Anti HIV-1 agents 5: Synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro

In continuation of our program aimed at the discovery and development of compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 21N-arylsulfonyl-3-acetylindole analogs (2a-u) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among of all the analogs, several compounds exhibited significant anti-HIV-1 activity, especially N-phenylsulfonyl-3-acetyl-6-methylindole (2j) and N-(p-ethyl)phenylsulfonyl-3-acetyl-6-methylindole (2n) showed the most potent anti-HIV-1 activity with EC50 values of 0.36 and 0.13 mu g/mL, and TI values of >555.55 and 791.85, respectively. It demonstrated that introduction of the acetyl group at the 3-position of N-arylsulfonyl-6-methylindoles could generally lead to the more potent analogs. (C) 2010 Elsevier Ltd. All rights reserved.

大珠母贝精子介导外源基因转移研究

将大珠母贝(PinctadamaximaJameson)精子与“全鱼”GH基因重组体pCAgcGH和pCAgcGHc的线性DNA混合,温育30min,经6次、27、10kV脉冲电处理后,与卵子受精,得到若干贝苗。从贝苗中提取DNA,经PCR扩增和Southernblot分子杂交表明,部分受体带有外源基因,当与精子温育的外源基因浓度分别为2μg/mL,6μg/mL及18μg/mL时,相应贝苗携带外源基因比率分别为56%,20%和50%。即在此范围内,基因转移的阳性率与外源基因的浓度呈正相关。

在高低温工作条件下对光电器件进行测试的装置和方法

本发明公开了一种在高低温工作条件下对光电器件进行测试的装置，该装置包括:一导温密封腔，用于容置待检测光电器件，具有一光窗口，用于被检测光电器件的光输出或光输入;一支架，该导温密封腔固定于该支架的顶端;一托架，设置于该支架的下端，可沿支架上下移动;一加热或冷却设备，固定于该托架上，随托架一起沿支架上下移动，用于对导温密封腔进行加热或冷却，实现高低温工作条件。本发明提供的在高低温工作条件下对光电器件进行测试的装置和方法，解决了在高低温工作条件下窄脉宽光发射器件和微光光电探测器件参数测试的短线电连接问题，既保证了规定高低温工作环境温度的准确和稳定，又解决了短连线信号输入输出要求、结霜短路和结霜挡光等问题，且结构简单，造价低廉，具有很高的应用价值。

Preparation of polymer/silica nanoscale hybrids through sol-gel method involving emulsion polymers. II. Poly(ethyl acrylate)/SiO2

Poly(ethyl acrylate) (PEA)/SiO2 hybrids with different compositions were prepared under different casting temperatures and pH values. Their morphology as investigated by transmission electron microscopy (TEM) shows that samples with different compositions have different morphologies. When the SiO2 content is lower, PEA is the continuous phase and SiO2 is the dispersed phase. At higher SiO2 content, the change in phase morphology takes place, nd PEA gradually dispersing in the form of latex particles in SiO2 matrix. Change in phase morphology depends mainly on the time the sol-gel transition occurs. At suitable casting temperature and pH value, PEA/SiO2 in 95/5 and 50/50 hybrids with even dispersion was obtained.

两种催化裂化催化剂载体的矿物学特性研究－高岭土和酸活化水黑云母

通过对贵州大方高岭土（GZK-1）、苏州高岭土（JSK）、新疆伊宁高岭土（XJK-6）和新疆尉犁水黑云母及其酸活化处理样矿物学特征的系统研究，得出如下讨论：（1）GZK-1、JSK、和XJK-6的微活指数依次为 29%, 13%和0%，在微活指数上埃洛石＞高岭石＞地开石；（2）高岭土的微活指数仅与杂质铁(Fe_2O_3+FeO)的含量有一定的正相关关系；（3）高岭土的微活指数与其孔体积和比表面积有正相关关系；（4）高岭土的微活指数主要与矿物成分有关，其结构羟基的特性是活性的根源；（5）XJK-6的比表面积小(9 m~2/g)、孔体积小(0.026 ml/g)、大孔多、热稳定性好、几乎无活性；（6）在一定的实验条件下，可获得即具大的比表面积、孔径和孔体积，又尽可能保持原有晶体结构的酸活化产物；（7）活化样品中K_2O、Fe_2O_3、MgO的含量可指示其比表面积的变化；（8）水黑云母含金云母晶层的矿物晶体结构决定了其比蛭石晶层耐酸腐蚀，在较为苛刻的条件下金云母晶层仍然保持；（9）酸活化产物的特点：结构中含一定量的镁；Na_2O含量低，K_2O的含量高；比表面积大(130 m~2/g)；孔体积高(0.119 ml/g)，中孔多；微活指数低 (4.7%).

Two Arginine-Glutamate Ionic Locks Near the Extracellular Surface of FFAR1 Gate Receptor Activation

Activation of a number of class A G protein-coupled receptors (GPCRs) is thought to involve two molecular switches, a rotamer toggle switch within the transmembrane domain and an ionic lock at the cytoplasmic surface of the receptor; however, the mechanism by which agonist binding changes these molecular interactions is not understood. Importantly, 80% of GPCRs including free fatty acid receptor 1 (FFAR1) lack the complement of amino acid residues implicated in either or both of these two switches; the mechanism of activation of these GPCRs is therefore less clear. By homology modeling, we identified two Glu residues (Glu-145 and Glu-172) in the second extracellular loop of FFAR1 that form putative interactions individually with two transmembrane Arg residues (Arg-183(5.39) and Arg-258(7.35)) to create two ionic locks. Molecular dynamics simulations showed that binding of agonists to FFAR1 leads to breakage of these Glu-Arg interactions. In mutagenesis experiments, breakage of these two putative interactions by substituting Ala for Glu-145 and Glu-172 caused constitutive receptor activation. Our results therefore reveal a molecular switch for receptor activation present on the extracellular surface of FFAR1 that is broken by agonist binding. Similar ionic locks between the transmembrane domains and the extracellular loops may constitute a mechanism common to other class A GPCRs also.

The Absolute Configuration for Inthomycin C: Revision of Previously Published Work with a Reinstatement of the (3R)-Configuration for (-)-Inthomycin C

Abstract Image

Stereochemical evidence is presented to demonstrate that (−)-inthomycin C has (3R)- and not (3S)-stereochemistry. Careful reappraisal of the previously published work2−5 now indicates that the Hatakeyama, Hale, Ryu, and Taylor teams all have synthesized (−)-(3R)-inthomycin C. The newly measured [α]D of pure (−)-(3R)-inthomycin C (98% ee) is −7.9 (c 0.33, CHCl3) and not −41.5 (c 0.1, CHCl3) as was previously reported in 2012.

Spitzer infrared spectrograph point source classification in the Small Magellanic Cloud

The Magellanic Clouds are uniquely placed to study the stellar contribution to dust emission. Individual stars can be resolved in these systems even in the mid-infrared, and they are close enough to allow detection of infrared excess caused by dust. We have searched the Spitzer Space Telescope data archive for all Infrared Spectrograph (IRS) staring-mode observations of the Small Magellanic Cloud (SMC) and found that 209 Infrared Array Camera (IRAC) point sources within the footprint of the Surveying the Agents of Galaxy Evolution in the Small Magellanic Cloud (SAGE-SMC) Spitzer Legacy programme were targeted, within a total of 311 staring-mode observations. We classify these point sources using a decision tree method of object classification, based on infrared spectral features, continuum and spectral energy distribution shape, bolometric luminosity, cluster membership and variability information. We find 58 asymptotic giant branch (AGB) stars, 51 young stellar objects, 4 post-AGB objects, 22 red supergiants, 27 stars (of which 23 are dusty OB stars), 24 planetary nebulae (PNe), 10 Wolf-Rayet stars, 3 H II regions, 3 R Coronae Borealis stars, 1 Blue Supergiant and 6 other objects, including 2 foreground AGB stars. We use these classifications to evaluate the success of photometric classification methods reported in the literature.

Trilhos do Algarve: roteiro de bolso

Dissertação de mest., Produção, Edição e Comunicação de Conteúdos (Comunicação Multimédia), Faculdade de Ciências Humanas e Sociais, Univ. do Algarve, 2012

L'Écho de Paris

1894/01/30 (Numéro 3536).