桑白皮总黄酮的镇咳祛痰作用

目的研究桑白皮总黄酮镇咳祛痰作用。方法采用浓氨水、SO2小鼠引咳法,小鼠气管酚红排泌及大鼠气管毛细管分泌液模型,观察桑白皮黄酮的镇咳祛痰作用。结果125 mg.kg-1显著抑制浓氨水、SO2所致小鼠咳嗽潜伏期,减少氨水引咳次数,桑白皮总黄酮250 mg.kg-1显著减少SO2引咳次数。桑白皮总黄酮125 mg.kg-1增加小鼠气管酚红排泌,桑白皮总黄酮180 mg.kg-1显著增加大鼠气管分泌液。结论桑白皮总黄酮具有镇咳祛痰作用。     

桑皮苷的镇咳平喘作用

目的探讨桑皮苷镇咳、祛痰、平喘作用。方法采用小鼠浓氨水引咳法、小鼠SO2引咳法和豚鼠枸橼酸引咳法制造3种引咳模型,灌胃给予桑皮苷,以咳嗽潜伏期、咳嗽次数为评价指标,观察桑皮苷的镇咳作用;采用豚鼠磷酸组胺喷雾法制作引喘模型,以引喘潜伏期为评价指标,观察桑皮苷的平喘作用;采用小鼠酚红排痰法制作祛痰模型,以酚红排泌量为观测指标,观察桑皮苷的祛痰作用。结果桑皮苷80 mg.kg-1能明显抑制浓氨水引咳的潜伏期,桑皮苷80 mg.kg-1能明显抑制浓氨水引咳次数,桑皮苷20 mg.kg-1g能明显抑制SO2引咳次数,桑皮苷50 mg.kg-1能明显抑制枸橼酸引咳次数;桑皮苷100 mg.kg-1对组胺引起豚鼠支气管哮喘具有明显的平喘作用;桑皮苷质量浓度提高到160 mg.kg-1,对小鼠酚红排出量仍无影响。结论桑皮苷具有镇咳、平喘作用,但无祛痰作用。     

南芪北芪祛痰、镇咳和平喘作用的实验研究

目的:观察南蓖与北芪在祛痰、镇咳及平喘作用中效果的异同,为南芪的广泛运用提供实验依据.方法:通过小鼠气管酚红法、家鸽纤毛运动实验、小鼠浓氨水引咳法、豚鼠枸橼酸引咳法及豚鼠组胺-乙酰胆碱超声雾化法观察两者的祛痰镇咳平喘作用.结果:南芪、北芪均能增加小鼠气管酚红排泌量,促进家鸽气管内墨汁运动,明显减少氨水引发小鼠咳嗽反应的次数和枸橼酸引发豚鼠咳嗽反应的次数,并延长咳嗽潜伏期,对抗组胺-乙酰胆碱引起的豚鼠支气管哮喘.结论:两者均具有良好的祛痰、镇咳及平喘作用,且效果无显著差异.     

浙贝乙素胆汁酸盐的制备及其镇咳、祛痰和平喘活性的筛选

为了寻找具有优良镇咳、祛痰和平喘活性且毒性较低的药物，将贝母中的主要药效成分之一浙贝乙素和蛇胆中各主要药效成分进行酸碱反应,得到一系列浙贝乙素胆汁酸盐并对所得的盐进行镇咳、祛痰和平喘活性的筛选。活性筛选结果显示，浙贝乙素胆酸盐和浙贝乙素鹅去氧胆酸盐的镇咳、祛痰和平喘活性较强，尤其是二者显示出比磷酸可待因还强的镇咳活性值得关注。借鉴药物化学中的结构拼合思路有望在中药复方的研究开发中开辟出一条新的途径。     

熊胆贝母止咳胶囊对动物的镇咳袪痰解热作用

目的研究熊胆贝母止咳胶囊的解热、镇咳、袪痰作用。方法观察熊胆贝母止咳胶囊对酵母菌致大鼠发热作用的影响;采用氨水致豚鼠、小鼠咳嗽法观察其镇咳作用;小鼠气管酚红排痰量法、大鼠毛细管排痰量法观察其祛痰作用。结果熊胆贝母止咳胶囊对酵母致热有微弱的解热作用,含生药4.44、2.22 g.kg-1的熊胆贝母止咳胶囊能明显减少豚鼠和小鼠的咳嗽次数,同时有显著促进小鼠由气管排泌酚红、增加大鼠排痰量的作用。结论熊胆贝母止咳胶囊具有显著的镇咳、祛痰及微弱的解热作用。     

复方护肺颗粒镇咳袪痰平喘的药效学作用

目的:研究复方护肺颗粒的镇咳、袪痰、平喘作用。方法:采用枸橼酸引咳法和喷雾致喘法观察复方护肺颗粒对豚鼠的镇咳和平喘作用,采用气管对酚红的排泌法观察复方护肺颗粒对小鼠化痰作用。结果:与对照组比较,复方护肺颗粒能使豚鼠咳嗽潜伏期、哮喘潜伏期明显延长;可使小鼠气管粘膜排泌的酚红量增加。结论:复方护肺颗粒具有良好的镇咳、化痰、平喘作用。     

沙参提取物镇咳祛痰及免疫增强作用研究

目的：以沙参提取物作为受试物,观察其镇咳祛痰作用及对免疫功能的影响。方法：采用豚鼠枸橼酸引咳法、小鼠酚红排泌试验法观察沙镇咳祛痰作用;采用碳粒廓清法和二硝基氟诱导小鼠迟发型变态反应试验法,观察沙参对非特异性免疫功能和特异性细胞免疫功能的影响。结果：结果显示沙参乙醇和乙酸乙酯提取物对豚鼠枸橼酸引咳具有显著的对抗作用,乙酸酯提取并有显著地促进小鼠酚红排泌作用。沙参多糖及水提取物能显著地增加碳 粒清指数     

镇咳平喘颗粒镇咳、祛痰作用的实验研究

目的观察镇咳平喘颗粒的主要药理作用。方法采用小鼠因氨水所致咳嗽法、豚鼠因枸橼酸所致咳嗽法观察其镇咳作用;小鼠呼吸道酚红排痰量法、大鼠毛细管排痰量法观察其祛痰作用。结果镇咳平喘颗粒可以延长小鼠因氨水所致的咳嗽潜伏期及因枸橼酸所致豚鼠的咳嗽潜伏期,同时减少咳嗽次数;可以增加小鼠呼吸道的酚红排痰量及增加大鼠毛细管的排痰量。结论镇咳平喘颗粒具有镇咳、祛痰作用。     

熊胆贝母止咳胶囊对动物的镇咳祛痰解热作用

目的 研究熊胆贝母止咳胶囊的解热、镇咳、祛痰作用.方法 观察熊胆贝母止咳胶囊对酵母菌致大鼠发热作用的影响;采用氨水致豚鼠、小鼠咳嗽法观察其镇咳作用;小鼠气管酚红排痰量法、大鼠毛细管排痰量法观察其祛痰作用.结果 熊胆贝母止咳胶囊对酵母致热有微弱的解热作用,含生药4.44、2.22 g·kg<'-1>的熊胆贝母止咳胶囊能明显减少豚鼠和小鼠的咳嗽次数,同时有显著促进小鼠由气管排泌酚红、增加大鼠排痰量的作用.结论 熊胆贝母止咳胶囊具有显著的镇咳、祛痰及微弱的解热作用.     

肺清颗粒药效学作用初探

目的研究肺清颗粒镇咳、祛痰、平喘和抗菌作用。方法以小鼠氨水引咳法、小鼠枸橼酸引咳法和豚鼠枸橼酸引咳法观察其镇咳作用;以小鼠酚红排泌法观察其祛痰作用;以豚鼠乙酰胆碱-组胺引喘法和豚鼠离体气管条试验观察其平喘作用;采用抑菌圈测定法观察肺清颗粒的体外抑菌作用。结果肺清颗粒对小鼠氨水引咳具有显著的镇咳作用,对乙酰胆碱-组胺所致的豚鼠哮喘具有显著的平喘作用;对组胺或乙酰胆碱致痉的豚鼠离体气管条有显著的解痉作用;体外对金黄色葡萄球菌、肺炎球菌和肺炎克雷伯菌有一定的抑制作用。结论肺清颗粒对实验动物具有显著的镇咳、祛痰及平喘作用,并具有一定的抗菌作用。     

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.     

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.