Tween胶束体系中水杨酸铜络合物的SOD样活性

合成了水杨酸铜络合物并分析了其组成，提纯了Tween-20,-40,-60,-80,并测定了它们在pH7．4的磷酸缓冲液中的CMC，用Cyt.c，还原法分别测定了水杨酸铜络合物在不同介质中的SOD样活性，详细研究了表面活性剂与水杨酸铜络合物协同清除O2^-的作用，观察到在胶束体系中水杨酸铜络合物的SOD样活性明显高于缓冲液体系无表面活性剂时的SOD样活性，表面活性剂本身也具有清除O2^-的功能，抗红细胞膜脂质过氧化实验也得到类似结果，这可用胶束催化解释，水杨酸铜－Tween体系可能是一种潜在的抗炎药物。     

脂质体的电性对水杨酸铜SOD样活性的影响(英文)

采用细胞色素c法研究了水杨酸铜分别在中性、正负电性脂质体中SOD样活性的变化情况。证明中性脂质体包裹的水杨酸铜的SOD样活性比水杨酸铜在水溶液中提高了3倍多。但正负电性脂质体包裹的水杨酸铜的SOD样活性降低。并发现在实验浓度范围内,负电性脂质体包裹的水杨酸铜,活性变化无规则,且荷负电量多的脂质体包裹的水杨酸铜促进超氧自由基的歧化,而荷负电量少的脂质体仅在低浓度区对超氧的歧化表现为促进作用。     

两种Cu(Ⅱ)一姜黄素络合物作为SOD拟物和自由基清除剂的比较研究

对Cu(Ⅱ)一姜黄素以1:1(络合物1)和1:2(络合物2)两种不同化学计量关系形成的络合物进行了清除自由基和抗氧化活性对比实验,以了解化学计量关系与结构的改变对它们抗氧化活性的影响。1)用EPR光谱分析溶于J:DMSO中的络合物1和2,结果证实这两种络合物的结构分别为扭曲的斜方型和对称的正方平面型。而前者的结构具有更高的SOD活性。2)通过细胞色素C(Fe~(2+))吸收法研究2个     

大黄十五种化合物的SOD样活性研究

研究中草药中具有SOD样活性的有效成分，可以为进一步开发利用中草药提供科学依据，从我国药材大黄中分离出四类化合物，作者分别测定其中十五种化合物的SOD样活性，用其对超氧负离子自由基的清除率表示，实验结果表明，四类化合物的SOD样活性不同：大黄鞣质的儿茶精类化合物的SOD样活性较强，其中以（－）－表儿茶精的活性最强；芪甙类化合物的活性相对较弱；而大黄酚－8－葡萄糖甙和去氧土大黄甙不但无SOD样活性，还有促进超氧负离子自由基生成的作用。     

口服外源SOD的完整生物大分子吸收的研究

分别用Cu2+,降解成多肽的无活性的SOD和完整SOD对ICR小鼠灌胃,发现Cu2+不引起血液中红细胞SOD的活性变化,而降解后的无活性的SOD却能使红细胞中SOD活性升高,可见降解后的SOD片段可能诱导了内源SOD的生成,口服完整的SOD也能使其活性升高,通过Western-blotting分析,找到了完整的SOD分子经胃肠道吸收、穿过了红细胞膜,进入了红细胞内的证据.     

SOD脂质体生产新工艺研究

建立了一种适于工业生产SOD脂质体的工艺,即将已有的冷冻-融化法改进为冷冻干燥法.产品为冻干态SOD脂质体,使SOD包封率由近50%提高到65%以上,渗漏也大大减少.产品水化后振荡即可重新形成脂质体.产品稳定性增强,常温下12mo分散度无明显改变,粒径多为0.66μm,适合作为化妆品添加剂.在提高包封率方面,膜材须选用氧化指数小的新制备的蛋黄卵磷脂SOD应溶于4mmol/L PBSpH 7.4中以保持其活性.     

超氧化物歧化酶脂质体的制备及其药物动力学

采用逆相蒸发法制得稳定的 SOD 脂质体,其包封率为54.76±4.81%。研究了两种 SOD 脂质体(Ⅰ和Ⅱ)在兔体内的药物动力学,其半衰期分别为5.94±1.95h 和5.85±2.11h。小鼠给予脂质体Ⅱ后SOD 活性以脾、肺和肝组织中最高,肾、心、脑次之,胃中无规律性。     

SOD基因的组织结构、表达与分子克隆

超氧化物歧化酶（SOD）是一种天然的含金属抗氧化酶，它具有抗衰老、抗辐射和消炎等多种疗效。SOD包括Cu/Zn-SOD、Mn-SOD和Fe-SOD三类，其中以Cu/Zn-SOD为最重要。SOD均由核内染色体上的基因编码，这类基因既有单拷贝序列，也有多基因家庭。线粒体和叶绿体内的SOD在核内合成后，再分泌到细胞器中。多数SOD基因的表达都具有组织特异性，并受许多环境因素的诱导，有关的分子机理正在研究中，并且正在尝试SOD基因的分子克隆以及重组SOD基因在培养细胞和转基因植物中的表达。     

SOD脂质体在小鼠体内的分布及其对脂质过氧化物的影响

目的 优化超氧化物岐化酶(SOD)脂质体的制备工艺,并考察SOD脂质体和SOD溶液在小鼠体内组织的分布.方法 采用逆相蒸发法和正交试验优化工艺制备SOD脂质体;以邻苯三酚自氧化法和脂质过氧化物法确定药物在小鼠体内组织的分布.结果 SOD脂质体的各质量评价结果良好.与SOD溶液相比,前者可提高各组织中SOD的含量,并降低脂质过氧化物水平,以血、脑、肾等最为显著.注射SOD脂质体小鼠的各组织中SOD增量最高可达102.9%,脂质过氧化物含量最低降至25.0%.结论 所得SOD脂质体有较高的包封率和稳定性,在小鼠体内具有明显的缓释和降低脂质过氧化物含量的效果.     

五灵脂类SOD活性研究

实验表明给小鼠五灵脂提取液，小鼠血液SOD活性增强，测定五灵脂有类SOD活性，在pH4.5-8.5，温度25－100℃条件下活性稳定。     

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.