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.     

纳米氧化镱对熔融石英析晶动力学机制的影响

本文研究引入纳米氧化镱对熔融石英析晶机制及动力学过程的影响.通过X射线衍射仪(XRD)测试结果分析了纳米氧化镱的引入对熔融石英陶瓷析晶率的影响,采用动力学方法分析了纳米氧化镱的引入对熔融石英陶瓷析晶机制的影响,同时探讨了其等温析晶动力学过程.研究表明,熔融石英陶瓷的晶粒向二维兼有一维及三维的方式生长,引入纳米氧化镱的熔...     

Green Tea (Camellia sinensis): A Review of Its Phytochemistry,Pharmacology, and Toxicology

Objectives Green tea (Camellia sinensis) is a kind of unfermented tea that retains the natural substance in fresh leaves to a great extent. It is regarded as the second most popular drink in the world besides water. In this paper, the phytochemistry, pharmacology, and toxicology of green tea are reviewed systematically and comprehensively. Key findings Green tea has been demonstrated to be good for human health. Nowadays, multiple pharmacologically active components have been isolated and identified from green tea, including tea polyphenols, alkaloids, amino acids, polysaccharides, and volatile components. Recent studies have demonstrated that green tea shows versatile pharmacological activities, such as antioxidant, anticancer, hypoglycemic, antibacterial, antiviral, and neuroprotective. Studies on the toxic effects of green tea extract and its main ingredients have also raised concerns including hepatotoxicity and DNA damage. Summary Green tea can be used to assist the treatment of diabetes, Alzheimer’s disease, oral cancer, and dermatitis. Consequently, green tea has shown promising practical prospects in health care and disease prevention.     

Benzothiadiazole-based Conjugated Polymers for Organic Solar Cells

Benzothiadiazole(BT) is an electron-deficient unit with fused aromatic core, which can be used to construct conjugated polymers for application in organic solar cells(OSCs). In the past twenty years, huge numbers of conjugated polymers based on BT unit have been developed,focusing on the backbone engineering(such as by using different copolymerized building blocks), side chain engineering(such as by using linear or branch side units), using heteroatoms(such as F, O and S atoms, and CN group), etc. These modifications enable BT-polymers to exhibit distinct absorption spectra(with onset varied from 600 nm to 1000 nm), different frontier energy levels and crystallinities. As a consequence, BT-polymers have gained much attention in recent years, and can be simultaneously used as electron donor and electron acceptor in OSCs, providing the power conversion efficiencies(PCEs) over 18% and 14% in non-fullerene and all-polymer OSCs. In this article, we provide an overview of BTpolymers for OSCs, from donor to acceptor, via selecting some typical BT-polymers in different periods. We hope that the summary in this article can invoke the interest to study the BT-polymers toward high performance OSCs, especially with thick active layers that can be potentially used in large-area devices.     

Rapid Detection of Five Estrogens Added Illegally to Dietary Supplements by Combining TLC with Raman Imaging Microscope

Estrogens added illegally to dietary supplements are hazardous to human health. Traditional detection and analysis methods have many limitations, and we have developed an assay that combines thin-layer chromatography with Raman imaging microscopy (TLC-RIM). The five estrogens (estrone, estradiol, estriol, ethinyl estradiol, and diethylstilbestrol) were initially separated by TLC, then detected by area scanning Raman imaging with a 532 nm laser under a microscope. Raman spectra were obtained for each estrogen, which were used for detecting estrogen illegally added to botanical dietary supplements. The LOD of each estrogen was 0.4, 1.0, 0.8, 0.2, and 0.2 mg/mL, respectively. The matrix in the real sample did not interfere with the detection of estrogens. The method was fast, sensitive, stable, specific, and reliable.     

深圳城市气溶胶物理光学特性的观测研究

气溶腔是影响气候变化和空气污染的重要因子,在深圳地区展开气溶胶观测实验,可以获得可靠的光学物理特征,进而有助于准确评估气溶胶在新型超极城市区域的气像和环境效应,本文利用2010年12月至2011年8月太阳光度计、黑碳和浊度计等气溶胶观测资料,分析了新型超级城市深圳地区的气溶胶物理光学特性,深圳地区气溶胶呈明显季节变化,冬、春季由于城市污染性气溶胶的影响,气溶胶光学厚度和Angstrom波长指数都较大,夏季受海盐气溶胶的影响,光学厚度较小Angstrom波长指数也较小,光学厚度与Angstrom波长指数对比表明城市综合性污染是引起深圳气溶胶高光学厚度的主要原因,深圳地区气溶胶的散射系数、吸收系数的平均值(标准偏差)分别为178.7×10-6 m-1 (126.6×10-6m-1和32.5×1O-6m 1 (18.1×10-6m1),均低于珠三角腹地多年观测平均值的二分之一和国内其他大型城市观测值,而单次散射反照率为0.81,与珠三角其他地区得到的结果接近.此外,气溶胶吸收、散射和单次散射反照率呈明显日变化,可能主要受大气边界层变化的影响.     

异戊醇萃取-原子荧光光谱法间接测定中草药中铜含量

提出了一种原子荧光光谱法间接测定中草药中铜含量的方法。在弱酸性介质中,CuI与HgI42-反应生成稳定的Cu2HgI4,经异戊醇萃取分离后,通过用原子荧光光谱法测定有机相中剩余的汞量,间接换算成铜含量。铜的质量浓度在0.01～0.1mg.L-1范围内与荧光强度呈线性关系,方法的检出限(3S/N)为3.5μg.L-1。方法用于国家标准物质黄芪(GSB-19)、茶叶(GSB-7)和柑橘叶(GSB-11)的分析,测定值与认定值相符,测定值的相对标准偏差(n=9)在0.8%～2.4%之间。     

Annihilation of persistent slip bands and its effect on the fatigue life of copper single crystals

In single-slip-oriented copper single crystals, which were cyclically deformed under constant plastic shear strain amplitude control, a persistent slip band (PSB) was initiated on the persistent slip line (PSL) that first formed in the matrix vein dislocation structure. During intermediate temperature recovery (ITR) treatment in vacuum at 245 to 400°C, the variations in dislocation configurations and other defects of fatigued specimens were studied by using the scanning electron microscopy (SEM) electron channelling contrast (ECC) and the positron annihilation life (PAL) techniques. The results show that the ladders in the PSBs became curved and broken, or escaped locally until the PSBs disappeared completely during ITR treatment. The annihilation of the PSBs and other dislocation structures in the fatigued specimens prolonged the fatigue life to a certain extent.     

Optical bistability based on surface plasmon coupled between two noble metal films involving Kerr materials

We successfully investigate an optical bistability phenomenon in a layered structure consisting of Kretschmann configuration involving the Kerr-type nonlinear and the silver film. Pure theoretical approaches are employed to investigate that the surface plasmon could easily be coupled and both the reflection and transmission curves versus the incident intensity forms optical bistability. The transmission curves are greatly influenced by the thickness of the second silver film. These results may be useful for designing novel surface plasmon-based optical devices and will be essential for future classical and quantum information processes.     

Facile synthesis of sulfenyl-substituted isocoumarins,heterocycle-fused pyrones and 3-(inden-1-ylidene)isobenzofuranones by FeCl3-promoted regioselective annulation of o-(1-alkynyl)benzoates and o-(1-alkynyl)heterocyclic carboxylates with disulfides

Reported herein is the FeCl₃-promoted intermolecular sulfoesterification of o-(1-alkynyl)benzoates with disulfides, which provides a convenient and efficient method for synthesis of 4-sulfenylisocoumarins. Various functional groups such as methoxy, halides, ester, cyano and silicon groups in the substrates are tolerated, and heterocycle-fused chalcogenylpyrones are also successfully achieved directly from the corresponding heterocyclic precursors under the same reaction conditions. In addition, starting from diynylbenzoate, this reaction sequence can be combined with a bicyclization step leading to the tetracyclic (E)-3-(2-phenyl-3-phenylchalcogenylinden-1-ylidene)isobenzofuranone frameworks with high regiospecificity and exclusive trans stereoselectivity.