槐花米中药用有效成分芦丁提取方法研究

本实验以槐花米中芦丁含量和粗品提取率为评价指标,采用L9(34)正交试验,对影响槐花米的水提取效果的各因素(药材的粉碎度、溶剂用量、提取次数、放置析晶时间)进行选择,最后筛选出的工艺稳定、可行、提取率及含量较高,有较高利用价值.     

槐花米中芦丁提取的优化研究

目的 研究槐花米中芦丁的最佳提取工艺条件.方法 根据芦丁的物理性状,通过单因素水平试验分析了槐花米的粉碎度、表面活性剂、超声温度、超声时间、乙醇浓度、料液比,设计了6个因素对芦丁提取率的影响.结果 与结论 最佳提取工艺条件是:槐花米粉碎至5号筛粒度,50℃加料液比(1:20)的100%乙醇超声5min,在搅拌下加入质量比(1:20)的吐温20.     

微波法提取槐花米中的芦丁

目的　优选槐花米中芦丁的最佳提取工艺。方法　以槐花米为原料 ,水为溶剂 ,利用微波辐射提取芦丁。结果　在微波功率为 2 7.2～ 30 .6W的条件下 ,回流提取 (2 4min× 4 ) ,收率 17%。结论　微波加热法提取芦丁 ,方法简便、快速、高效。     

超声提取法测定槐花中总黄酮含量

目的:用超声提取法测定槐花中总黄酮含量。方法:采用60%的乙醇超声提取槐花中的总黄酮,采用紫外可见分光光度法,在500 nm波长处测吸光度,计算样品中总黄酮的含量。结果:芦丁对照品溶液在4.0～20.0μg·mL-1范围内线性关系良好,平均回收率为99.7%,RSD=0.98%(n=5)。结论:本方法工艺简单,采用超声提取、纯化方法得到的黄酮类物质其纯度较高,并且测定总黄酮含量的方法可靠。     

煎器对提取芦丁的影响

目的:研究不同煎器从槐花米中提取芦丁的影响。方法:用6种不同材料的容器(不锈钢、搪瓷、铜、铝、铁及陶瓷),分别以水为溶剂煎煮槐花米,分别用分光光度法、薄层扫描法测定煎出液中芦丁含量。结果:分光光度法不能正确地反映不同容器提取芦丁的得率,而薄层扫描法能正确反映不同容器提取芦丁的得率。结论:传统的中药罐和不锈钢器皿是最有效的提取芦丁煎器,能较好地使芦丁在提取过程中保持稳定;而铜铁煎器最不利于提取芦丁。     

复方槐花颗粒中槐花和侧柏叶总黄酮提取工艺的优化

目的 优选复方槐花颗粒中槐花和侧柏叶总黄酮最佳提取工艺。方法 采用超声浸提法对复方槐花颗粒中槐花和侧柏叶总黄酮进行提取,以乙醇体积分数、超声功率、超声时间和料液比为考察因素,通过单因素试验和正交优选,确定较优提取工艺,并与常规的热回流提取法进行比较研究。结果 超声浸提法最佳提取工艺条件为：用60%乙醇,在料液比1:10和超声功率40kHz条件下超声波辅助连续提取2次,每次15min,槐花和侧柏叶总黄酮提取率可达93.31%。结论 该工艺研究为复方槐花颗粒中槐花和侧柏叶总黄酮共提提供一种新方法和思路,具有耗时短、能耗低、溶剂用量少和提取效率高等优势。     

煎器对提取芦丁的影响

目的：研究不同煎器从槐花米中提取芦丁的影响。方法：用6种不同材料的容器（不锈钢、搪瓷、铜、铝、铁及陶瓷），分别以水为溶剂煎煮槐花米，分别用分光光度法、薄层扫描法测定煎出液中芦丁含量。结果：分光光度法不能正确地反映不同容器提取芦丁的得率，而薄层扫描法能正确反映不同容器提取芦丁的得率。结论：传统的中药罐和不锈钢器皿是最有效的提取芦丁煎器，能较好地使芦丁在提取过程中保持稳定；而铜铁煎器最不利于提取芦丁。     

苦杏仁3种提取工艺中苦杏仁苷提取率的比较

目的比较3种杏仁提取工艺中苦杏仁苷提取率.方法以硝酸银滴定法测量3种苦杏仁提取工艺中苦杏仁苷的含量并计算提取率.结果 3种提取方法提取率,分别为95.77%、64.88%、55.61%,其中蒸馏苦杏仁水法最高,醇提苦杏仁苷法次之.结论三种提取方法均可得到较高的提取率.     

正交试验优化独子藤果实中雷公藤红素的醇提工艺

目的:优选独子藤果实中雷公藤红素的醇提工艺。方法:采用高效液相色谱法测定雷公藤红素的含量。以提取时间、提取次数、料液比为考察因素,以雷公藤红素的提取率为考察指标设计正交试验,并进行验证试验。结果:最优醇提工艺为45%甲醇提取3次、每次2 h、料液比1∶8;验证试验中,雷公藤红素的平均提取率为0.917 mg/g(RSD=2.85%,n=3)。结论:本研究优化的醇提工艺稳定可行、提取率较高,适用于独子藤果实中雷公藤红素的提取。     

正交优选苣荬菜中总黄酮的提取工艺

目的:探讨苣荬菜中总黄酮的提取工艺方法.方法:以总黄酮为指标,采用L9(34)正交设计实验,考察了乙醇浓度、提取时间、料液比和提取次数对提取率的影响,优选出合理的提取工艺.结果:将苣荬菜用25倍50%乙醇提取3次,每次30 min,可以获得较高的提取率.结论:正交实验工艺有效成分提取率高,方法快速、简单.     

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.