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Immobilized phospholipid capillary electrophoresis (IPCE) was developed for studying the interactions between a set of nonsteroidal anti-inflammatory drugs (NSAIDs) and membrane and predicting the biological activity of NSAIDs. Supported vesicle layers and supported phospholipid bilayers were attached to the inner surface of a capillary wall simply by rinsing with liposome solutions. The liposomes, composed of soybean phosphatidylcholine (SPC) or SPC and different proportions of cholesterol (Ch), were small unilamellar vesicles prepared by sonication. The normalized capacity factor (K(IPCE)) was introduced into IPCE for evaluating drug-membrane interactions. Related theories and equations were derived to calculate K(IPCE) values from apparent migration time of a solute and electroosmotic flow. The strong relationships were observed between logK(IPCE) (SPC) values and logK(lw) values (the partition coefficients determined in free SPC-liposome partitioning system) (R=0.9855 and P<0.0001) or logK(ILC) values (the normalized capacity factors determined by immobilized POPC-liposome chromatography, POPC represents 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine) (R=0.9875 and P<0.0001). In addition, logK(IPCE) (SPC/Ch 80:20%) values correlated well with the pIC50 (the minus logarithm of IC50) values for cyclooxygenase 2 determined on intact cells (R=0.959 and P<0.001). These results confirmed that IPCE, K(IPCE) value as evaluation index, can be effectually used for studying drug-membrane interactions and it has the potential to predict drug activity. Cholesterol-containing (20 mol%) liposomes may be more suitable to mimic real cell membrane. 相似文献
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以乙二醇为溶剂,采用溶剂热法合成出由纳米晶组装而成的Cu2ZnSnS4(CZTS)微球。采用X射线衍射仪(XRD)、拉曼光谱仪(Raman)、扫描电子显微镜(SEM)、透射电子显微镜(TEM)、紫外-可见漫反射光谱(DRS)对所得微球的结构与成分、颗粒大小与形貌和光学性质进行了测试分析。研究结果表明:溶剂热法制得的CZTS粉体具有四方晶相结构,微球由纳米晶组装而成,对可见光有良好的吸收;随着反应时间的增加,颗粒尺寸逐渐增大,且对形貌有一定影响;此外,文中还对CZTS微球的形成机理做了推测。 相似文献
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The binding model of 3-(2-chloropyrid-5-ylmethylamino)-2-cyanoacrylate photosystem Ⅱ (PSⅡ) electron transport inhibitors with the D 1 protein of PSII was built. The high herbicidal activity of this kind of inhibitors was explained by docking studies: in addition to usual factors, the N atom on the pyridine ring could form an H-bond with the backbone amide of Phe265 on the D1 protein. 3D-QSAR analysis on sixteen 3-(2-chloropyrid-5-yl- methylamino)-2-cyanoacrylate compounds was performed using CoMFA method to explain the nature of interactions between the compounds and D1 protein. These studies may provide useful insights for designing new PSII electron transport inhibitors. 相似文献
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硝酸镧对大鼠肝脏的亚慢性毒性实验研究 总被引:14,自引:0,他引:14
以大鼠为对象,连续用生理盐水和20,10,2,0.2,0.1mg.kg^-1La(NO3)3灌胃6个月后,观察了体重,肝体比变化;检测了血清中谷草转氨酶,谷丙转氨酶,碱性磷酸酶和δ-谷氨酰转移酶含量的变化,应用组织化学及透射电镜技术观察了不同剂量La(NO3)3对大鼠肝脏形态结构的影响。20mg/kg^-1La(NO3)3组动物体重增长缓慢,0.1mg.kg^-1La(NO3)3组动物体重增加较快;20mg/kg^-1La(NO3)3组肝脏汇管区有炎细胞浸润,有些肝细胞内有少量的脂滴,糖原减少,线粒体基质密度增高,有电子密度高的致密体,肝细胞核形态正常或轻度变形。 相似文献