LC/MS检定前列舒乐胶囊中的淫羊藿苷的含量

目的 建立前列舒胶囊中淫羊藿苷含量LC/MS测定方法。方法 采用LC/MS测定前列舒乐胶囊中淫羊藿苷的含量,并比较其与HPLC法的优劣。结果LC/MS测定淫羊藿苷0.05～0.50 mg范围内线性关系良好,与标准方法比较相对偏差小于2%,符合药品标准的规定。结论 LC/MS检测前列舒乐胶囊中的淫羊藿苷方法简便,快速,灵敏度高,可以进行定量分析。     

HPLC测定大鼠血浆中的三七皂苷R1和人参皂苷Rg1、Rb1

目的 采用HPLC测定大鼠血浆中三七皂苷R1和人参皂苷Rg1、Rb1的含量.方法 以淫羊藿为内标,采用C18色谱柱,乙腈-水线性梯度洗脱,流速1.0 mL·min-1,柱温30℃,检测波长203 nm.结果 样品中的3种皂苷成分分离良好,且线性关系良好;R1、Rg1和Rb1的线性范围分别为2～200、5.5～550、1...     

醒脑再造胶囊质量标准的研究

目的 为控制醒脑再造胶囊的质量，制定质量标准。方法 采用薄层色谱法对样品中的黄芪、红参(含三七)、黄连及冰片进行定性鉴别；采用HPLC测定淫羊藿中的淫羊藿苷含量。结果 鉴别方法专属性强；淫羊藿苷在0．1—2．1μg范围呈良好的线性关系，r＝0．9999，平均回收率为98．7％，RSD＝1．2％。结论 本质量标准可有效地控制醒脑再造胶囊的质量。     

补肾强身胶囊质量标准研究

目的建立补肾强身胶囊的质量标准。方法采用薄层色谱法对处方中淫羊藿、金樱子、菟丝子、女贞子和狗脊进行鉴别;用HPLC法测定淫羊藿苷的含量。结果在薄层色谱中能鉴别出淫羊藿、金樱子、菟丝子、女贞子和狗脊;HPLC法测定淫羊藿苷在0.1022~1.022μg范围内呈良好的线性关系(r=0.999 9),平均回收率为98.52%,RSD=1.09%。结论建立的方法快速准确,重复性好,专属性强,可用于为补肾强身胶囊的质量控制。     

不同产地和品种淫羊藿中淫羊藿苷的HPLC分析

目的 :对中药淫羊藿中淫羊藿苷的含量分析进行方法学研究 ,并测定淫羊藿的不同产地、不同品种、不同药用部位的淫羊藿苷的含量。方法 :采用RP HPLC技术对 7个品种 2 3个样品进行测定。以PERKIN EIMER SH/5C18柱为分析柱 ,流动相为乙腈 水 36%乙酸 ( 2 5∶73.5∶1 .5)流速 1 .0ml/min。UV检测波长 2 70nm。结果 :本方法测定淫羊藿苷含量在 0 .0 2 1 2～ 0 .1 2 7μg ,0 .53～ 1 .696μg范围内呈良好的线性关系。不同产地、不同品种、不同药用部位的淫羊藿其淫羊藿苷的含量为 0 .0 0 30 7%～ 1 .55%。同一植株不同部位中淫羊藿苷的含量分布叶 >叶茎 >茎 >根。结论 :淫羊藿由于产地不同、品种不同其淫羊藿苷的含量相差悬殊。本测定方法为筛选优良品种和扩大药源提供了简便易行的方法     

HPLC法测定不同产地淫羊藿饮片中淫羊藿苷的含量

目的：研究不同产地的淫羊藿饮片中淫羊藿苷的含量。方法从市场上随机采购7批淫羊藿饮片,采用稀乙醇超声萃取提取淫羊藿苷,然后采用高效液相色谱法测定淫羊藿苷含量,考察其合格率。结果按《中国药典》对淫羊藿苷含量要求,用 HPLC 法检测淫羊藿苷浓度,7批淫羊藿饮片有4批合格。结论不同产地的淫羊藿中淫羊藿苷含量不同。     

RP-HPLO测定前列癃闭通胶囊中淫羊藿苷的含量

目的 建立前列癃闭通胶囊中淫羊藿苷的含量测定方法.方法 采用RP-HPLC法,Hypersil ODS C18色谱柱;乙腈-0.1%磷酸溶液(27:73)为流动相;检测波长为270nm;流速:1.0 ml/min-1.结果 淫羊藿苷在0.08μg～0.41μg范围内具有良好的线性关系,平均加样回收率为99.62%,RSD为0.96%.结论 本方法简便、准确可靠、重现性好,可用于前列癃闭通胶囊中淫羊藿苷的含量测定.     

用HPLC法测定黄麦合剂中淫羊藿苷含量的不确定度分析

目的：建立HPLC法测定黄麦合剂中淫羊藿苷含量的不确定度分析方法。方法：对HPLC法测定淫羊藿苷含量的流程进行分析,确定不确定度来源,得出扩展不确定度。结果：HPLC法测定黄麦合剂中淫羊藿苷含量的不确定度的主要因素包括对照品溶液配制、样品制备、重复性、拟合回归模型和其他因素,扩展不确定度为0.039μg/ml,含量测定结果为（5.299±0.039）μg/ml,k=2。结论：该方法可作为HPLC法测定淫羊藿苷含量不确定度评定的参考。     

心痛康胶囊质量标准研究

目的　建立心痛康胶囊质量标准。方法　对红参进行显微鉴别 ,白芍和淫羊藿进行薄层鉴别 ,并用HPLC法测定制剂中芍药苷和淫羊藿苷的含量。结果　显微鉴别特征明显 ,薄层图谱斑点清晰 ,阴性对照无干扰 ,芍药苷在 2 5 34～ 12 6 70 μg间、淫羊藿苷在 1 96～ 17 6 6 μg间呈现良好的线性关系 ;芍药苷回收率为 99 5 1% ,RSD为 1 2 9% ,淫羊藿苷回收率为 99 11% ,RSD为 1 6 2 %。结论　结果准确 ,重复性好 ,可用于该制剂的质量控制。     

反相高效液相色谱法测定前列康胶囊中淫羊藿苷的含量

目的:建立测定前列康胶囊中淫羊藿苷含量的方法.方法:采用RP - HPLC法,色谱柱为Dismonsil C18(250mm×4 6mm,5μm)柱,以乙腈-水(25:75)为流动相,流速1.0mL·min -1,检测波长为270nm,柱温30℃.结果:淫羊藿苷在0.372～1.860μg范围内存在良好的线性关系(r=...     

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.