葛根总黄酮对大强度耐力训练大鼠不同组织Mg2+-ATPase活性的影响

以成年雄性Sprague Dawley(SD)大鼠为研究对象，通过递增强度跑台训练建立大强度耐力训练运动模型，研究了葛根总黄酮对大强度耐力训练大鼠对心肌、肝脏、肾脏、脑和股四头肌组织的Mg^2 -ATPase活性的影响．结果表明，葛根总黄酮能使耐力训练大鼠心肌、肝脏、肾脏、脑和股四头肌组织的Mg^2-6ATPase活性显著升高，具有提高细胞膜泵的工作效率，增强膜维持胞内外离子分布与平衡的功能．     

Synthesis, Structure and H+/K+-ATPase Inhibitory Activity of Novel Triazolyl Substituted Tetrahydrobenzofuran Derivatives via One-pot Three-component Click Reaction

Eleven triazolyl substituted tetrahydrobenzofuran derivatives were synthesized in high yields as novel H⁺/K⁺‐ATPase inhibitor via one‐pot CuI‐catalyzed three‐component click reaction of azide, secondary amine and 3‐bromopropyne under mild conditions in water. Their structures were characterized by NMR, IR, ESI‐MS, elemental analysis and single‐crystal X‐ray diffraction analysis. Most of the target compounds exhibited better H⁺/K⁺‐ATPase inhibitory activity than commercial omeprazole with IC₅₀ values less than 15 µmol·L^?1. The initial structure‐activity analysis suggested that the triazole substituted by cycloalkyl, aromatic ring or O‐containing side‐chain seemed to be beneficial for enhancing the activity.     

Synthesis and Crystal Structure of （E）-2-phenyl-6,7dihydrobenzofuran-4（5H）-one O-cyanomethyl Oxime

A pair of E/Z-isomers of 2-phenyl-6,7-dihydrobenzofuran-4（5H）-one O-cyanomethyl oxime,C16H14N2O2,as potential drugs for treating peptic ulcer and other acid-related diseases have been synthesized and characterized by IR,MS and NMR spectra.Meanwhile,the crystal of IIIa was obtained and determined by X-ray single-crystal diffraction.Crystal data： monoclinic system,space group P21 /c,a = 8.423（8）,b = 19.596（16）,c = 8.770（8）,β = 107.750（12）°,V = 1379（2）3,Z = 4,F（000） = 560,Dc = 1.283 g/cm3,μ = 0.086 mm 1,R = 0.0681 and wR = 0.2029 for 14472 independent reflections（Rint = 0.0782） and 2428 observed ones（I 2σ（I））.     

Structural Insights into the Interactions of Digoxin and Na+/K+-ATPase and Other Targets for the Inhibition of Cancer Cell Proliferation

Digoxin is a cardiac glycoside long used to treat congestive heart failure and found recently to show antitumor potential. The hydroxy groups connected at the C-12, C-14, and C-3′a positions; the C-17 unsaturated lactone unit; the conformation of the steroid core; and the C-3 saccharide moiety have been demonstrated as being important for digoxin’s cytotoxicity and interactions with Na⁺/K⁺-ATPase. The docking profiles for digoxin and several derivatives and Na⁺/K⁺-ATPase were investigated; an additional small Asn130 side pocket was revealed, which could be useful in the design of novel digoxin-like antitumor agents. In addition, the docking scores for digoxin and its derivatives were found to correlate with their cytotoxicity, indicating a potential use of these values in the prediction of the cancer cell cytotoxicity of other cardiac glycosides. Moreover, in these docking studies, digoxin was found to bind to FIH-1 and NF-κB but not HDAC, IAP, and PI3K, suggesting that this cardiac glycoside directly targets FIH-1, Na⁺/K⁺-ATPase, and NF-κB to mediate its antitumor potential. Differentially, digoxigenin, the aglycon of digoxin, binds to HDAC and PI3K, but not FIH-1, IAP, Na⁺/K⁺-ATPase, and NF-κB, indicating that this compound may target tumor autophagy and metabolism to mediate its antitumor propensity.     

有机磷农药对小白菜中可溶性蛋白质及SOD、Mg2+-ATPase、Ca2+-ATPase和CAT的影响

使用一定浓度甲胺磷农药喷洒小白菜后,测定7d中其可溶性蛋白质及抗氧化酶（SOD、CAT、和蛋白酶Mg^2＋-ATPase、Ca^2＋-ATPase）的含量变化．结果表明,喷药后可溶性蛋白质在第2～4天含量比对照组减小,随后呈上升趋势;SOD和CAT在第2～6天均高于对照;而Mg^2＋-ATPase、Ca^2＋-ATPase第1～4天与对照相差不大,第5、6天略高于对照;第7天各物质都基本还原到与对照接近或持平．说明有机磷农药喷洒后致使植物体内产生了大量氧自由基,进而诱导细胞内防御活性氧自由基毒害的物质产生．     

希土化合物对离体巨噬细胞的影响

本文应用细胞培养法和单细胞阳离子测定系统研究了希土化合物以地巨噬细胞的影响，结果表明，在培养介质中ＳｍＣｌ３和Ｙｃｌ３的浓度大于１ｍｍｏｌ．ｄｍ＾－３时，有明显的细胞毒性，Ｙｃｌ３的细胞毒性大于ＳｍＣｌ３，ＳｍＣｌ３和ＹＣｌ３的细胞毒性明显大于Ｓｍ（Ａｌａ）３Ｃｌ３和Ｙ（Ａｌａ）２Ｃｌ３。希土化合物的作用使细胞（Ｃａ＾２＋ｉ）升高；毒性越大，Ｃａ＾２＋ｉ升高越甚。低浓度Ｓｍ＾３＋和Ｙ６３＋对细胞膜     

尼罗罗非鱼在淡、海水中Na~+-K~+-ATPase活性变化

用ATPase活性测试盒测定了尼罗罗非鱼鳃和肾中Na+-K+-ATPase活性在海、淡中的变化.从淡水到海水中,尼罗罗非鱼鳃和肾Na+-K+-ATPase活性分别增强了1.61倍和1.41倍;把尼罗罗非鱼由淡水直接放入海水,鳃中的Na+-K+-ATPase活性升高较剧烈,在前期(0.5 h)最高,在鱼即将死亡的后期(8 h)次之,在中期(3 h)较低;肾中Na+-K+-ATPase活性升高较缓慢,在前期较小,中期较高,后期最高.除了在淡水中,肾的Na+-K+-ATPase活性高于鳃外,在海水中以及海水的前期、中期和后期中,鳃的Na+-K+-ATPase活性都高于肾,与肾相比,鳃对肾盐协迫更为敏感.     

盐胁迫下植物质膜H+-ATPase研究进展

质膜H -ATPase在植物细胞的跨膜物质转运、胞内pH值调节以及植物对环境胁迫的响应等诸多方面具有重要作用,是植物生命活动过程的主宰酶.盐胁迫是影响植物生长发育的主要环境因子,植物质膜H -ATPase活性的调节是植物适应盐环境、提高耐盐性的重要细胞机理.综述了植物质膜H -ATPase活性变化及其调节机理对盐胁迫响应的研究状况,对质膜H -ATPase活性调节机理研究中仍未解决的问题进行了展望.     

IDENTIFICATION OF MEMBRANE PROTEINS IMAGED BY ATOMIC FORCE MICROSCOPY USING A TEMPLATE MATCHING ALGORITHM

The atomic force microscope allows to image biological samples in their native environment. But the identification and the topography of individual randomly distributed membrane proteins is still a challenge. We used membranes of isolated vacuoles of barley mesophyll cells. Images at low resolution indicate that vacuoles spontaneously attach, rupture and finally adsorb completely as planar membrane to mica. Height profiles indicate that the membrane at the peripheral boundary exposes the extravacuolar surface to the scanning tip. At molecular resolution a template matching correlation algorithm was used to identify the most abundant membrane protein, the vacuolar H⁺-ATPase by the characteristic extravacuolar head of the transport molecule. The data indicate the possibility to analyse single randomly distributed membrane proteins in their native environment with the knowledge of a suitable template.     

Modeling the effect of external electric field and current on the stochastic dynamics of ATPase nano-biomolecular motors

The rotary motion of the F₀ part of the F₀F₁-ATPase motor that synthesizes the ATP molecules used by the intracellular stepping motors, such as kinesins, is modeled within a stochastically fluctuating medium via the application of the Langevin dynamics wherein the random intramembrane fluctuations are represented by a white noise. We have investigated the influence of an applied electric field and an applied electric current on this rotary motion, and the subsequent production rate of the ATP molecules. It is seen that the application of a field, or a current, changes both the elastic behavior of the cell membrane and the transmembrane potential. These changes in turn transform the dynamics of the F₀ part of the motor. We have found that at low fields, the role of transmembrane potential becomes significant in the production rate of the ATP molecules, whereas at high fields the changes induced in the surface tension of the membrane also contribute to the production rate of the ATP.