Steroidal Antimetabolites Protect Mice against Trypanosoma brucei

Trypanosoma brucei, the causative agent for human African trypanosomiasis, is an emerging ergosterol-dependent parasite that produces chokepoint enzymes, sterol methyltransferases (SMT), not synthesized in their animal hosts that can regulate cell viability. Here, we report the lethal effects of two recently described natural product antimetabolites that disrupt Acanthamoeba sterol methylation and growth, cholesta-5,7,22,24-tetraenol (CHT) and ergosta-5,7,22,24(28)-tetraenol (ERGT) that can equally target T. brucei. We found that CHT/ERGT inhibited cell growth in vitro, yielding EC₅₀ values in the low nanomolar range with washout experiments showing cidal activity against the bloodstream form, consistent with their predicted mode of suicide inhibition on SMT activity and ergosterol production. Antimetabolite treatment generated altered T. brucei cell morphology and death rapidly within hours. Notably, in vivo ERGT/CHT protected mice infected with T. brucei, doubling their survival time following daily treatment for 8–10 days at 50 mg/kg or 100 mg/kg. The current study demonstrates a new class of lead antibiotics, in the form of common fungal sterols, for antitrypanosomal drug development.     

柔性有机电致发光器件导电基板的工艺性能

在聚对苯二甲酸乙二醇酯(PET)柔性衬底上采用直流磁控溅射技术制备了氧化铟锡(ITO)透明导电薄膜,研究了衬底温度、溅射功率和溅射压强等工艺条件对薄膜光电性能的影响,并利用原子力显微镜(AFM)表征了衬底及ITO薄膜的表面形貌。结果表明,在PET衬底温度50℃、溅射功率100W和溅射压强2.66×10-1Pa的条件下,可以得到低方阻(50Ω/□)和高透过率(>90%)的透明导电薄膜。以此柔性ITO衬底为阳极,制备了结构为PET/ITO/NPB/Alq3/Mg∶Ag的柔性有机电致发光器件,在驱动电压为13V时,器件的发光亮度达到了2834cd/m2。     

转移基板材质对Si衬底GaN基LED芯片性能的影响

在Si衬底上生长了GaN基LED外延材料,分别转移到新的硅基板和铜基板上,制备了垂直结构蓝光LED芯片。研究了这两种基板GaN基LED芯片的光电性能。在切割成单个芯片之前,对大量尺寸为(300μm×300μm)的这两种芯片分别通高达1 A的大电流在测试台上加速老化1 h。结果显示,铜基板Si衬底GaN基LED芯片有更大的饱和电流,光输出效率更高,工作电压随驱动电流的变化不大,光输出在老化过程中衰减更小。铜基板芯片比硅基板芯片可靠性更高,在大功率半导体照明器件中前景诱人。     

6H-SiC衬底片的表面处理

相比于蓝宝石,6H-SiC是制作GaN高功率器件更有前途的衬底.本文研究了表面处理如研磨、化学机械抛光对6H-SiC衬底表面特性的影响.用显微镜、原子力显微镜、拉曼光谱、卢瑟福背散射谱表征了衬底表面.结果表明经过两步化学机械抛光后提高了表面质量.经第二步化学机械抛光后的衬底具有优异的表面形貌、高透射率和极小的损伤层,其表面粗糙度RMS是0.12nm.在该衬底上用MOCVD方法长出了高质量的GaN外延膜.     

Intensification of Double Kinetic Resolution of Chiral Amines and Alcohols via Chemoselective Formation of a Carbonate–Enzyme Intermediate

Chiral amines and alcohols are synthons of numerous pharmaceutically-relevant compounds. The previously developed enzymatic kinetic resolution approaches utilize a chiral racemic molecule and achiral acyl donor (or acyl acceptor). Thus, only one enantiodivergent step of the catalytic cycle is engaged, which does not fully exploit the enzyme’s abilities. The first carbonate-mediated example of simultaneous double chemoselective kinetic resolution of chiral amines and alcohols is described. Herein, we established a biocatalytic approach towards four optically-pure compounds (>99% ee, Enantioselectivity: E > 200) via double enzymatic kinetic resolution, engaging chiral organic carbonates as acyl donors. High enantioselectivity was ensured by extraordinary chemoselectivity in lipase-catalyzed formation of unsymmetrical organic carbonates and engaged in a process applicable for the synthesis of enantiopure organic precursors of valuable compounds. This study focused not only on preparative synthesis, but additionally the catalytic mechanism was discussed and the clear impact of this rarely observed carbonate-derived acyl enzyme was shown. The presented protocol is characterized by atom efficiency, acyl donor sustainability, easy acyl group removal, mild reaction conditions, and biocatalyst recyclability, which significantly decreases the cost of the reported process.     

基片光学特性对薄膜光强透过谱的影响

在考虑基片与空气界面反射率以及基片吸收不能忽略的情况下，对常见的基片上薄膜的光强透过率公式进行了修正，导出了该情况下的透过率公式．以非晶硅薄膜为研究对象，采用模拟计算说明基片光学特性对薄膜光强透过谱的影响．     

第三族金属氧化物离子对二氧化碳转化的红外光谱研究

本文利用红外光解离光谱研究了第三族金属氧化物离子对二氧化碳分子的转化机制. 研究表明,对于[ScO(CO₂)_n]⁺体系,在n≤4时,形成了溶剂化结构;在n=5时,形成了碳酸盐结构,实现了二氧化碳的转化. 对于[YO(CO₂)_n]⁺体系,需要4个二氧化碳分子就可以实现二氧化碳的转化. 而在[YO(CO₂)_n]⁺体系中,只发现了溶剂化结构,没有观察到碳酸盐结构. 理论计算表明,[YO(CO₂)_n]⁺体系拥有最小的溶剂化结构向碳酸盐结构转化能垒,[LaO(CO₂)_n]⁺体系拥有最大的溶剂化结构向碳酸盐结构转化能垒. 本文从分子水平揭示了不同金属氧化物离子对二氧化碳分子转化的影响规律.     

Nanostructured Polyelectrolyte-based System as a Toolbox for Metal Ions Detection

The capability of certain heavy metal ions to induce fluorescence decrease by a quenching mechanism suggested us to design and build a sensor potentially tunable for different ions at different concentrations. We propose a quenching-based sensor exploiting a nanostructured architecture in which fluorescent molecules (the sensing probe) are entrapped to recognize a specific analyte (heavy metal ions) through an optical transduction. The polyelectrolyte nanostructured system, named nanocapsule, improves the fluorophore-ion quenching sensitivity allowing a micromolar detection. Furthermore we couple our sensor with an electrical device in order to refine the sensing procedure: the electric field created allows a metal ions spatial gradient, necessary to detect a specific element on a single sample solution, avoiding a comparative analysis with an intensity reference value. Results obtained will show the advantages and the potentialities of our system as a smart toolbox for metal ions detection.     

193 nm氟化物增透膜的特性

 为了研制低损耗、高性能的193 nm氟化物增透膜,研究了基底和不同氟化物材料组合对氟化物增透膜的影响。在熔石英基底上,将挡板法和预镀层技术相结合,采用热舟蒸发方式制备了不同氟化物材料组合增透膜,对增透膜的剩余反射率和光学损耗等光学特性,以及表面粗糙度和应力等特性进行了测量和比较。在分析比较和优化的基础上,设计制备的3层1/4波长规整膜系AlF3/LaF3增透膜在193 nm的剩余反射率低于0.14%,单面镀膜增透膜的透射率为93.85%,增透膜表面均方根粗糙度为0.979 nm,总的损耗约为6％。要得到高性能的193 nm增透膜,应选用超级抛光基底。