液晶冠醚、碳纳米管、水溶性杯芳烃在分析化学中的应用

综述了液晶冠醚、碳纳米管、水溶性杯芳烃在分析化学中应用的新进展。介绍了液晶冠醚在离子传输、分子识别、色谱分析、LB膜等各方面的应用;讨论了碳纳米管在扫描显微镜探针针尖、气体传感器、化学修饰电极和化学分离与检测方面的应用,以及水溶性杯芳烃在光度法、电化学、色谱分离方面的应用。     

植物绿原酸的研究进展

介绍了绿原酸的性质、作用、提取、应用,揭示了绿原酸具有潜在的、广阔的应用前景。     

稀土硫化物的研究进展

稀土硫化物是一类结构复杂、性能丰富、应用广泛的功能材料,在无机颜料、热电材料、光学材料及磁性材料等领域有着独特的优势和广阔的应用前景,是近些年来国际上的研究热点之一.本文总结了稀土硫化物的制备方法及其应用研究进展,对稀土硫化物制备的一些常见方法进行了总结和评述,对稀土硫化物的应用研究进行了总结,重点介绍了γ-稀土倍半硫化物的结构、性能特点以及相应的应用,尤其是它在环保颜料、高温热电材料以及纳米材料等领域中应用;此外,本文对稀土硫化物研究中还存在的一些问题进行了评述,并对未来的相关研究进行了展望.     

漫反射傅里叶变换红外光谱技术在定量分析中的应用

综述了漫反射傅里叶变换红外光谱(中红外)技术在定量分析中的应用,包括在药品、食品、环境样品及其它领域的应用情况,重点阐述了该技术的优缺点及其与化学计量学结合的应用情况,并对其应用前景进行了展望(引用文献52篇)。     

有序介孔材料在生物医药领域中的应用

本文简述了有序介孔材料的特性,详细介绍了其在生物医药领域中的应用研究,如用于酶的固定化、生物传感器、药物的包埋和控释、生物活性材料、生物分子的吸附和分离等,阐述了不同类型的有序介孔材料在这些应用中的性能以及为适用于该领域应用进行的材料开发和结构修饰,最后对材料的改进和应用前景进行了展望。     

灌注色谱法的发展和应用

介绍了灌注色谱法的发展、应用及其相关技术,并对灌注色谱法的特征、理论和应用作了评述。     

离子液体在生物柴油合成中的应用进展

介绍了合成生物柴油常用的酯交换方法以及离子液体的定义、结构、性质和制备方法, 简单描述了酸性离子液体作为催化剂在酯化反应中的应用, 综述了离子液体在生物柴油合成中的应用进展并展望了其应用前景.     

Gaussian 03 软件在染整课程中的应用

讨论了Gaussian 03 在染整课程中的具体应用,尤其对结构的稳定性、振动频率、染料颜色和结构的关系、分子的电荷布局在化学反应中的应用进行具体介绍。这些应用极大的丰富了课堂教学内容,提高教学质量。     

核壳结构纳米复合材料的制备及应用

核壳结构纳米复合材料由于独特的物理、化学特性和广泛的应用前景,近年来成为研究的热点.本文系统地综述了核壳结构纳米复合材料的类型,针对应用方向总结了核壳结构纳米复合材料的研究现状.系统地归纳了核壳结构纳米复合材料在光学、催化、医药与生物、光子晶体、超疏水涂层等方面的应用,评述了其特点和发展的方向,并对其应用前景进行了展望...     

Gaussian 03软件在染料化学教学中的应用

讨论了Gaussian 03在染整课程中的具体应用,尤其对结构的稳定性、振动频率、染料颜色和结构的关系、分子的电荷布局在化学反应中的应用进行具体介绍.这些应用极大的丰富了课堂教学内容,提高教学质量.     

Isatin hybrids and their anti-tuberculosis activity

Tuberculosis (TB) is one of the most common and even fatal infectious diseases known to mankind. Millions of new cases are reported every year over the world, and one-third of the world's population is potentially infected with mycobacteria tuberculosis (MTB). Research to develop novel anti-TB drugs led to the identification of several isatin-based antimycobacterial agents, among which a number of potential candidates displayed excellent antimycobacterial activity and were found to be free of cytotoxicity. This review outlines the advances in the application of isatin hybrids as antimycobacterial agents and the critical aspects of design and structure-activity relationship of these derivatives.     

Determination of isoniazid concentration in rabbit vertebrae by isotope tracing technique in conjunction with HPLC

Medications compounded with isoniazid (INH) are usually applied to surgical sites at the completion of surgery to locally kill postoperative residual tubercle bacilli. However, the distribution and elimination of INH in the vertebrae in vivo are not known. In this study, isotope tracing was used in conjunction with high‐pressure liquid chromatography (HPLC) to address this. INH and technetium‐99 m‐labeled INH were applied to the vertebrae of rabbits. After 2 and 6 h, osseous tissues containing INH, as determined by radionuclide imaging, were collected for detection with HPLC. The results showed that INH mainly stayed around the vertebrae 6 h after its application and did not permeate widely into the blood or other organs, except for the kidneys. The standard deviations of INH concentrations in the technetium‐99 m‐INH group were approximately four‐fold smaller than those in the INH group. This method of coupling isotope tracing and HPLC can effectively limit experimental error during sample collection, allowing accurate and reliable identification of the concentration levels of INH in osseous tissues in vivo. Copyright © 2013 John Wiley & Sons, Ltd.     

Synthesis and Antimycobacterial Evaluation of N-(4-(Benzyloxy)benzyl)-4-aminoquinolines

Tuberculosis remains a global health problem that affects millions of people around the world. Despite recent efforts in drug development, new alternatives are required. Herein, a series of 27 N-(4-(benzyloxy)benzyl)-4-aminoquinolines were synthesized and evaluated for their ability to inhibit the M. tuberculosis H37Rv strain. Two of these compounds exhibited minimal inhibitory concentrations (MICs) similar to the first-line drug isoniazid. In addition, these hit compounds were selective for the bacillus with no significant change in viability of Vero and HepG2 cells. Finally, chemical stability, permeability and metabolic stability were also evaluated. The obtained data show that the molecular hits can be optimized aiming at the development of drug candidates for tuberculosis treatment.     

Synthesis of New Cyclomarin Derivatives and Their Biological Evaluation towards Mycobacterium Tuberculosis and Plasmodium Falciparum

Cyclomarins are highly potent antimycobacterial and antiplasmodial cyclopeptides isolated from a marine bacterium (Streptomyces sp.). Previous studies have identified the target proteins and elucidated a novel mode of action, however there are currently only a few studies examining the structure–activity relationship (SAR) for both pathogens. Herein, we report the synthesis and biological evaluation of 17 novel desoxycyclomarin-inspired analogues. Optimization via side chain modifications of the non-canonical amino acids led to potent lead structures for each pathogen.     

Synthesis and biological evaluation of theophylline acetohydrazide hydrazone derivatives as antituberculosis agents

A series of small molecules, theophylline acetohydrazide hydrazone derivatives were obtained via condensation of theophylline-7-acetohydrazide with different aromatic/heterocyclic aldehydes. The compounds were synthesized and characterized by using conventional methods. Further, the compounds and standard drugs were evaluated against Mycobacterium tuberculosis H37Rv strain, the activity obtained was varying depending on the functional group attached to theophylline acetohydrazide hydrazone compounds. Among these, Br-substituted compounds showed more potent against M. tuberculosis with MIC 3.6–4 μM and better than the reference drugs used. The molecular docking studies have shown the possible binding modes of the compounds with protein (PDB ID: 4RHX); the compound 4h has shown highest glide score and binding energy. For all compounds, ADME properties were predicted.     

An Outline of the Latest Crystallographic Studies on Inhibitor-Enzyme Complexes for the Design and Development of New Therapeutics against Tuberculosis

The elucidation of the structure of enzymes and their complexes with ligands continues to provide invaluable insights for the development of drugs against many diseases, including bacterial infections. After nearly three decades since the World Health Organization’s (WHO) declaration of tuberculosis (TB) as a global health emergency, Mycobacterium tuberculosis (Mtb) continues to claim millions of lives, remaining among the leading causes of death worldwide. In the last years, several efforts have been devoted to shortening and improving treatment outcomes, and to overcoming the increasing resistance phenomenon. The structural elucidation of enzyme-ligand complexes is fundamental to identify hot-spots, define possible interaction sites, and elaborate strategies to develop optimized molecules with high affinity. This review offers a critical and comprehensive overview of the most recent structural information on traditional and emerging mycobacterial enzymatic targets. A selection of more than twenty enzymes is here discussed, with a special emphasis on the analysis of their binding sites, the definition of the structure–activity relationships (SARs) of their inhibitors, and the study of their main intermolecular interactions. This work corroborates the potential of structural studies, substantiating their relevance in future anti-mycobacterial drug discovery and development efforts.     

Comparative proteomics analysis between biofilm and planktonic cells of Mycobacterium tuberculosis

Tuberculosis is highly persistent and displays phenotypic resistance to high concentrations of antimicrobials. Recent reports exhibited that Mycobacterium tuberculosis biofilm was implicated to its pathogenicity and drug resistance. In this study, there were 47 kinds of differential proteins in the biofilm of M. tuberculosis H37Rv cells compared with the planktonic bacteria, and 37 proteins were nonredundant and identified by proteomics approach, such as 2DE and LC‐MS/MS. Moreover, six kinds of proteins were identified as HspX, which were conservative and highly expressed in biofilm. Note that 47 differential proteins were divided into seven categories, such as cell wall and cell processes, conserved hypotheticals, intermediary metabolism and respiration, and so on by TUBERCULIST. The Gene Ontology classification results showed that the largest protein group involved in metabolism, binding proteins, and catalytic function accounts for 30% and 57% of all identified proteins, respectively. Moreover, the protein interaction network analyzed by STRING showed that the minority proteins such as RpoA, SucC, Cbs, Tuf, DnaK, and GroeL in the interaction network have high network connectivity. These results implied that the proteins involved in metabolic process and catalytic function and the minority proteins mentioned above may play an important role in M. tuberculosis biofilm formation. To our knowledge, this is the first report about differential proteins between biofilm and planktonic M. tuberculosis, which provided the potential antigens for vaccines and target proteins for anti‐mycobacterial drugs.     

2009-2014年重庆市某中心医院儿童结核病的疫情报告及登记情况分析

目的：了解综合性医疗机构对儿童结核病的疫情报告和结核病患儿到结防机构的登记情况,为儿童结核病防治工作提供理论依据。方法以某区中心医院2009—2014年确诊的0~14岁结核病患儿病案信息、结核病信息网络直报系统和法定传染病报告监测系统中的信息建立数据库,按照不同性别、年龄和诊断进行分组,计算不同组结核病患儿的疫情报告率和在当地结防机构的登记比例。结果某区中心医院共确诊了78例结核病患儿,疫情报告66例,疫情报告率为84．42%,肺外结核病患儿的疫情报告率(61．11%)远低于肺结核患儿(91．84%)和结核性胸膜炎(90．91%);剔重4例,33例在结防机构登记,登记比例为53．23%,10~14岁组在结防机构的登记比例(72．22%)远高于0~4岁组(25．0%)和5~9岁结核病患儿组(28．57%), PTB(63．41%)和结核性胸膜炎(60．00%)的登记比例高于EPTB (9．09%),非结核性脑膜炎和血播型结核病的患儿登记比例(62．75%)高于结脑和血播型结核病的患儿(9．09%)。结论综合医院儿童结核病的疫情报告差,在结防机构登记的比例低。因此,加强医防合作,从而提高非结防机构对儿童结核病的疫情报告和在结防机构的登记比例。     

Ameliorating effects of Tamarindus indica fruit extract on anti-tubercular drugs induced liver toxicity in rats

The study aimed to evaluate the hepatoprotective potential of aqueous extract of Tamarindus indica fruit against combination of two antitubercular drugs viz. Isoniazid and Rifampicin induced hepatotoxicity in rats. In vitro antioxidant activity of aqueous extract of T. indica by DPPH–HPLC method was found to be 81.48%. Treatment with aqueous extract of T. indica significantly reduced the elevated levels of biochemical markers such as SGOT, SGPT, ALP, bilirubin, TBARS and increased the albumin level as well antioxidant activities of SOD, CAT and GSH in intoxicated rats. The biochemical changes were supported by histological observations. Results of this study clearly demonstrate that aqueous extract of T. indica fruit protects against anti tuberculosis induced oxidative liver damage in rats and thus possess significant hepatoprotective activity. Further, it could be suggested that supplementation with this food extract might prove beneficial in the individuals on anti-TB drugs.     

Arylquinolinecarboxamides: Synthesis,in vitro and in silico studies against Mycobacterium tuberculosis

A series of fourteen 6-substituted-2-(methoxyquinolin-3-yl) methyl)-N-(pyridin-3-ylmethyl) benzamides was prepared from commercially available anilines in five simple and convenient synthetic steps. The structures of all new products were confirmed by routine spectroscopic methods: IR, ¹H and ¹³C NMR, and HRMS (electrospray ionization). The resulting arylquinolinecarboxamides were subjected to biological screening assay for in vitro inhibitory activity against Mycobacterium tuberculosis (Mtb) H37Rv strain. Several compounds exhibited modest antitubercular activity with compounds 8–11 , 15 and 19 exhibiting MIC₉₀ values in the range of 32–85 μM. The antitubercular data suggested that inhibition of Mtb can be imparted by the introduction of a non-polar substituent on C-6 of the quinoline scaffold. Further, to understand the possible mode of action of the series, the reported compounds and bedaquiline were subjected to in silico docking studies against MtbATPase to determine their potential to interfere with the mycobacterial adenosine triphosphate (ATP) synthase. The results showed that these compounds have the potential to serve as antimycobacterial agents. In silico ADME pharmacokinetic prediction results showed the ability of these arylquinolinecarcboxamides to be absorbed, distributed, metabolized and excreted efficiently.