五香血藤中五味子醇甲与五味子甲素含量测定

目的建立同时测定五香血藤中五味子醇甲与五味子甲素含量的高效液相色谱法。方法采用反相高效液相色谱法,C18色谱柱(4.6 mm×250 mm,5μm),乙腈(A)-水(B)为流动相,梯度洗脱,流速1 mL.min-1,五味子醇甲检测波长216 nm,五味子甲素检测波长209 nm。结果五味子醇甲在0.019 6～0.215 6μg之间线性关系良好,回收率99.11%,RSD=2.02%(n=9);五味子甲素在0.018 4～0.147 2μg之间线性关系良好,回收率102.35%,RSD=1.73%(n=9)。结论该方法简便、准确,可用于五香血藤中五味子醇甲与五味子甲素的含量测定。     

HPLC法测定八味肾气丸中五味子醇甲含量的研究

目的建立八味肾气丸中五味子醇甲含量测定的高效液相色谱法。方法采用C18柱(KR100-5C18,4,6mm×250mm,5μm),甲醇-水(65∶35)为流动相;流动速为1.0mL.min-1;检测波长为250nm。结果五味子醇甲在0.105~1.05μg范围内,线性关系良好(r=0.9999),方法平均回收率为97.82%,RSD=1.13%(n=6)。结论方法简便,结果准确,可用于八味肾气丸中五味子醇甲的定量。     

高效液相色谱法测定北五味子藤茎超临界提取物中五味子甲素、五味子乙素和五味子醇甲的含量

目的 高效液相色谱(HPLC)法测定北五味子藤茎超临界提取物中五味子甲素、五味子乙素、五味子醇甲的含量.方法 采用ODS-C18(5 μm,4.6 × 250 mm),以甲醇-水(75:25)为流动相,流速:1.0 ml/min,检测波长为254 nm.结果 五味子甲素、五味子乙素、五味子醇甲的线性范围分别为0.1～2.0μg/(r=0.9994)、0.1～2.0μg(r=0.9997)、0.12～2.0μg(r=0.9992),平均加样回收率分别为99.03%、103.60%、99.80%,RSD分别为1.72%、2.09%、1.33%(n=5).结论 本方法简便准确、重现性好,能有效测定北五味子藤茎超临界提取物中五味子甲素、五味子乙素、五味子醇甲的含量.     

五子衍宗丸中五味子醇甲的含量测定

目的建立五子衍宗丸中五味子醇甲含量的测定方法。方法采用高效液相色谱法,色谱柱为钻石ODS柱(200mm×4.6mm,5μm),流动相为甲醇-水(64∶36),流速为1.0mL/min,检测波长为250nm,柱温为室温。结果五味子醇甲进样量线性范围是0.1076～1.614μg,r=0.9999,方法平均加样回收率为98.03%,RSD=1.04%(n=9)。结论该方法可用于测定五子衍宗丸中五味子醇甲的含量。     

HPLC法测定六味五灵片中五味子醇甲的含量

目的采用高效液相色谱法测定六味五灵片中五味子醇甲的含量。方法采用高效液相色谱法,使用色谱柱为Agilent SB-C18柱(4.6 mm×250 mm,5μm),以乙腈-水为流动相,流速:1.0 mL·min-1,检测波长为250 nm,柱温:40℃。结果五味子醇甲在0.010 1～0.404 4μg范围内线性关系良好,r=1.000,平均回收率为99.87%,RSD=0.39%。结论本法可用于测定六味五灵片中五味子醇甲含量。     

HPLC同时测定益脑胶囊中五味子醇甲和五味子乙素的含量

目的建立使用高效液相色谱法同时测定益脑胶囊中五味子醇甲、五味子乙素的含量,完善、提高益脑胶囊的质量标准。方法 Dikma RP-C18(250mm×4.6mm,5μm)色谱柱;流动相:乙腈(A)-0.1%磷酸溶液(B);检测波长:250nm;体积流量:1.0m L/min;柱温:30℃。结果该方法的五味子醇甲线性范围在0.01577~1.5768μg(r=0.9999),平均回收率为103.1%,RSD为1.0%。五味子乙素线性范围在0.004160~0.2080μg(r=0.9999),平均回收率为101.7%,RSD为1.2%。结论该方法可行、重复性好,能有效控制益脑胶囊中五味子的质量。     

高效液相色谱法测定琥珀安神丸中五味子醇甲含量

目的建立测定琥珀安神丸中五味子醇甲含量的高效液相色谱(HPLC)法。方法色谱柱为kromasil C18柱(250 mm×4.6 mm,5μm),流动相为甲醇-水(65∶35),流速为0.8 mL/min,检测波长为250 nm,柱温为室温。结果五味子醇甲进样量的线性范围为0.047 08～0.235 4μg,r=1.000 0(n=5),平均回收率为97.98%,RSD=0.88%(n=6)。结论该法简便、快速、准确,可用于产品的质量控制。     

HPLC法测定参芪消渴胶囊中五味子醇甲的含量

目的:建立高效液相色谱法(HPLC)测定参芪消渴胶囊中五味子醇甲的含量.方法:采用Agilent HC-C18(4.6 mm×250 mm,5μm)色谱柱;流动相为以甲醇为流动相A,水为流动相B,进行梯度洗脱;检测波长为250 nm,结果:五味子醇甲在0.0924～2.31μg范围内线性关系良好(r=0.999 9),平均回收率为99.58%,RSD为0.92%(n＝6).结论:本方法可作为参芪消渴胶囊的质量控制方法.     

高效液相色谱法测定复方益肝灵片中五味子醇甲、五味子醇乙和五味子甲素的含量

目的建立益肝灵片中五味子醇甲、五味子醇乙和五味子甲素含量测定的高效液相色谱法。方法采用Ag-ilent TC-C18(4.6 mm×250 mm,5μm)色谱柱;流动相为甲醇-水(73∶27);流速:1.0 mL.min-1;检测波长:250 nm;柱温为室温。结果五味子醇甲、五味子醇乙、五味子甲素分别在0.105～2.1、0.041 2～0.824、0.018 8～0.376μg与峰面积有良好的线性关系;平均回收率分别为97.8%、98.1%、97.3%,RSD分别为1.2%、1.9%、0.82%。结论所建立的操作简单,重现性好,适用于复方益肝灵片中五味子醇甲、五味子醇乙和五味子甲素的含量测定。     

HPLC法测定无糖型宁心安神糖浆中五味子醇甲和五味子乙素

目的建立无糖型宁心安神糖浆中五味子醇甲和五味子乙素的测定方法。方法采用KromasilC18色谱柱(250mm×4.6mm,5μm),流动相:甲醇-水(73:27),检测波长:250nm,柱温:30℃,体积流量:1.0mL/min,进样体积:10μL。结果五味子醇甲、五味子乙素分别在0.16～1.6μg(r=0.9999)和0.04～0.40μg(r=0.9991)呈良好的线性关系,平均加样回收率分别为100.00%、100.04%,RSD分别为0.60%、0.18%(n=6)。结论该方法简便、准确、重现性好,可作为无糖型宁心安神糖浆质量控制的方法。     

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.

     

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.     

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.     

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.     

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.