Synthesis and Anti‐HIV Activity of Triazolo‐Fused,Medium‐Sized Cyclic Nucleoside Analogs Prepared by an Intramolecular Huisgen 1,3‐Dipolar Cycloaddition

Medium‐sized cyclic nucleosides containing a fused triazole ring were synthesized via intramolecular Huisgen 1,3‐dipolar cycloadditon reaction. 2′,3′‐seco‐Uridine was employed as the key intermediate for the introduction of azido and alkynyl moieties in the defined positions of the reaction precursors. The cycloaddition reactions were achieved in high yields by heating the precursor in refluxing toluene. The uracil base in these target compounds was successfully transformed to the corresponding cytosine. The synthesized compounds were evaluated in a MAGI assay for their anti‐HIV activities, and in a H9 T lymphocytes assay for their cell toxicities.     

Electrochemical detection of ultratrace nitroaromatic explosives using ordered mesoporous carbon

A sensitive electrochemical sensor has been fabricated to detect ultratrace nitroaromatic explosives using ordered mesoporus carbon (OMC). OMC was synthesized and characterized by scanning electron microscopy, transmission electron microscopy and nitrogen adsorption/desorption measurements. Glassy carbon electrodes functionalized with OMC show high sensitivity of 62.7 μA cm⁻² per ppb towards 2,4,6-trinitrotoluene (TNT). By comparison with other materials such as carbon nanotubes and ordered mesoporous silica, it is found that the high performance of OMC toward sensing TNT is attributed to its large specific surface area and fast electron transfer capability. As low as 0.2 ppb TNT, 1 ppb 2,4-dinitrotoluene and 1 ppb 1,3-dinitrobenzene can be detected on OMC based electrodes. This work renders new opportunities to detect ultratrace explosives for applications of environment protections and home securities against chemical warfare agents.     

Impact of sugar stereochemistry on natural killer T cell stimulation by bacterial glycolipids

Natural killer T (NKT) cells recognize glycolipids produced by Sphingomonas bacteria, and these glycolipids contain C6-oxidized sugars, either glucuronic acid or galacturonic acid, linked to ceramides. Glycolipids with gluco stereochemistry are the most prevalent. Multiple studies have demonstrated that galactosylceramides are more potent stimulators of NKT cells than their glucose isomers. To determine if this stereoselectivity is retained in the context of the C6-oxidized sugars found in bacterial glycolipids, we prepared two sets of gluco and galacto-glycolipids oxidized at their C6 positions and compared their NKT stimulatory properties. In the context of carboxylic acid groups at C6, gluco stereochemistry gave the more potent responses. We also prepared bacterial glycolipids containing more complex ceramide groups to determine if these chains impact NKT cell responses.     

Pharmacokinetic Study of ZS-1, a Targeted Peptide to NCI-H1299, in Rats Following Intravenous Administration

To investigate the pharmacokinetics of ZS-1 following intravenous injection in rats, ZS-1 was administered at doses of 20, 30 and 45 mg kg^?1, respectively. Blood samples were collected at 0.5, 3, 8, 12, 15, 20, 30, 40 and 45 min. ZS-1 in rat plasma was measured by LC. The limit of detection (LOD) was 0.02 μg mL^?1. The relative standard deviation (RSD) of intra- and inter-day precisions were <10%, and the accuracy of intra- and inter-day were >94%. The mean extraction recovery of ZS-1 was 86.1%. After intravenous injection at doses of 20, 30 and 45 mg kg^?1, the concentration–time curves of ZS-1 fitted well to one compartment model. Area under the concentration–time curves (AUC) increased with dose. Clearance rates (CL) and elimination half-lives (T _1/2) had no significant difference between different dose groups (P > 0.05). ZS-1 was stable in plasma after at 25 °C for 2, 4, 6 h, after three freeze–thaw cycles, after ?20 °C for a month, and after ?80 °C for 3 months. The accuracy of ZS-1 was between 96.8 and 106.9%. The results indicated there was no significant degradation. These data indicated that the method for analysis of ZS-1 was reliable and the pharmacokinetic data could guide dosing regimens to be tested in future clinical pharmacokinetic study.     

Organic dye bearing asymmetric double donor-π-acceptor chains for dye-sensitized solar cells

A novel efficient metal free sensitizer containing asymmetric double donor-π-acceptor chains (DC) was synthesized for dye-sensitized solar cells (DSSCs). Comparing to 3.80%, 4.40% and 4.64% for the DSSCs based on the dyes with single chain (SC1, SC2) and cosensitizers (SC1 + SC2), the overall conversion efficiency reaches 6.06% for DC-sensitized solar cells as a result of its longer electron lifetime and higher incident monochromatic photon-to-current conversion efficiency.     

Precursor-directed fungal generation of novel halogenated chaetoglobosins with more preferable immunosuppressive action

Precursor-fed cultivation of endophytic Chaetomium globosum 1C51 afforded nine novel "unnatural" halogenated chaetoglobosins including those with more preferable immunosuppressive activity.     

离子束辅助沉积对类金刚石膜结构影响的计算机模拟

采用分子动力学(MD)模拟研究了离子束辅助沉积(1BAD)生长类金刚石(DLC)膜的物理过程.分 别选C₂分子和Ar离子作为沉积源和辅助沉积粒子.改变Ar的入射能量和到达比(A r／C)，研 究了它对DLC膜结构的影响.重点讨论了Ar辅助沉积引起表面原子的瞬间活性变化对薄膜结构 产生的影响.分析表明，由于Ar离子的轰击引起的能量和动量的传递，大大地增强了C原子在 表面的反冲动能及迁移概率，增加了合成薄膜的SP³键含量.研究结果和实验 观察一致，并从合成机理上给出了一些定量解释. 关键词： 类金刚石膜 离子束辅助沉积 分子动力学模拟     

Broadband optical limiting performance of polymer-wrapped carbon nanotubes in the orange-NIR region

Soluble multi-walled carbon nanotubes (MWNTs) have been obtained by noncovalent modification with poly [2-methoxy,5-(2′-ethyl-hexyloxy)-p-phenylene vinylene] (MEH-PPV). For the composite MWNT/MEH-PPV, there is π-π interaction between the MEH-PPV and MWNTs in addition to the wrapping of the polymer. The nonlinear optical transmittance was measured using a nanosecond optical parametric oscillator pumped with a Nd:YAG system. Excellent optical limiting performance of the composite MWNT/MEH-PPV was observed both in the visible region of 590-680 nm and at the wavelength of 1064 nm. By means of time-correlated single-photon counting fluorescence measurement, an explanation based on the nonlinear absorption of MWNT dominated by the intermolecular energy transfer was proposed.     

催化极谱法测定L-谷氨酸的应用与研究

本文提出了催化极谱法测定L-谷氨酸的新体系并建立了相应的分析方法,对体系的反应机理也进行了初步研究。实验结果表明:当体系pH为8～10,[Cu~(2 )]=5×10~(-4)M,硼砂浓度为0.04M时,L-谷氨酸于-1.10V处产生一个清晰、灵敏的催化波。当其浓度为10~(-5)～10~(-6)M时,与峰高成良好的线性关系。机理实验结果证明,此波为吸附催化氢波。