正交实验法优选青皮的醇提工艺

目的优选青皮的最佳醇提工艺。方法以橙皮苷为标样,采用HPLC归一化法测定出的总黄酮提取率为考察指标,先比较不同浓度的乙醇对青皮的提取效果,然后采用L9(34)正交试验法,考察乙醇用量、提取时间及提取次数对提取效果的影响。结果 60%乙醇的提取效果最好,提取次数对考察指标具有显著性影响。结论青皮的最佳醇提工艺为加8倍药材量的60%乙醇,加热回流提取3次,每次1.0h。     

正交设计优选健脾颗粒中橙皮苷的提取工艺

目的：优选健脾颗粒中橙皮苷的提取工艺。方法：以处方中的主要药效成分橙皮苷含量为观察指标,采用正交设计法筛选最佳提取工艺条件。结果：最佳提取方法为回流1.0 h、加95%甲醇50 ml。结论：优选的提取方法为健脾颗粒中橙皮苷含量测定提供可靠方案,保证产品质量。     

榅桲子总黄酮提取工艺研究

目的 优选榅桲子中总黄酮的最佳提取工艺条件.方法 以芦丁为对照品,用分光光度法在506 nm波长处测定榅桲子总黄酮含量,优选总黄酮的提取工艺.结果 测得样品中总黄酮含量为13.60 mg•g-1,最佳提取工艺：乙醇浓度为75%,料液比1：10(倍)、回流时间 2.5 h,回流温度60 ℃,提取3次.结论 选用芦丁为对照品,用紫外分光光度法测定榅桲子总黄酮含量准确度较高,方法 简便,切实可行.     

大孔树脂分离纯化青皮中总黄酮的工艺研究

目的:研究大孔树脂分离纯化青皮中总黄酮的工艺参数.方法:以总黄酮的含量为评价指标,通过动态吸附与解吸附实验研究,筛选大孔树脂分离纯化青皮中总黄酮的最佳工艺.结果:吸附工艺:上样液浓度为0.25 g·ml-1,上样量为1.1 g·g-1树脂,树脂径高比为1:8;洗脱工艺为5倍柱体积水洗除杂,10 倍柱体积 50%乙醇洗脱.所得中间体总黄酮含量90%以上.结论:大孔树脂具有较好的分离纯化青皮中总黄酮的应用价值.     

泽漆中总黄酮超声提取工艺优化研究

目的研究泽漆总黄酮超声提取法的最佳提取工艺,在此基础上采用分光光度法测定不同部位总黄酮的含量。方法正交设计试验寻找超声提取法提取泽漆总黄酮的最佳工艺条件,以芦丁为考察指标,通过分光光度法对泽漆不同部位总黄酮含量进行精密测定。结果乙醇浓度50%,物料比1∶25,超声提取时间20 min,超声提取温度60℃为最佳提取工艺。泽漆叶中总黄酮含量最高,根次之,茎最低。结论优选的泽漆总黄酮提取工艺方法,简便易行,快速灵敏,实验结果准确可靠。     

唐古特白刺中总黄酮提取工艺的研究

目的研究唐古特白刺中总黄酮的最佳提取工艺。方法采用单因素试验确定唐古特白刺中总黄酮的最佳提取条件,通过紫外分光光度法测定总黄酮含量,并用正交试验确定各因素的影响大小。结果温度对唐古特白刺中总黄酮的提取影响作用最大,唐古特白刺中总黄酮的最佳提取工艺为乙醇75%、料液比1∶7、温度85℃、提取4次(2h.次-1)。结论本研究可为唐古特白刺中总黄酮工业化提取提供理论依据。     

正交设计优选满山红总黄酮的提取工艺

目的优选满山红的提取工艺.方法采用正交设计对满山红提取工艺优化,用紫外分光光度法测定满山红中总黄酮成分含量.结果满山红总黄酮的最佳提取工艺为60%乙醇15倍量回流提取2次,每次1 h.结论此法简单可行方法重现性好,适用于工业化生产.     

正交试验优化中药萹蓄中总黄酮的提取工艺

目的利用索氏提取法提取萹蓄中总黄酮,并应用分光光度法对总黄酮含量进行测定。方法以总黄酮为考察参数,通过正交试验优化提取工艺。结果体积分数为7 0%的乙醇溶液、提取时间为1.5 h、提取温度85℃、m(萹蓄)∶V(乙醇)=1 g∶40 L时为最佳提取工艺。结论通过最佳工艺条件下测定萹蓄中总黄酮的萃取率为15.40%,总黄酮含量质量分数为0.308%,回收率在99.8%～102.4%之间,RSD=0.957%(n=5)。     

用正交设计法优选老鹰茶总黄酮的提取工艺

目的优选老鹰茶总黄酮提取的最佳工艺.方法以芦丁为对照,AlCl3为显色剂,用紫外分光光度法在410 nm处测定总黄酮含量,以总黄酮含量为指标,应用正交实验,优选老鹰茶总黄酮提取的最佳工艺.结果老鹰茶总黄酮的最佳提取工艺为80%乙醇,12倍量,回流提取3次,每次2 h.结论紫外分光光度法方便、快捷,可用于老鹰茶总黄酮提取工艺的优选.     

正交试验优选醋制青皮的炮制工艺

目的优选醋制青皮的最佳炮制工艺。方法以橙皮苷的含量为考察指标,考察加醋量、焖润时间、炒制温度、炒制时间对指标成分含量的影响。结果最佳炮制工艺为加10%醋,焖润时间3h,炒制温度200℃,炒制时间8min。结论提取工艺设计合理、结果可靠,为优化醋制青皮的最佳炮制工艺提供了理论依据。     

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.