HPLC测定齐墩果酸滴丸中齐墩果酸的含量

目的建立齐墩果酸滴丸的含量测定方法.方法采用HPLC法,色谱柱为Hypersil C18柱(4.0 mm×250 mm,5 μm),流动相为乙腈-水(75:25,v/v),检测波长220 nm.结果齐墩果酸在0.017～0.098 g·L-1呈良好线性关系(r=0.999 7),平均加样回收率为101.4%(n=6),RSD=0.88%.结论本测定方法简单、准确、可靠,可作为该制剂的质量控制方法.     

RP-HPLC法同时测定不同采收期连翘中乌索酸和齐墩果酸的含量

目的建立同时测定连翘中乌索酸和齐墩果酸含量的测定方法。方法采用HPLC法测定其含量。色谱柱为Nucleodur C18色谱柱(4.6 mm×250.0 mm,5μm),流动相为甲醇-水(体积比为88∶12),流速为0.8 mL.min-1,检测波长为210 nm,柱温为25℃。结果乌索酸、齐墩果酸进样量分别在0.4265~4.2650μg(r=0.9997)和0.4624~4.6240μg(r=0.9999)内峰面积与进样量呈良好的线性关系;乌索酸和齐墩果酸的平均回收率分别为99.6%(RSD为0.7%)和98.7%(RSD为0.8%)。结论该方法可用于中药连翘的质量评价和控制。     

反相高效液相色谱法测定陆英中乌索酸和齐墩果酸含量

目的建立陆英药材中乌索酸和齐墩果酸含量的测定方法。方法选用SymmetryC18(3.9mm×150mm,5μm)色谱柱,流动相甲醇-水(88∶12),检测波长220nm,流速0.6mL/min,柱温25℃。结果乌索酸的线性范围0.098~2.35μg,r=0.9999;齐墩果酸的线性范围0.099~2.38μg,r=0.9997。乌索酸和齐墩果酸平均回收率分别为97.9%(RSD为2.11%)和98.6%(RSD为1.84%)。结论本法可同时测定乌索酸和齐墩果酸含量,具有准确、灵敏、数据可靠的优点,可用于陆英药材的质量控制。     

HPLC法测定山楂降脂通片中齐墩果酸的含量

目的 建立HPLC法测定山楂降脂通片中齐墩果酸的含量.方法 采用HPLC法,色谱柱为Hypersil ODS C18(4.6×250mm,5μm),检测波长为215nm,流动相为甲醇-水-醋酸铵-乙腈(9:20:0.8:70),流速为1.0ml*min-1.结果 齐墩果酸在浓度64μg·mL-1～320μg·mL-1范围内线性关系良好(r=0.9995),平均回收率为100.1%,RSD为1.32%.结论 本方法 操作简便,快速,重复性好,精密度高,结果 准确可靠,可用于山楂降脂通片中齐墩果酸的含量测定.     

HPLC法测定肝速康片中齐墩果酸的含量

目的建立肝速康片齐墩果酸的含量测定方法。方法采用HPLC法,色谱柱:Symmetry C18柱(250 mm×4.6mm,5μm);流动相:甲醇-0.4%磷酸(90∶10);检测波长:210nm;流速:1.0 mL.min-1;柱温:室温。结果齐墩果酸在0.219～2.409μg范围内线性关系良好(r=0.999 9),平均回收率为97.8%,RSD为1.6%。结论方法准确、快速、稳定、重现性好,可用于肝速康片的质量控制。     

UPLC-PDA法测定藏药翼首草不同药用部位中齐墩果酸和熊果酸的含量

目的:建立测定藏药翼首草不同药用部位中齐墩果酸和熊果酸含量的方法,并比较其不同部位之间的含量差异。方法:采用超高效液相色谱-光电二极管阵列检测器(UPLC-PDA)测定翼首草不同药用部位(全草、地上部位和地下部位)齐墩果酸和熊果酸含量。色谱柱为Acquity UPLC HSS T3(150 mm×2.1 mm,1.8μm);流动相为甲醇-0.1 mol/L乙酸铵溶液(88∶12,V/V),流速为0.2 m L/min;检测波长为210 nm;柱温为30℃;进样量为5μL。结果:齐墩果酸和熊果酸的检测质量浓度线性范围分别为10.65~1 065μg/m L(r=0.999 6)、18.8~1 880μg/m L(r=0.999 4),平均加样回收率分别为96.95%(RSD=1.24%,n=9)、98.12%(RSD=2.13%,n=9),精密度、稳定性、重复性试验的RSD均小于3%。不同药用部位的齐墩果酸和熊果酸含量的高低整体趋势为地上部位>全草>地下部位;翼首草全草中齐墩果酸和熊果酸平均总量为0.35%,地上部位中为0.56%,地下部位中为0.09%。结论:建立的方法快速、准确可靠、重复性好,适合于藏药翼首草不同药用部位中齐墩果酸和熊果酸含量的测定。翼首草地上部位中齐墩果酸和熊果酸含量较全草、地下部位高,建议使用地上部位入药。     

HPLC测定不同产地大苞荆芥中的齐墩果酸和熊果酸

目的 采用HPLC法同时测定大苞荆芥中齐墩果酸和熊果酸的含量,并分析不同产地大苞荆芥质量的差别。方法 采用JADE-PAK ODS-AQ色谱柱(250 mm×4.6 mm, 5μm),流动相为甲醇-0.05 mol·L^-1乙酸铵(85:15),检测波长210 nm,柱温30℃。结果 齐墩果酸和熊果酸的线性范围分别为0.108～4.32μg(r²=0.9993,n=6)、0.212～8.48μg(r²=0.9994,n=6),加样回收率与RSD均符合要求。大苞荆芥中齐墩果酸和熊果酸的平均含量分别为0.0686%、0.1186%。结论 所用方法简便、准确、稳定、可靠,可用于大苞荆芥的质量评价。     

HPLC梯度洗脱法同时测定复方荆芥熏洗剂中的升麻素苷、5-O-甲基维斯阿米醇苷、齐墩果酸和熊果酸含量

目的采用高效液相梯度洗脱法建立复方荆芥熏洗剂中升麻素苷、5-O-甲基维斯阿米醇苷、齐墩果酸和熊果酸含量测定方法。方法 Hypersil C18色谱柱(4.6 mm×250 mm,5μm);流速:1.1 mL·min-1;流动相A为乙腈-甲醇(2:1),流动相B为1%冰醋酸溶液,梯度洗脱;检测波长分别为254 nm(升麻素苷和5-O-甲基维斯阿米醇苷)和205 nm(齐墩果酸和熊果酸)。结果升麻素苷、5-O-甲基维斯阿米醇苷、齐墩果酸和熊果酸分别在0.028 4⁰.568 0μg(r=0.999 7)、0.022 60.568 0μg(r=0.999 7)、0.022 6⁰.452 0μg(r=0.999 8)、0.010 80.452 0μg(r=0.999 8)、0.010 8⁰.216 0μg(r=0.999 3)、0.035 80.216 0μg(r=0.999 3)、0.035 8⁰.716 0μg(r=0.999 5)进样量与峰面积呈良好的线性关系,平均加样回收率分别为98.2%、98.0%、96.9%、97.7%,RSD(n=6)分别为0.85%、0.54%、0.93%、1.4%。结论方法简便、准确、灵敏、重复性好,可作为复方荆芥熏洗剂中升麻素苷、5-O-甲基维斯阿米醇苷、齐墩果酸和熊果酸的含量控制方法。     

HPLC法测定通脉活络康颗粒中齐墩果酸含量

目的:为更好的控制通脉活络康颗粒的质量,建立通脉活络康颗粒中齐墩果酸高效液相色谱测定方法。方法:采用Kromasil-ODS(4.6mm×150mm,5μm)色谱柱;流动相为甲醇-水(91∶1),流速为1.0mL.min-1,在220nm波长处检测,柱温为25℃。结果:齐墩果酸在0.126～2.016mg.ml-1浓度范围内,线性关系良好,r=0.9991,平均加样回收率97.2%,RSD为1.3%(n=5)。结论:本法简便、准确、重现性好,可以用于测定通脉活络康颗粒中齐墩果酸的含量。     

HPLC法同时测定复方痤疮胶囊中齐墩果酸和熊果酸的含量

目的：建立HPLC法同时测定复方痤疮胶囊中齐墩果酸、熊果酸的含量。方法：采用Waters symmetry-C18色谱柱（250mm×4.6mm,5μm）,流动相为甲醇-水-冰醋酸-三乙胺（87：13：0.04：0.02）,检测波长210nm,柱温为30℃。结果：齐墩果酸在10～80mg·L^-1范围内有良好线性关系（r=0.9996）,平均加样回收率为100.76%（RSD=1.86%）。熊果酸在10～80 mg·L^-1范围内有良好线性关系（r=0.9998）,平均加样回收率为100.63%（RSD=1.48%）。结论：本方法测定复方痤疮胶囊中齐墩果酸、熊果酸的含量,方法简便、准确,结果稳定,可为复方痤疮胶囊的质量评价提供依据。     

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.