RP-HPLC法测定上清丸(大蜜丸)中黄芩苷含量

目的建立高效液相色谱法测定上清丸中黄芩苷含量的方法.方法采用Diamonsil-C18色谱柱(150 mm×4.6 mm,5μm),流动相为甲醇-水-磷酸(43570.205),柱温为25℃,流速为1.0 ml·min-1,检测波长为280 nm.结果黄芩苷在浓度为16.3～260.8 μg·ml-1时线性关系良好,r=0.999 9平均回收率为99.4%RSD为1.5%(n=6).结论该法简便,可靠,准确,可作为上清丸的质量控制.     

HPLC法测定龙胆泻肝丸中黄芩苷的含量

目的:用HPLC法测定龙胆泻肝丸中的黄芩苷的含量。方法:采用Nova-Pak C18柱(3.9 mm×150 mm,4μm),以甲醇-水-冰醋酸(45∶55∶1)为流动相,流速1.0 ml/min,检测波长275 nm。结果:对照品在0.815~4.075μg/ml范围内呈线性关系(r=0.999 6),加样回收率平均为99.4%,RSD为1.12%。结论:本方法简便、准确、重复性好,可用于测定龙胆泻肝丸中黄芩苷的含量。     

高效液相色谱法测定一清胶囊中黄芩苷的含量

目的 建立一清胶囊中黄芩苷的含量测定方法.方法 色谱柱为ODS柱(Kromasil 250mm×4.6mm,5μm),DAD检测器;流动相:甲醇0.2mol/L磷酸水溶液(47:53),流速为1ml/min,柱温25℃,检测波长为280nm.结果 黄芩苷在0.08～0.40μm范围内呈良好的线性关系(r=0.9998);加样回收实验中平均回收率为99.8%,RSD为2.56%(n=5).结论 本法操作简捷,结果 准确可靠,适用于一清胶囊中黄芩苷的含量测定.     

高效液相色谱法测定牛黄清火丸中黄芩苷的含量

目的:建立牛黄清火丸中黄芩苷的含量测定方法.方法:采用高效液相色谱法.色谱柱:Thermo ODS-2HYPERSIL C18(250 mm×4.6 mm,5μm),流动相:甲醇-0.4%磷酸溶液(45:55,V/V),流速:1.0ml·min-1,检测波长:312 nm,柱温:30℃.结果:黄芩苷在-.01～0.06 mg·ml-1范围内线性关系良好(r=0.999 6);平均加样回收率为99.06%,RSD=0.8%(n=9).结论:方法简便易行,结果准确可靠,可适用于牛黄清火丸的质量控制.     

HPLC法测定青果丸中黄芩苷的含量

目的:建立测定青果丸中黄芩苷含量的方法。方法:采用高效液相色谱法。色谱柱为Agilent TC-C18(150 mm×4.60mm,5μm),流动相为甲醇-水-0.02 mol/l磷酸(45∶55∶0.2,V/V/V),流速为1.0 ml/min,柱温为30℃,进样量为10μl,检测波长为278 nm。结果:黄芩苷检测质量浓度在10²00μg/ml范围内与峰面积积分值呈良好的线性关系(r=0.999 9,n=6);精密度、稳定性、重复性试验的RSD≤0.96%;平均加样回收率为99.53%,RSD=1.07%(n=9)。结论:该方法简便、准确、重复性好,可用于青果丸中黄芩苷的含量测定。     

高效液相色谱法测定金砂五淋丸中黄芩苷含量

目的 建立高效液相色谱法测定金砂五淋丸中黄芩苷含量的方法.方法 色谱柱为迪马BDS C18(250 mn×4.6 mm,5 μm),流动相为甲醇-0.05%磷酸溶液(49:51),检测波长为280nm,流量1.0 ml/min.结果 黄芩苷在0.20-1.00μg范围内线性关系良好,其回归方程为Y=22614753x-182777(r=0.999 7),平均回收率为98.0%(RSD=1.3%,n=5).结论 该方法操作简便、准确,重现性好,可用于金砂五淋丸的质量控制.     

HPLC法测定利胆消石丸中黄芩苷的含量

目的:建立HPLC法测定利胆消石丸中黄芩苷含量的方法。方法:采用Shim-pack VP-ODS色谱柱(150 mm×4.6 mm,5μm),流动相为甲醇-水-磷酸(47:53:0.2),检测波长280nm,流速1.0ml·min~(-1),柱温加℃。结果:黄芩苷在0.24～1.21μg(r=0.999 9)范围内呈良好的线性关系;平均加样回收率为101.1%,RSD=2.0%(n=6)。结论:该方法简便,准确,可用于利胆消石丸的质量控制。     

基于高效液相色谱法的儿童清肺丸中汉黄芩苷含量测定

目的 采用高效液相色谱法建立儿童清肺丸中汉黄芩苷的含量测定方法,以期为儿童清肺丸的质量控制提供参考。方法 采用高效液相色谱法测定儿童清肺丸中汉黄芩苷含量,色谱柱为Agilent Eclipse XDB-C₁₈(4.6 mm×150 mm, 5μm),流动相为乙腈-0.4%磷酸溶液(27∶73),流速为1.0 ml/min,检测波长为276 nm,柱温为30℃,进样体积为10μl。结果 该方法的精密度、稳定性、重复性均符合要求,汉黄芩苷在9.92～74.40μg/ml(r=0.999 8)范围内与峰面积呈良好线性关系,平均加样回收率为100.92%,RSD为1.08%(n=9),6批儿童清肺丸中汉黄芩苷含量在0.55～0.64 mg/g范围内。结论 基于高效液相色谱法建立的儿童清肺丸中汉黄芩苷含量测定方法操作简便、精密、准确、专属性强,可作为儿童清肺丸中汉黄芩苷的质量控制方法。     

HPLC法测定坤宝丸中黄芩苷的含量

目的:建立坤宝丸中黄芩苷的HPLC含量测定方法.方法:采用Diamonsil C18柱(250mm×4.6mm, 5μm),甲醇-0.1%磷酸溶液(52:48)为流动相,检测波长280nm,流速0.8 ml·min-1.结果:黄芩苷在0.39-2.36μg范围内,呈良好的线性关系(r=0.9999),平均加样回收率为99.9% (RSD=1.7%, n=5).结论:本方法简便、快速准确,可较好的控制该制剂的质量.     

高效液相色谱法测定耳聋丸中黄芩苷含量的研究

目的:建立耳聋丸中黄芩苷含量测定方法。方法:采用高效液相色谱法,Diamonsil(钻石)C185μ200×4.6mm色谱柱,流动相为甲醇-水-磷酸(50∶50∶0.2);流速:1.0ml/min;检测波长:280nm,进样量在0.0792~1.584μg范围内呈线性关系,平均回收率为98.6%,RSD0.45%。结论:方法简便、准确、快速,可作为耳聋丸中黄芩苷的含量测定方法。     

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.