Chiral interaction in Gly-capped N-terminal motif of 3(10)-helix and domino-type induction in helix sense

Chiral interaction of helical peptide with chiral molecule, and concomitant induction in its helix sense have been demonstrated in optically inactive nonapeptide (1) possessing Gly at its N-terminus: H-Gly-(Delta(Z)Phe-Aib)(4)-OCH(3) (1: Delta(Z)Phe = Z-dehydrophenylalanine; Aib = alpha-aminoisobutyric acid). Spectroscopic measurements [mainly nuclear magnetic resonance (NMR) and circular diochroism (CD)] as well as theoretical simulation have been carried out for that purpose. Peptide 1 in the 3(10)-helix tends to adopt preferentially a right-handed screw sense by chiral Boc-L-amino acid (Boc: t-butoxycarbonyl). Induction in the helix sense through the noncovalent chiral domino effect should be derived primarily from the complex supported by the three-point coordination on the N-terminal sequence. Thus the 3(10)-helical terminus consisting of only alpha-amino acid residues enables chiral recognition of the Boc-amino acid molecule, leading to modulation of the original chain asymmetry. Dynamics in the helix-sense induction also have been discussed on the basis of a low-temperature NMR study. Furthermore, the inversion of induced helix sense has been achieved through solvent effects.     

N-Arachidonyl-glycine inhibits the glycine transporter, GLYT2a

N-arachidonyl-glycine is one of a series of N-arachidonyl-amino acids that are derived from arachidonic acid. N-arachidonyl-glycine is produced in a wide range of tissues with greatest abundance in the spinal cord. Here we report that N-arachidonyl-glycine is a reversible and non-competitive inhibitor of glycine transport by GLYT2a, but has little effect on glycine transport by GLYT1b or gamma-amino butyric acid transport by GAT1. It has previously been reported that the activity of GLYT2a is down-regulated by protein kinase C and therefore we investigated whether the actions of N-arachidonyl-glycine on GLYT2a are mediated by second messenger systems that lead to the activation of protein kinase C. However, the protein kinase C inhibitor, staurosporine, had no effect on the actions of N-arachidonyl-glycine on GLYT2a. Thus, the actions of N-arachidonyl-glycine are likely to be mediated by a direct interaction with the transporter. We have further defined the pharmacophore by investigating the actions of other N-arachidonyl amino acids as well as the closely related compounds arachidonic acid, anandamide and R1-methanandamide. Arachidonic acid, anandamide and R1-methanandamide have no effect on glycine transport, but N-arachidonyl-l-alanine has similar efficacy at GLYT2a to N-arachidonyl-glycine, and N-arachidonyl-gamma-amino butyric acid is less efficacious. These observations define a novel recognition site for the N-arachidonyl amino acids.     

城镇化过程中流域不透水面演变格局——以天津于桥水库流域为例

不透水面是衡量流域城镇化发展状况的一个关键指标,其扩展对流域生态水文过程产生重要影响.本文以天津于桥水库流域为例,在ENVI 5.1软件支持下,利用遥感影像获取1984、1994、2004和2013年4个时相的不透水面信息,采用修正后的归一化水体指数剔除水体信息,排除水体对不透水面提取精度的影响,运用线性光谱混合分析法生成流域不透水表面指数(ISA),并对其时空演变格局进行分析.结果表明: 模型均方根误差(RMSE)为0.005,像元精度为85.4%,试验结果准确可靠.1984—2013年,流域内不透水面覆盖度ISA平均值从0.16线性增长到0.23,在全流域范围内的不透水面面积增加了4.9%,其总不透水面面积增加近1倍.不透水面沿城镇区域呈现辐射式增长,沿子流域路网呈现填充式增长.不透水面覆盖度为中等等级的斑块形状不规则,破碎化程度最高.整个流域景观破碎化程度和多样性均逐年增高,人为干扰强度不断增大.     

0.7 MPa(7ATA)高气压下大鼠脊髓突触体甘氨酸摄取的变化

目的:研究氮麻醉时甘氨酸神经递质功能变化。方法:制备脊髓突触体,用同位素方法观察0.7MPa(7ATA)高压空气环境中大鼠脊髓突触体摄取甘氨酸的情况。结果:0.7MPa(7ATA)时甘氨酸摄取速度减慢,达到饱和摄取量时间延长,最大饱和摄取量下降。甘氨酸摄取的Vm减小,Km增加。在加入10-7mol.L-1皮质酮后,可增加0.7MPa(7ATA)高压空气时甘氨酸摄取Vm。结论:在高气压下发生氮麻醉时,甘氨酸摄取转运体的功能降低,与甘氨酸亲和力下降;皮质酮有助于高亲和力甘氨酸转运体功能恢复。     

增效混剂对神经细胞钠通道的抑制作用

应用膜片钳技术,以MN-9D神经细胞为材料研究了溴氰菊酯及辛硫磷混剂的增效机理。膜片钳实验表明10^-5mol/L辛硫磷对Na⁺通道电流抑制作用很小,并随作用时间延长而逐步恢复。加药1 min Na⁺电流抑制率为6.99%,10 min为3.65%。10^-6 mol/L溴氰菊酯1 min抑制率为20.28%,10 min为21.43%。对蜚蠊中枢神经系统传导的动作电位抑制中时为53 min;10^-6mol/L溴氰菊酯与10^-5 mol/L辛硫磷混剂1 min抑制率为34.15%,10 min为36.69%,动作电位抑制中时为40 min,因此混剂可增强对Na⁺通道电流的抑制作用。通过Na⁺电流数据、尾电流衰减时间常数统计分析表明溴氰菊酯的修饰作用主要发生在关闭和静止状态的Na⁺通道,减缓通道的打开,延长通道关闭或失活状态。     

基于生物多样性保护的兴安落叶松与白桦最佳混交比例——以阿尔山林区为例

选取内蒙古阿尔山林区7种不同混交比例的松桦混交林,包括落叶松纯林、白桦纯林及5种不同比例的混交林为研究对象。对植物和昆虫种群丰富度、多样性进行了研究,并对种群在乔木层混交状况梯度下的分布进行了分析。结果表明:植物和昆虫种群分布受乔木层混交状况影响显著。同时,郁闭度能改变其分布状况及决定于松桦比例。兴安落叶松和白桦混交比例介于5∶5和7∶3之间时最有利于森林多样性,是进行林分疏伐的理想模式。     

兔孤束核腹外侧区微量注射谷氨酸钠及甘氨酸对弓状核诱发电位的影响

实验在６６只麻醉、制动,断双侧颈迷走神经和人工通气的家兔上进行。通过微量注射神经元胞体兴奋剂谷氨酸钠和神经元胞体抑制剂甘氨酸,改变孤束核腹外侧区神经元兴奋活动,探讨对下丘脑弓状核诱发电位的影响及其可能的机制和意义。实验结果如下：（１）孤束核腹外侧区微量注射谷氨酸钠,可使膈神经放电显著增加和使弓状核诱发电位Ｐ２及Ｎ２波幅显著降低;而微量注射甘氨酸则使膈神经放电显著减少和使弓状核诱发电位Ｐ２及Ｎ２波幅显著增大。（２）静脉注射纳洛酮对谷氨酸钠引起的膈神经放电兴奋效应无明显影响,但能翻转谷氨酸钠对弓状核诱发电位Ｐ２及Ｎ２波幅的抑制效应。提示：孤束核腹外侧区呼吸神经元的兴奋活动可扩散至弓状核,并对弓状核诱发电位产生影响,此影响可能是由内源性阿片系统参与而实现的。     

Differential mechanism of light-induced and oxygen-dependent restoration of the high-potential form of cytochrome b559 in Tris-treated Photosystem II membranes

The effect of illumination and molecular oxygen on the redox and the redox potential changes of cytochrome b₅₅₉ (cyt b₅₅₉) has been studied in Tris-treated spinach photosystem II (PSII) membranes. It has been demonstrated that the illumination of Tris-treated PSII membranes induced the conversion of the intermediate-potential (IP) to the reduced high-potential (HP^Fe2+) form of cyt b₅₅₉, whereas the removal of molecular oxygen resulted in the conversion of the IP form to the oxidized high-potential (HP^Fe3+) form of cyt b₅₅₉. Light-induced conversion of cyt b₅₅₉ from the IP to the HP form was completely inhibited above pH 8 or by the modification of histidine ligand that prevents its protonation. Interestingly, no effect of high pH or histidine modification was observed during the conversion of the IP to the HP form of cyt b₅₅₉ after the removal of molecular oxygen. These results indicate that conversion from the IP to the HP form of cyt b₅₅₉ proceeds via different mechanisms. Under illumination, conversion of the IP to the HP form of cyt b₅₅₉ depends primarily on the protonation of the histidine residue, whereas under anaerobic conditions, the conversion of the IP to the HP form of cyt b₅₅₉ is driven by higher hydrophobicity of the environment around the heme iron resulting from the absence of molecular oxygen.     

溴虫腈、茚虫威与氟啶脲混配对小菜蛾毒力最佳配比筛选及田间防效研究

为了延缓小菜蛾Plutella xylostella(L.)抗药性的产生和发展,本研究选用常用的3种化学杀虫剂,即氟啶脲、溴虫腈、茚虫威,采用交互测定法进行了最佳配比的筛选,并根据孙云沛法计算其共毒系数,最后筛选出具增效作用的混配配方,氟啶脲∶溴虫腈(有效成分含量为13.20∶1.72),共毒系数为241;氟啶脲∶茚虫威(有效成分含量为2.20∶3.60),共毒系数为142。田间试验结果表明氟啶脲与溴虫腈混配2000倍液药后7d校正防效为84.24%,与其他处理的校正防效具有极显著差异;氟啶脲与茚虫威混配1000倍液药后7d校正防效为85.08%,与其他处理的校正防效有显著性差异。     

A comparison of force fields for ethanol–water mixtures

Aqueous ethanol mixtures are studied through molecular dynamics simulations with the focus on exploring how various force field models reproduce the association and its influence on selected thermo-physical properties of these mixtures. The most important conclusion seems to be the inadequacy of all classical force fields to reproduce the very peculiar shape of the excess enthalpy of these mixtures, as a function of the ethanol concentration, neither quantitatively nor qualitatively. The Kirkwood–Buff (KB) integrals calculated using the simulation data follow the same trends as the experimental ones. This suggests complicated correlation of the excess enthalpy with the concentration fluctuation and clustering in these mixtures. The KB force field shows better overall agreement with experimental results than the other studied models.