收率98.08%,RSD=1.24%。本法操作简便、快速、准确,可用于复方五仁醇胶囊的含量测定。     

HPLC法测定肝脂清胶囊中大黄素、大黄酚的含量

目的:建立肝脂清胶囊中大黄素、大黄酚的含量测定方法。方法:采用高效液相色谱法,以waters ODS C_(18)柱为固定相,甲醇-0.1%磷酸溶液(85:15)为流动相,检测波长254nm,流速1.0ml·min~(-1),柱温室温。结果:大黄素在13.84～83.04ng (r=0.9998),大黄酚在27.92～167.52ng(r=0.9998)范围内呈良好线性关系,平均回收率大黄素为99.47%、RSD为1.11%;大黄酚99.60%,RSD为1.09%。结论:本方法简便,准确,重现性好,为控制肝脂清胶囊的质量提供了科学依据。     

肝炎康胶囊质量标准的建立

目的:研究肝炎康胶囊的质量标准。方法:分别采用薄层色谱法鉴别肝炎康胶囊中的虎杖、黄芪、太子参、半枝莲、白花蛇舌草、丹参、柴胡;用高效液相色谱法测定肝炎康中的大黄素含量。结果:薄层色谱法能明显从肝炎康胶囊中鉴别出虎杖、黄芪、太子参、半枝莲、白花蛇舌草、丹参、柴胡。测得肝炎康胶囊中所含大黄素的含量是2.05 mg·g-1,大黄素的含量在范围2.34~74.88μg·ml-1之间呈现良好的线性关系(r=0.999 4),平均回收率为100.5%,RSD为1.52%(n=9)。结论:肝炎康胶囊质量标准准确、可靠,可作为肝炎康胶囊的质量控制方法。     

高效液相色谱法测定复方卡托普利尼群地平胶囊中卡托普利的含量

目的建立高效液相色谱法测定复方卡托普利尼群地平胶囊中卡托普利的含量。方法采用美国Agilent高效液相色谱仪,流动相:以0.01mol·L-1的磷酸二氢钠溶液-甲醇-乙腈(65∶30∶5)(用磷酸调节pH至3.0)为流动相,流速:1.1mL·min-1,检测波长为215nm。柱温40℃。结果卡托普利在25.75～257.5μg·mL-1范围内,线性关系良好,r=0.9992。回收率为99.8%。结论本法可准确测定复方卡托普利尼群地平胶囊中卡托普利的含量,适用于产品的质量控制。     

HPLC法同时测定复方苏润江滴丸中秋水仙碱、芦荟苷及芦荟大黄素的含量

目的:建立高效液相色谱法同时测定复方苏润江滴丸中秋水仙碱、芦荟苷、芦荟大黄素的含量。方法:采用Cosmosil-C18色谱柱(250 mm×4.6 mm,5μm),柱温为35℃,以甲醇(A)和水(B)为流动相,梯度洗脱[0～23 min,A-B(45∶55);23～40 min,A-B(65∶35)],流速1 mL·min-1,双波长检测:254 nm(检测芦荟大黄素),350 nm(检测秋水仙碱和芦荟苷)。结果:样品中秋水仙碱、芦荟苷和芦荟大黄素分离良好,秋水仙碱在16.54～82.71 mg·L-1(r=0.9998)、芦荟苷在13.19～105.54 mg·L-1(r=0.9997)、芦荟大黄素在6.00～47.97 mg·L-1(r=0.9999)范围内均呈良好线性关系;秋水仙碱、芦荟苷和芦荟大黄素的回收率分别为99.53%(RSD为1.3%),97.70%(RSD为1.0%),100.8%(RSD为0.96%),供试品溶液在12 h内稳定。结论:该方法简单准确,专属性强,重现性好,可用于同时测定复方苏润江滴丸中秋水仙碱、芦荟苷和芦荟大黄素的含量。     

决明子及其制剂银屑灵胶囊的含量分析

目的:建立决明子药材及其制剂银屑灵胶囊中大黄酚的含量测定方法.方法:反相高效液相测定法,Hpyersil C18分析柱(250mm×4.6mm.5μm),流动相:甲醇-0.1%磷酸(80:20),检测波长:439nm,流速1.0ml·min-1.结果:大黄酚在0.0784-0.3920μg范围内,线性关系良好(r=o.9998),平均回收率为98.5%.结论:本法简便,准确,可用于决明子及其制剂银屑灵胶囊的质量控制.     

HPLC法测定大黄通便颗粒中大黄素和大黄酚的含量

建立大黄通便颗粒中大黄素和大黄酚含量的HPLC测定方法.采用Spherixorb C18色谱柱,流动相:甲醇-0.1%磷酸溶液(90:10),流速:0.8ml·min-1,检测波长:254nm.线性范围:大黄素0.0135～0.2160μg(r=0.9998),大黄酚0.0240～0.3840μg(r=0.9995).平均加样回收率(n=5)分别为大黄素100.8%,RSD=1.1%;大黄酚100.2%,RSD=0.8%.本法简便,快速,结果准确.     

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.