高效液相色谱法测定瑞舒伐他汀钙及其片剂的含量

目的建立高效液相色谱法测定瑞舒伐他汀钙含量的方法。方法色谱柱:KromasilC18色谱柱(4.6mm×250mm,5μm);检测波长:242nm;流动相:乙腈0.3%草酸铵溶液(醋酸调节pH4.0)(42∶58);流速:1.0ml·min-1。结果在10～500μg·ml-1内有良好的线性关系,相关系数为0.9999,精密度小于1.0%(n=6)。结论本方法简便、准确,可用于瑞舒伐他汀钙及其片剂的含量测定。     

HPLC法测定藿香正气胶囊中厚朴酚与和厚朴酚的含量

目的测定藿香正气胶囊中厚朴酚与和厚朴酚的含量.方法采用HPLC法.色谱柱:采用Thermo 1254133T色谱柱(250×4.6mm,5μm);流动相:甲醇-水(75∶25);流速:1.0mL·min-1;检测波长:294nm.结果厚朴酚平均回收率为99.81%,RSD=0.3%(n=5);和厚朴酚平均回收率为100.14%,RSD=0.8%(n=5).结论方法简单易行,结果准确,可靠,适用于本品的含量测定.     

高效液相色谱法测定复方亚油酸乙酯胶丸中橙皮苷的含量

目的建立复方亚油酸乙酯胶丸中橙皮苷的含量测定方法。方法液相色谱法。色谱柱:Kromasil C18柱(4.6mm×250mm,5μm);流动相:甲醇-0.5%冰醋酸溶液(40∶60);流速1.0mL.min-1;柱温:40℃;检测波长:283nm。结果橙皮苷在0.07505～0.3752μg范围内呈线性关系(r=0.9997,n=5),平均加样回收率为99.16%,RSD为1.7%(n=6)。结论该方法操作简便,结果可靠,可用于复方亚油酸乙酯胶丸中橙皮苷的含量测定。     

高效液相色谱法测定丹参药材中丹参素的含量

目的:建立丹参药材中丹参素含量测定的方法.方法:色谱条件:色谱柱为C18柱,流动相为甲醇-0.5%冰醋酸水溶液(15:85),检测波长为280 nm.结果:其回归方程为Y=714 525.615 4X-274 34.826 6,r=0.999 9,丹参素在0.343～2.058μg范围内线性关系良好;重现性RSD为0.76%(n=5);平均回收率为97.95%,RSD为0.38%(n=5).结论:本方法灵敏、简便、准确可靠,可作为丹参药材中丹参素的含量测定标准.     

液相色谱法测定强力救心滴丸中蟾酥的华蟾酥毒基和酯蟾毒配基含量

目的:测定强力救心滴丸中蟾酥的主要成分华蟾酥毒基和酯蟾毒配基含量。方法:样品经甲醇超声处理提取,采用高效液相色谱法测定,色谱柱为 Alltima C_(18)色谱柱(4.6mm×250mm,5μm);柱温:40℃;流速:1mL·min~(-1);流动相:乙腈-0.5%磷酸二氢钾(pH=3.2)(50:50);检测波长:296nm。结果:华蟾酥毒基在0.25-1.51μg 范围内、酯蟾毒配基在0.26-1.55μg 范围内具有良好线性关系。华蟾酥毒基平均加样回收率为99.6%,RSD=2.1%(n=5);酯蟾毒配基平均加样回收率为98.2%,RSD=1.4%(n=5)。结论:该法准确、可靠,可用于强力救心滴丸中蟾酥的酯蟾毒配基和华蟾酥毒基含量测定。     

RP-HPLC法测定川芎CO_2超临界流体萃取物中丁烯基苯酞的含量

目的测定川芎二氧化碳超临界流体萃取物中丁烯基苯酞的含量。方法采用HPLC法。色谱条件为色谱柱:Diamonsil C18(200 mm×4.6 mm,5μm);流动相:甲醇体积分数为10%异丙醇水溶液(体积比为60∶40);流速:1.0 mL.min-1;检测波长:235 nm;柱温:40℃。结果丁烯基苯酞在7.28~72.8μg.mL-1内线性关系良好(r=0.999 5),平均回收率为99.7%(RSD=2.72%,n=6)。3批样品中丁烯基苯酞的含量质量分数分别为4.86%(RSD=1.25%,n=3)、5.00%(RSD=1.87%,n=3)和4.81%(RSD=1.87%,n=3)。结论HPLC法可以测定川芎二氧化碳超临界流体萃取物中丁烯基苯酞的含量,供试品中丁烯基苯酞与其他组分的色谱峰分离度良好。     

高效液相色谱法测定复方氨酚苯海拉明片中对乙酰氨基酚和咖啡因的含量

目的建立一种快速、准确的高效液相色谱法测定复方氨酚苯海拉明片中对乙酰氨基酚和咖啡因含量的方法。方法色谱柱HypersilODS2(5μm,250mm×4.6mm)流动相:甲醇-水(30∶70);流速:1mL.m in-1;检测波长:280nm;柱温:室温;进样量:20μL。结果对乙酰氨基酚进样量在1.50μg~9.00μg范围内线性良好,r=0.99999。平均回收率为99.97%,RSD=0.51%(n=9);咖啡因进样量在0.15μg~0.90μg范围内线性良好,r=0.99999(n=9)平均回收率为99.79%,RSD=0.99%(n=9)。结论试验结果表明本法简便快速,重现性好,结果准确可靠,可以作为复方氨酚苯海拉明片中对乙酰氨基酚和咖啡因的含量测定的方法。     

HPLC同时测定升麻中三个酚酸类成分的含量

目的建立快速测定升麻中咖啡酸、阿魏酸及异阿魏酸含量的HPLC方法。方法色谱柱为C18柱(4.6 mm×250 mm,5μm);流动相:乙腈-0.01%磷酸梯度洗脱;柱温:30℃;检测波长:320 nm;流速:1.0 ml/min。结果咖啡酸、阿魏酸、异阿魏酸分别在5.78~115.6μg/ml(r=0.9998,n=6),4.03~80.60μg/ml(r=1,n=6),16.45~329.00μg/ml(r=1,n=6)范围内线性关系良好,回收率在97.6%~101.5%。结论建立的方法准确可靠,可以用于测定升麻中咖啡酸、阿魏酸、异阿魏酸的含量。     

双波长梯度洗脱高效液相色谱法测定冲和软膏中芍药苷和蛇床子素的含量

目的:建立RP-HPLC法同时测定冲和软膏中芍药苷和蛇床子素含量的方法。方法:色谱柱为Phenomisl C18柱(150 mm×4.6 mm5,μm);以乙腈-水为流动相进行梯度洗脱;流速为1.0 mL·min-1;柱温为35℃;检测波长为230和330 nm。结果:芍药苷与蛇床子素的线性范围分别为3.12～249.8μg·mL-1(r=0.999 8)和1.54～123μg·mL-1(r=0.999 9);平均加样回收率分别为101.0%(RSD=1.07%,n=9)和100.8%(RSD=1.21%,n=9)。结论:本方法操作简便,测定结果准确,重复性好,可作为该产品质量控制的方法。     

高效液相色谱法测定复方达克罗宁乳膏中盐酸达克罗宁、马来酸氯苯那敏、地塞米松磷酸钠的含量

目的建立高效液相色谱法测定复方达克罗宁乳膏中盐酸达克罗宁、马来酸氯苯那敏、地塞米松磷酸钠含量的方法。方法采用高效液相色谱法。色谱柱为VP-ODS C18柱(250 mm×4.6 mm,5μm);流动相为磷酸缓冲液-乙腈(80∶20);流速:1.0 mL.min-1;测定波长:240 nm;柱温:30℃:进样:10μL。结果该方法不受处方中基质干扰。盐酸达克罗宁、马来酸氯苯那敏、地塞米松磷酸钠的线性范围分别为0.100 3~0.702 1μg(r=0.999 8,n=6),0.028 56~0.199 9μg(r=0.999 9,n=6),0.006 694~0.046 85μg(r=0.999 7,n=6),平均回收率分别为98.8%、99.0%、99.0%,RSD分别为0.97%、1.3%、0.98%(n=9)。结论该方法操作简便,灵敏度高,重现性好,可用于复方达克罗宁乳膏中盐酸达克罗宁、马来酸氯苯那敏、地塞米松磷酸钠的含量测定。     

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.