十一味抗异散的质量标准

目的建立十一味抗异散的质量标准.方法采用薄层色谱法鉴别金银花、牡丹皮;高效液相色谱法测定盐酸小檗碱的含量.结果薄层色谱斑点清晰,盐酸小檗碱在12～180 μg·ml-1之间呈良好的线性关系(r=0.9997),平均回收率为99.2%,RSD=O.5%(n=6).结论所建立的方法简便、准确、专属性强,可用于十一味抗异散的质量控制.     

炎可宁片质量标准的建立

目的:建立炎可宁片的质量控制方法.方法:用薄层色谱法对炎可宁片中的大黄、黄芩进行定性鉴别;以盐酸小檗碱为对照品,采用HPLC法测定炎可宁片中盐酸小檗碱的含量.结果:薄层色谱中斑点清晰,易于识别;盐酸小檗碱线性范围0.079～0.792 μg(r =0.999 9),回收率为99.79％,RSD=1.29％(n=6).结论:本方法简便,灵敏度高,可有效地控制炎可宁片的质量.     

泌尿宁颗粒质量标准研究

目的建立泌尿宁颗粒的质量标准。方法采用薄层色谱法对泌尿宁颗粒中的黄柏、续断进行定性鉴别；以盐酸小檗碱为对照品，采用高效液相色谱法测定盐酸小檗碱含量，色谱柱：Hppersil ODS C18 (250 mm×4.6 mm，5 μm)；流动相：乙腈 磷酸二氢钾（0.1 mol·L-1） 十二烷基硫酸钠（0.025 mol·L-1）（50：25：25）；检测波长：345 nm。结果薄层色谱中斑点清晰，易于识别；盐酸小檗碱线性范围0.019 5～0.195 0 μg（r=0.999 9），回收率99.42%，RSD=0.72%（n=5）。 结论该方法简便，灵敏度高，可有效控制泌尿宁颗粒的质量。     

乳康片质量标准研究

目的 建立乳康片的质量标准.方法 采用薄层色谱法鉴别乳康片中苍术、当归、川芎、香附、连翘,采用高效液相色谱法测定该制剂中盐酸小檗碱含量.结果 薄层色谱定性鉴别分离度好,专属性强;盐酸小檗碱含量测定的线性范围为9.131～73.050 μg,平均回收率为96.41%,RSD＝1.33%（n＝6).结论 所建立的方法可靠、准确、专属性强,可用于该制剂的质量控制.     

湿热痹胶囊质量标准研究

目的:建立湿热痹胶囊的质量标准.方法:采用显微鉴别法鉴别处方中的薏苡仁,防己,连翘;采用薄层色谱法对处方防己,连翘,防风,关黄柏进行定性鉴别;采用高效液相色谱法测定盐酸小檗碱和盐酸巴马汀的含量.结果:显微特征明显;薄层色谱中可检出防己,连翘,防风,关黄柏,阴性均无干扰;盐酸小檗碱在5.2～105.1 μg· L-1范围内时,线性关系良好(r=0.999 9),盐酸巴马汀在5.2～ 104.4 μg· L-1范围内,线性关系良好(r =0.999 9);本方法平均回收率分别为97.4％,99.3％,RSD分别为1.2％,2.0％(n=6).结论:该方法准确,重复性好,可用于湿热痹胶囊的质量控制.     

胃安丸的质量标准研究

目的对胃安丸进行质量标准的研究.方法采用薄层色谱法对处方中的浙贝母、三七进行定性鉴别;采用高效液相色谱法对黄连(吴茱萸制)中的盐酸小檗碱进行含量测定.结果在薄层色谱中均可检出浙贝母、三七的特征斑点;盐酸小檗碱在0.0702～0.6318μg间线性关系良好,r=0.9999,平均加样回收率为97.31%(RSD=1.25%,n=5).结论本方法简便可行、重复性好,能有效控制该制剂的质量.     

肠炎清合剂的质量控制方法研究

目的:建立肠炎清合剂中君药黄连的鉴别及盐酸小檗碱、盐酸巴马汀含量测定方法。方法:采用薄层色谱法对合剂中黄连进行定性鉴别;采用HPLC进行含量测定。结果:薄层色谱均能明显的检出黄连的特征有效成分盐酸小檗碱和盐酸巴马汀;HPLC法中,盐酸小檗碱在1.34～42.8μg.mL-1内线性关系良好(r=0.9999),平均回收率99.3%,RSD=0.92%(n=9);盐酸巴马汀在1.24～39.8μg.mL-1内线性关系良好(r=0.9999),平均回收率98.6%,RSD=0.82%(n=9)。结论:本法简便、快速、灵敏、准确,重现性好,可以作为该合剂的质量控制方法。     

肾保康胶囊的质量标准

目的:建立肾保康胶囊的质量控制方法.方法:用薄层色谱法对肾保康胶囊中的金银花、发酵虫草菌粉进行定性鉴别;采用高效液相色谱法测定盐酸小檗碱的含量.结果:薄层色谱中斑点清晰,易于识别;盐酸小檗碱线性范围为0.0351～0.263μg,r=0.9999,平均回收率为96.30%,RSD为1.45%.结论:本方法简便,灵敏度高,可有效地控制肾保康胶囊的质量.     

肾舒颗粒质量标准研究

目的 建立肾舒颗粒(白花蛇舌草、大青叶、黄柏、甘草等)的质量标准.方法 采用薄层色谱法对制剂中的黄柏、大青叶、甘草进行鉴别,用高效液相色谱法测定黄柏中的盐酸小檗碱的含量.结果 在TLC色谱法中均能检出黄柏、大青叶和甘草.盐酸小檗碱对照品在0.00424～0.222 μg范围内线性关系良好(r=0.9999),平均回收率为101.06%,RSD为1.57%.结论 本方法简便、准确、重现性好,可用于肾舒颗粒的质量控制.     

双黄降糖胶囊质量标准研究

目的建立双黄降糖胶囊的质量标准。方法采用薄层色谱法鉴别方中黄芪、牡丹皮、丹参,高效液相色谱法测定黄连中盐酸小檗碱含量。结果薄层色谱法鉴别重现性好,阴性对照无干扰;含量测定盐酸小檗碱的线性范围为0.204～2.04μg(r=0.999 3),重现性好,平均回收率为98.54%,RSD为0.73%(n=6)。结论该方法准确可靠,重复性好,可作为双黄降糖胶囊的质量控制方法。     

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.

---

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.