延胡索醇提工艺的优选

目的优选延胡索的醇提最佳工艺。方法以延胡索乙素含量和醇溶性浸出物为评价指标,采用正交设计法优选延胡索的提取工艺。结果延胡索的最佳提取工艺为:粗粉,加75%乙醇提取2次,第1次加9倍量醇提取1.5 h,第2次加7倍量醇提取1.0 h。结论优选出的工艺简单可行,可用于延胡索的提取。     

正交试验法优选消妇炎胶囊的煎煮工艺

目的优选消妇炎胶囊的煎煮工艺。方法采用正交试验法,以干浸膏收率、60%乙醇浸出物含量和没食子酸提取量为考核指标,对消妇炎胶囊的煎煮工艺进行考察。结果消妇炎胶囊的最佳煎煮工艺为加10倍量水,煎煮2次,每次煎煮2 h。结论该工艺干浸膏收率、60%乙醇浸出物含量和没食子酸提取量都较稳定,可作为煎煮提取的最佳工艺。     

温胃胶囊提取工艺研究

目的优选出温胃胶囊挥发油提取和醇提工艺的最佳参数。方法采用正交试验法,以浸泡时间、加水量、提取时间3因素3水平,以挥发油提取率为考察指标,优选挥发油提取工艺;以乙醇体积分数、加醇量、提取时间3因素3水平,以醇浸膏得率和总黄酮含量为考察指标,优选醇提工艺。结果与结论温胃胶囊挥发油提取的最佳工艺参数为浸泡2h,加10倍量水,水蒸气蒸馏8h;醇提最佳工艺参数为加6倍量体积分数60%乙醇提取2h。     

正交试验法优选妇痛安片醇提部分的工艺研究

目的优选成药妇痛安片醇提部分的最佳工艺。方法正交设计法,考察延胡索乙素提取量、总固体物得率两个指标。结果优选出的提取工艺为:70%乙醇提取两次,加醇量分别为8倍、6倍,提取时间分别为1.0h、0.5h。结论本工艺适合大生产。     

正交试验优选盆炎康栓提取工艺

目的:优选盆炎康栓的提取工艺。方法:采用正交试验法,以绿原酸、丹酚酸B及干膏收率作为水提评价指标,以延胡索乙素和干膏收率为醇提评价指标,优选盆炎康栓提取工艺。结果:水提工艺中,提取次数对水提效果有显著影响,而加水量和提取时间无显著影响。最佳水提工艺为:8倍加水量,提取2次,每次提取1 h。醇提工艺中,乙醇浓度对提取效果有较大影响,而提取时间、加醇量无显著影响。醇提最佳工艺为:60%乙醇,6倍量,每次1.5 h,提取2次。结论:优选的提取方法稳定、合理、可行。     

正交试验法优选胃乐舒颗粒的醇提工艺

目的：优选胃乐舒颗粒药材中醇溶性成分的提取工艺.方法：以延胡索乙素、木香烃内酯、去氢木香内酯提取量和浸膏收率为评价指标,采用正交试验设计确定最佳醇提工艺.结果：胃乐舒颗粒最佳提取工艺为：加6倍量的80%乙醇,加热回流3次,每次1 h.结论：该提取工艺高效、稳定,适用于大生产.     

正交试验法优选胃灵片的乙醇提取工艺

目的优选胃灵片的最佳乙醇提取工艺。方法采用正交试验法,以浸膏收率和延胡索乙素提取率为指标,考察醇溶性成分的提取工艺。结果最佳工艺为5倍量85%乙醇回流提取3次,每次1 h。结论优选出的工艺为胃灵片的提取提供了实验依据。     

正交试验优选清肝利胆胶囊醇提工艺

目的:优选清肝利胆胶囊醇提工艺。方法:以大黄总蒽醌含量、乙醇浸出物量、三氯甲烷萃取物量和正丁醇萃取物量为综合指标,乙醇提取量、提取次数、提取时间为考察因素,通过正交试验优选清肝利胆胶囊最佳醇提工艺。结果:最佳醇提工艺为加8倍量80%乙醇提取2次,每次1.5h。结论:该提取工艺合理、简单可行,可为大生产提供理论依据。     

正交试验法优选冠心康胶囊挥发油提取工艺条件

目的:优选冠心康胶囊中川芎、当归、桂枝挥发油的提取工艺条件。方法:采用水蒸气蒸馏法提取川芎、当归、桂枝挥发油,以挥发油的收率作为评价指标,选择加水量、浸泡时间及提取时间等为主要影响因素,应用L9(34)正交试验设计选取最佳提取工艺条件。结果:水蒸气蒸馏法提取川芎、当归、桂枝挥发油最佳工艺条件为加8倍量的水,浸泡0.5h,蒸馏提取7h。结论:优选所得提取工艺条件稳定可行。     

损伤复元颗粒的醇提工艺研究

目的 优选损伤复元颗粒的最佳醇提工艺。方法以丹参酮ⅡA、阿魏酸、浸出物为指标,采用正交试验法,考察加乙醇量、乙醇浓度、提取次数、提取时间四个因素,对损伤复元颗粒的最佳醇提工艺进行优选。结果最佳醇提工艺为加饮片总量15倍量80％乙醇回流提取2次,每次1h。结论优选得到的最佳醇提工艺稳定、合理。     

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.