用D101大孔吸附树脂富集仙茅中苯甲酸酯类酚苷的工艺研究

目的:研究用D101大孔吸附树脂富集仙茅中苯甲酸酯类酚苷的纯化工艺。方法:以仙茅苷乙和仙茅苷的吸附量和解吸附率为指标,考察了D101大孔吸附树脂对仙茅中苯甲酸酯类酚苷的静态和动态吸附及解吸附性能。结果:D101大孔吸附树脂富集仙茅中苯甲酸酯类酚苷的最佳工艺条件如下:吸附时间为8h,药液pH值为6,洗脱溶剂pH值为8,上样吸附和洗脱均在室温下进行,药液中苯甲酸酯类酚苷浓度为0.22mg/ml为最佳上样浓度,吸附流速为2.5Bv/h,洗脱溶剂为30%乙醇,洗脱剂用量为12Bv,二次纯化样品中苯甲酸酯类酚苷浓度为0.17mg/ml。结论:本纯化工艺简单、稳定,能将仙茅中仙茅苷和仙茅苷乙的总含量从0.022%的平均含量提高到1.60%,经二次纯化含量能达到5.08%。     

大孔树脂分离纯化独一味总黄酮的工艺研究

目的 研究大孔树脂分离纯化独一味总黄酮的工艺条件与技术参数.方法 采用高效液相色谱法测定山栀苷甲酯和8-0-乙酰山栀苷甲酯的含量,紫外分光光度法测定独一味中总黄酮的含量.结果 D-101树脂对独一味总黄酮的富集效果最好.吸附条件为药液质量浓度1 g/mL,原液室温上样,吸附流速3 BV/h,洗脱剂为70%乙醇,洗脱流速5 BV/h,洗脱剂用量为10 Bv.结论 试验工艺稳定、可行.     

应用大孔树脂吸附分离技术制备地锦草总黄酮的研究

目的研究大孔树脂DA201和D101富集地锦草总黄酮的工艺条件和参数。方法以总黄酮含量为指标,采用正交试验设计,考察DA201和D101富集地锦草总黄酮的工艺条件。用分光光度法测定总黄酮含量。结果DA201精制的最佳工艺为:90 mL浓度约0.65 mg.mL-1的溶液(pH 7)上柱,吸附流速2 BV.h-1,洗脱剂为40%乙醇(pH 7),洗脱流速2 BV.h-1。D101精制的最佳工艺为:100 mL浓度约0.65 mg.mL-1溶液(pH 7)上柱,吸附流速4 BV.h-1,洗脱剂为40%乙醇(pH 9),洗脱流速2 BV.h-1。通过DA201和D101精制工艺,平均吸附率分别为83.38%和88.57%,平均洗脱率分别为89.28%和87.21%,洗脱液干燥后的总固物中总黄酮平均含量分别为14.48%和20.18%,分别高于原上样液总固物黄酮含量(8.49%和8.71%)。结论DA201和D101对地锦草总黄酮都有良好吸附分离性能,而D101综合性能更好。     

黄蜀葵花总黄酮的大孔树脂纯化工艺

目的选择5种大孔树脂分别对黄蜀葵花总黄酮进行静态与动态的吸附和解吸,筛选纯化黄蜀葵花总黄酮的最佳树脂。方法研究影响分离的各种因素如上样流速、上柱浓度和洗脱剂等优化分离工艺。结果研究结果表明：D101树脂宜于黄蜀葵花总黄酮的提纯,最佳工艺为：流速1BV·h^-1,黄蜀葵花总黄酮水溶液的上样浓度为4．15g·L^-1,乙醇为洗脱剂,洗脱浓度为70％。结论经D101树脂吸附分离纯化后,总黄酮含量提高15倍以上。     

HPD-600大孔吸附树脂对淫羊藿总黄酮的动态吸附洗脱性能研究

目的:研究HPD-600大孔吸附树脂对淫羊藿总黄酮的动态吸附洗脱性能,为分离淫羊藿总黄酮提供最佳吸附洗脱条件。方法:以总黄酮吸附量、醇洗物总黄酮含量、总黄酮回收率为考察指标,考察HPD-600大孔吸附树脂分离纯化淫羊藿总黄酮的动态吸附洗脱条件。结果:淫羊藿提取物上样浓度为20 mg·ml-1,药液的pH调节为5～6时,最大上样量为260ml,以2 mg·ml-1流速吸附,洗脱时采用70%乙醇为洗脱剂,洗脱剂用量为6倍量树脂体积(Br),以2 ml·min-1的流速进行洗脱,树脂可重复使用3次为最佳工艺条件。结论:在上述条件下,用HPD-600吸附分离淫羊藿总黄酮,乙醇洗脱物中总黄酮含量达45%以上,总黄酮解析率达85%以上,总黄酮纯度可达80%。     

大孔树脂D113吸附分离苹果原花青素的研究

目的：优选大孔树脂吸附分离苹果原花青素的工艺条件.方法：选用3种不同极性大孔吸附树脂D113、DM130和ADS-17对苹果提取液中原花青素的吸附性能进行研究,以pH、样品流速、乙醇浓度、乙醇流速为考察因素,以吸附率和解吸率为评价标准.结果：D113树脂分离效果较好,吸附率达到68.1％,吸附量为5.91 mg·g-1树脂.最佳工艺是pH为7的原花青素粗提液以0.8 ml·main-的流速上柱吸附,再用体积分数40％的乙醇、以0.8 ml·main-1的流速进行解吸.结论：D113大孔极性树脂适用于吸附分离苹果原花青素.     

大孔吸附树脂纯化黄芩4种黄酮类成分的工艺研究

目的:筛选纯化黄芩4种黄酮类成分的最佳树脂型号并优化其工艺条件。方法:以黄芩中黄芩苷、汉黄芩苷、黄芩素、汉黄芩素4种成分含量为指标,通过对大孔吸附树脂吸附性能和解吸附性能考察,确定黄芩4种黄酮类成分的最佳纯化工艺。结果:D101型大孔吸附树脂对黄芩4种黄酮类成分纯化效果最好,其纯化的最佳工艺条件为:上样浓度40mg(生药)/m L,上样流速2 BV/h,径高比为1:10,最大上样量为6 BV;洗脱剂75%乙醇,洗脱流速3 BV/h,洗脱剂用量为7 BV。结论:D101型大孔吸附树脂纯化工艺稳定,简单可行,适用于工业生产。     

大孔吸附树脂纯化鹿药总皂苷和总黄酮的研究

目的优化鹿药总皂苷和总黄酮成分的大孔吸附树脂分离纯化最佳工艺。方法以总皂苷和总黄酮为考察指标,对大孔吸附树脂的类型以及样品溶液的质量浓度、pH值、洗脱剂的体积分数、用量进行了优化,同时对大孔吸附树脂的重复性、使用周期进行考察。结果优选出D101大孔吸附树脂作为富集、纯化总皂苷和总黄酮的上柱树脂;获得D101大孔吸附树脂柱层析各项优化参数,即上样液质量浓度为1.5g生药.mL-1(其中皂苷质量浓度为6.52mg.mL-1,黄酮质量浓度为4.81mg.mL-1),上样液pH为4.0～5.0,依次用8BV水、4BV体积分数30%乙醇和4BV体积分数70%乙醇以2BV.h-1的流速洗脱,收集体积分数70%乙醇洗脱液。结论优选出的工艺稳定可行。     

大孔吸附树脂对红花多糖脱色工艺的影响研究

目的:探讨大孔吸附树脂对红花多糖脱色工艺的影响。方法:采用单因素试验,以脱色率和多糖保留率作为评价指标,比较AB-8、HPD-400A、HPD-100、HPD-750、D101、ADS-17等6种不同型号大孔吸附树脂在温度、多糖浓度、pH值、吸附流速、洗脱剂5个方面对红花多糖脱色效果的影响。结果:HPD-100大孔吸附树脂对红花多糖的脱色率和保留率较为理想。最佳工艺为40℃,多糖浓度为5 mg·mL-1,pH值为4,流速为1 ml·min-1,洗脱剂为pH 4的蒸馏水。在该条件下色素的吸附率可达86.71%,多糖保留率为72.10%。结论:HPD-100大孔树脂对红花多糖可以获得较高的脱色率和保留率。     

正交试验优选葛根、山楂降脂有效部位的纯化工艺

目的:评价大孔吸附树脂纯化葛根、山楂降血脂有效部位的可行性及优选其工艺条件和参数。方法:比较4种大孔吸附树脂对葛根总异黄酮、山楂总黄酮、山楂总三萜酸的吸附性能;以树脂吸附量为指标,对大孔吸附树脂纯化葛根、山楂降血脂有效部位的工艺进行筛选。结果:AB-8大孔吸附树脂对葛根、山楂降血脂有效部位的吸附性能最好,其纯化的最佳条件为原液浓度0·13g生药/ml、流速0·5ml/min、pH值与原液相同(3·5左右)、洗脱剂80%乙醇溶液、洗脱流速2ml/min;纯化后有效部位的纯度达到85%以上。结论:AB-8大孔吸附树脂可用于葛根、山楂降血脂有效部位的纯化,且工艺可行,树脂再生容易。     

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.

     

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.     

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.     

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.     

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.