In Vitro and In Vivo Antibacterial Activity,Toxicity and Resistance Analysis of Pleuromutilin Derivative Z33 against Methicillin-Resistant Staphylococcus aureus

The novel pleuromutilin derivative, which showed excellent in vitro antibacterial activity against MRSA, 22-(2-(2-(4-((4-(4-nitrophenyl)piperazin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)acetamido)phenyl)thioacety-l-yl-22-deoxypleuromutilin (Z33), was synthesized and characterized in our previous work. In this study, the preliminary pharmacodynamics and safety of Z33 were further evaluated. In in vitro antibacterial activity assays, Z33 was found to be a potent bactericidal antibiotic against MRSA that induced dose-dependent growth inhibition and long-term post-antibiotic effect (PAE). The drug-resistance test demonstrated that Z33 possessed a narrow mutant selection window and lower propensities to select resistance than that of tiamulin. Cytochrome P450 (CYP450) inhibition assay determined that the inhibitory effect of Z33 was similar to that of tiamulin against the activity of CYP3A4, and was lower than that of tiamulin on the activity of CYP2E1. Toxicity determination showed that both Z33 and tiamulin displayed low cytotoxicity of RAW264.7 cells. Furthermore, Z33 was found to be a high-security compound with a 50% lethal dose (LD₅₀) above 5000 mg/kg in the acute oral toxicity test in mice. In an in vivo antibacterial activity test, Z33 displayed better therapeutic effectiveness than tiamulin in the neutropenic mouse thigh infection model. In summary, Z33 was worthy of further development as a highly effective and safe antibiotic agent against MRSA infection.     

An Exploration of the Effect of the Kleier Model and Carrier-Mediated Theory to Design Phloem-Mobile Pesticides Based on Researching the N-Alkylated Derivatives of Phenazine-1-Carboxylic Acid-Glycine

The Kleier model and Carrier-mediated theory are effective for molecularly designing pesticides with phloem mobility. However, the single Kleier model or Carrier-mediated theory cannot achieve a reliable explanation of the phloem mobility of all exogenous substances. A detailed investigation of the two models and the scope of their applications can provide a more accurate and highly efficient basis for the guidance of the design and development of phloem-mobile pesticides. In the present paper, a strategy using active ingredient-amino acid conjugates as mode compounds is developed based on Carrier-mediated theory. An N-alkylated amino acid is used to improve the pesticide’s physicochemical properties following the Kleier model, thus allowing the conjugates to fall on the predicted and more accessible transportation region of phloem. Moreover, the influence of this movement on phloem is inspected by the Kleier model and Carrier-mediated theory. To verify this strategy, a series of N-alkylated phenazine-1-carboxylic acid-glycine compounds (PCA-Gly) were designed and synthesized. The results related to the castor bean seeds (R. communis L.) indicated that all the target compounds (4a–4f) had phloem mobility. The capacity for phloem mobility shows that N-alkylated glycine containing small substituents can significantly improve PCA phloem mobility, such as 4c(i-C₃H₇-N) > 4a(CH₃-N) ≈ 4b(C₂H₅-N) > 4d (t-C₄H₉-N) > PCA-Gly > 4e(C₆H₅-N) > 4f(CH₂COOH-N), with an oil–water partition coefficient between 1.2~2.5. In particular, compounds 4a(CH₃-N), 4b(C₂H₅-N), and 4c(i-C₃H₇-N) present better phloem mobility, with the average concentrations in phloem sap of 14.62 μΜ, 13.98 μΜ, and 17.63 μΜ in the first 5 h, which are 8 to 10 times higher than PCA-Gly (1.71 μΜ). The results reveal that the Kleier model and Carrier-mediated theory play a guiding role in the design of phloem-mobile pesticides. However, the single Kleier model or Carrier-mediated theory are not entirely accurate. Still, there is a synergism between Carrier-mediated theory and the Kleier model for promoting the phloem transport of exogenous compounds. Therefore, we suggest the introduction of endogenous plant compounds as a promoiety to improve the phloem mobility of pesticides through Carrier-mediated theory. It is necessary to consider the improvement of physicochemical properties according to the Kleier model, which can contribute to a scientific theory for developing phloem-mobile pesticides.     

Fe掺杂α-Bi2O3光电性质的第一性原理研究

采用第一性原理杂化泛函HSE06方法对Fe掺杂α-Bi2 O3的电子结构和光学性质进行了计算研究.结果表明,Fe掺杂α-Bi2 O3体系有较小的结构变形,本征α-Bi2 O3的禁带宽度为2.69 eV,Fe掺杂使α-Bi2 O3的禁带宽度减小(约为2.34 eV).对其光学性质研究得出Fe掺杂扩展了α-Bi2 O3对可...     

Evaluation of Water Ammonium Ion Test Kit and Its Feasibility for the Analysis of Protein in Food

The traditional method for the determination of protein in food needs the operations of digestion, distillation, absorption, and titration; therefore, it is complicated and time-consuming and requires professional personnel. Is there a more convenient and faster detection method that can directly determine the ammonium ions in protein digestion solution to obtain the protein content of food and avoid the distillation–absorption–titration process? The feasibility of water ammonium ion test kits for food protein rapid detection was discussed here. After digestion, the protein in food transforms into ammonium ions in the digestion solution. Because of the variety of food, there are many different inorganic ions left in the food digestion solution, and at the same time, digestion agents are added in the digestion process and become potential interference factors in ammonium determination. Therefore, the detection accuracy of ammonium test kits needs to be evaluated first, including their anti-interference ability. The standard curve of ammonium was established by the test kit. When the ammonium concentration was 0.00–2.50 mg/L, the absorbance at 620 nm was linearly related to the ammonium concentration, the determination coefficient R² was 0.9995, and the detection limit of this method was 0.01 mg/L. The influences of temperature, pH value, and reaction time on the test kit method were discussed. The precision was 0.90–3.33%; the repeatability was 1.71–4.86%; and the recovery rate of tap water, river water, and sea water was controlled within 90–103%. The anti-interference ability of the evaluated test kit was better than that of the national standard detection method. The test kit, combined with sample pretreatment and protein conversion formula, was used to detect protein in different types of food (milk powder, rice flour, wheat flour, soy, banana, milk, fish food, chicken food, and dog food). The results showed that there were no significant differences (ρ > 0.05) between the national method and the test kit method. The ammonium ion test kit method shortened the determination time and had higher sensitivity, showing its potential for the rapid determination of food protein.     

具有调制分布复合中心的非晶半导体超晶格中载流子的弛豫过程

本文提出一种具有调制分布的复合中心的连续时间无规行走(以下称CTRW)模型,用以求解非晶半导体超晶格中载流子被复合的动力学过程。对不同类型的时间分布函数,我们得到了载流子的存活几率,从中可以分析周期型势阱和调制型掺杂等因素对这种材料的宏观输运性质的影响。 关键词：     

多聚螯合物酶联抗体交联磁性纳米乳胶的脂联素免疫透射比浊方法研究

采用多聚螯合物酶联抗体交联磁性纳米乳胶的脂联素免疫透射比浊法检测了血清中脂联素. 发现多聚螯合物酶上含有大量HRP酶, 可以极大地放大检测信号; 在优化条件下, 免疫比浊信号强度在脂联素0.005~0.2ng?mL-1范围内变化时, 并随着ADPN浓度的增加呈线性关系(R2=0.998), 检出限为2 pg?mL-1. 该方法能成功用于血清样本中脂联素的检测.     

演化参数反演方法

给出了一类基于演化计算的演化参数反演方法,此类方法既可以给定参数的函数类,用遗传算法（Genetic Algorithms）来反演参数的最优估计值,也可以不指定函数类形式,用遗传程序设计（Genetic Programming）的方法反演出最优的函数模型,使参数反演实现客观化、自动化.由此建立反演系统后,在使用过程中可以根据最新获得的数据对模型中的物理参数作适时校准,一旦发现预报误差较大,就利用演化算法及时修正方程中的参数以改进预报.运用该方法于椭圆边值问题的物理参数反演的数值模拟,证实了此方法的有效性,为物理模型参数的反演提供了一种崭新的实用方法.     

Can contributions to B_s→l＋l-γ from the magnetic-penguin operator with real photons in the standard model be neglected？

Using the Bs meson wave function extracted from non-leptonic Bs decays, we reevaluate the rare decays Bs→l＋l- γ,（l=e,μ） in the Standard Model, including two kinds of contributions from the magnetic-penguin operator with virtual and real photons. We find that contributions to the exclusive decays from the magnetic-penguin operator b→sγ with real photons, which were regarded as negligible in the previous literature, are large and the branching ratios Bs→l＋l-γ are enhanced by a factor of almost 2. With the predicted branching ratios of the order of 10-8, it is expected that these radiative dileptonic decays will be detected in LHC-b and B factories in the near future.     

煤粉燃烧过程碳烟生成的激光测量研究

燃煤锅炉生成的碳烟不仅会增强火焰辐射、影响燃烧外,还排放到大气环境中带来严重危害。为了进一步了解其生成机理从而更好地对其生成量及特性进行控制,对煤粉燃烧过程中颗粒周围碳烟的分布规律进行定量的研究十分必要。本文自行设计了注射式微量给粉装置,成功实现了0.1 g/h量级给粉率下的连续给粉,并通过改进多元扩散燃烧器和以及结合激光诱导白炽光(Laser Induced Incandescence)技术,首次实现了对单颗粒煤粉燃烧过程中碳烟分布的定量测量,发现对于70μm左右的煤粉颗粒,碳烟分布直径约为1 mm。此外还通过控制气氛,研究了含氧量对碳烟生成的影响,发现随着氧含量的上升,碳烟总浓度下降并且峰值出现更早的规律。     

基于光谱特征的北京城区植被滞尘分布反演

植被叶片的滞尘量可以表征空气污染的程度, 分析城市植被滞尘的空间特征对于制定更为有效的空气污染控制政策具有重要的现实意义。基于北京市主城区采集的大叶黄杨、国槐、毛白杨和山桃等四种典型绿化植被叶片的滞尘量、光谱反射率和叶面积等数据,比较四种植被叶片滞尘前后的光谱曲线,进行窄波段与卫星波段滞尘前后叶片光谱反射率比值与滞尘量的相关分析。然后,分别建立相关性最大的卫星波段反射率和NDVI与滞尘量之间的回归模型, 选取拟合较好的模型反演北京城区植被的滞尘量分布,进而插值得到整个北京城区的尘埃分布。最后,根据高滞尘区域周围的土地覆盖和土地利用以及滞尘期间PM₁₀浓度的空间分布对反演的的合理性进行检验。结果表明：在780~1 300 nm波段,大叶黄杨、国槐、毛白杨和山桃四种植被的滞尘叶片反射率均明显低于干净叶片;窄波段反射率与滞尘量在520~650 nm波段和1 390~1 600 nm波段具有较高的相关性,相关系数的绝对值最高达到0.626;利用Landsat8的green波段和NDVI构建的滞尘反演模型,决定系数(R2)分别为0.446和0.465。NDVI模型反演的北京城区植被的滞尘量分布结果表明,北京城区滞尘含量呈现出北高南低,东高西低,中心城区高于郊区的空间分布格局。该研究通过高光谱和遥感影像数据反演滞尘量,可以为快速全面监测城市地区尘埃分布提供参考。