尿石通颗粒中总黄酮的含量测定

目的:测定尿石通颗粒中总黄酮的含量。方法:用70％乙醇提取并制成供试品,采用分光光度法测定。结果:平均回收率为98.28％,RSD=2.13％。3批尿石通颗粒样品中总黄酮的含量分别为1.448,1.403,1.427 mg·g~(-1)。结论:本方法简便、准确、灵敏度高,可作为该制剂的质量控制方法。     

石淋通颗粒质量标准的研究

目的制定石淋通颗粒的质量标准。方法对处方中的广金钱草进行了薄层鉴别。用紫外分光光度法测定了制剂中总黄酮的含量。检测波长为274nm。结果薄层鉴别方法专属性强,含量测定通过方法学考察,总黄酮以芦丁计在0.050125mg~0.30075mg范围内,呈良好的线性关系。芦丁的平均回收率为99.40%(n=9),RSD为0.93%。结论方法简便、准确、重现性好。可用于控制石淋通颗粒质量。     

葫芦茶的质量研究

目的　建立葫芦茶的质量控制方法。 方法 　用薄层色谱法对葫芦茶中的芦丁进行定性鉴别 ;用紫外分光光度法测定葫芦茶中总黄酮的含量。结果 　薄层色谱中斑点清晰 ,易于识别 ;紫外分光光度法精密度、重现性良好 ;芦丁在 9.2μg· m L- 1 ～ 5 5 .2μg· m L- 1 范围内呈线性关系 ,r= 0 .9998。平均加样回收率 98.86%,RSD=2 .2 1%( n=9)。 结论 　本法可有效地控制葫芦茶的质量     

肾石通颗粒质量标准研究

目的制定肾石通颗粒质量控制方法。方法采用TLC法对方中的扁艹蓄、牛膝进行定性鉴别;采用比色法对方中金钱草的总黄酮进行含量测定。结果本品定性鉴别薄层色谱特征明显,专属性强;总黄酮在0.008~0.048g·L-1,范围内具有良好的线性关系(r=0.9996),平均回收率为101.31%。结论该方法可以准确地进行定性、定量检测,有效地控制肾石通颗粒的质量。     

碎石利排汤质量标准的研究

目的:探讨建立碎石利排汤的质量控制方法.方法:用薄层色谱法对碎石利排汤中的金钱草进行定性鉴别,并采用分光光度法对总黄酮进行含量测定.结果:薄层色谱分离效果好,斑点清晰,易于识别;平均加样回收率98.4%(n=5),RSD=2.6%.结论:该方法较简单,重现性好,可作该制剂质量控制标准.     

银冬颗粒中总黄酮含量的测定

目的:建立紫外分光光度法测定银冬颗粒中总黄酮含量的方法.方法:紫外分光光度法测定总黄酮的含量,检测波长为510 nm.结果:总黄酮的检测浓度在6.45～51.6μg· mL-1范围内与吸光度呈良好线性关系(r=0.9997);平均回收率为99.85％,RSD=2.35％ (n=5).结论:该方法的精密度,重复性,稳定性,加样回收率良好,能用于银冬颗粒的质量控制.     

降脂颗粒的制备及质量控制

目的建立降脂颗粒的制备及质量控制方法,为考察其内在质量提供依据。方法采用薄层色谱法鉴别丹参、枸杞;采用紫外分光光度法,测定总黄酮的含量,检测波长为510nm。结果表明芦丁标准品在0.15~0.901范围内呈线性关系。平均回收率x=96.36%,RSD=1.25%(n=5)。结论本方法简便、准确,适合于医院制剂配制检验。     

降脂颗粒的制备及质量控制

目的建立降脂颗粒的制备及质量控制方法,为考察其内在质量提供依据。方法采用紫外分光光度法测定总黄酮的含量,检测波长为510nm;采用薄层色谱法鉴别丹参、枸杞子。结果表明芦丁对照品在0.15～0.901mg范围内呈线性关系,平均回收率96.36%,RSD=1.36%(n=5)。结论方法简便、准确,适合于医院制剂配制及检验。     

肿节风片的质量标准研究

目的:制订肿节风片质量标准。方法:紫外分光光度法测定了总黄酮的含量,对肿节风药材进行了薄层色谱鉴别。结果:加标回收率平均98.1 % (RSD=2.3% ,n=6) ,r=0.99996,重复性RSD =1.23% (n=6) ,精密度RSD=1.14 % (n =6)结论:方法稳定、可靠,可作为该制剂的质量控制方法之一。     

复方槐花颗粒质量标准研究

目的:建立复方槐花颗粒的质量标准。方法:采用薄层色谱(TLC)法对方中槐花、丹参、金银花进行定性鉴别;采用紫外分光光度法测定槐花中芦丁的含量。结果:TLC斑点清晰、分离度好。芦丁的检测浓度在2.904~14.52μg.mL-1范围内与峰面积积分值呈良好线性关系(r=0.9977);平均加样回收率为98.43%,RSD=0.55%(n=6)。结论:所建标准可用于复方槐花颗粒的质量控制。     

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.     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

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.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.