糖苷配合物与DNA作用机理的电化学研究进展

本文综述了糖苷配合物的合成、表征、生物功能及糖化学研究现状，并对糖苷功能配合物与DNA的作用机理及生物功能的电分析化学研究进行了探讨。着重讨论了应用电分析化学、谱学方法、单晶X-射线衍射分析来研究糖苷功能配合物。引用文献39篇。     

Novel Water Soluble Fluorescent Trimethine Indocyanines Containing N-ρ-Carboxybenzyl Group

Indocyanine dyes as fluorescent labeling reagents have been used in bioanalysis1,2. Arylsulfonate indocyanine dyes 1d and 1e developed by Waggoner A. S. et al.3,4 have excellent fluorescent properties combined with good aqueous solubility, are a new generation of fluorescent label compounds for proteins, oligonucleotides and other compounds containing hydroxyl, mercaptol or primary amine groups5. However, photostability of these dyes has been a problem. Z. G. YAO et al.6 reported that p…     

烟酸铬(Ⅲ)的配位结构与生物活性关系

合成了2种新型吡啶-3-羧酸(烟酸)铬(Ⅲ)螯合物,通过元素分析、热分析、红外光谱和电子光谱证明烟酸作为双齿配位体,形成具有3个六员环的螯合物Cr(Nic)3和具有2个六员环与2个H2O单体的混型配合物[Cr(Nic)2(H2O)2]Cl。通过使用效能等试验表明,在猪饲料中添加不同配位结构的烟酸铬均有明显提高饲料利用率、促进生长和显著提高机体对葡萄糖的清除率等作用。试验还表明,双齿配位的烟酸铬具有较高的生物活性、无毒、饲用后在肌体内无残留,作为饲料添加剂具有广阔的应用前景。     

二元酸茄呢醇乳糖和麦芽糖酯合成及生是活性测试研究

七个二元酸茄呢基单酯分别与溴代乙酰乳糖和溴代乙酰麦芽糖在四丁基溴化铵 催化下反应生成对应的糖酯，制得的十四个化合物均为新化合物，其结构经过了元 素分析、IR，~1H NMR和MS确证。并对六个化合物做了KB（人口腔上皮癌细胞）、 Bel-7402（人肝癌细胞）、HCT-8（人结肠癌细胞）三种癌细胞初步生理活性测试。     

2,3-二取代-4-(IH-l,2,4-三唑-l-基)-5-苯基氢基噻吩的合成及生物活性研究

合成了九个以噻吩为母体环的含三唑环的化合物——2，3-二取代-4-(1H-1， 2，4．三唑-1-基)-5-苯基氨基噻吩(2a-2i)，并测定了2a的晶体结构．晶体为三斜 晶系，P-1空间群，晶胞参数为：a=0．79816(15)nm，b=1．00259(13)nm，c=1． 4478(4)nm，a=100．326(16)°，β=94．69(2)°，r=106．083(9)°，V=1．0845 (4)nm～3，z=2，D_c=1．396 g／cm～3．初步生物活性表明所有目标化合物杀菌活 性较低，有一定的植物生长调节活性．     

Simultaneous quantification of ondansetron and tariquidar in rat and human plasma using a high performance liquid chromatography‐ultraviolet method

Ondansetron, a widely used antiemetic agent, is a P‐glycoprotein (P‐gp) substrate and therefore expression of P‐gp at the blood–brain barrier limits its distribution to the central nervous system (CNS), which was observed to be reversed by coadministration with P‐gp inhibitors. Tariquidar is a potent and selective third‐generation P‐gp inhibitor, and coadministration with ondansetron has shown improved ondansetron distribution to the CNS. There is currently no reported bioanalytical method for simultaneously quantifying ondansetron with a third‐generation P‐gp inhibitor. Therefore, we aimed to develop and validate a method for ondansetron and tariquidar in rat and human plasma samples. A full validation was performed for both ondansetron and tariquidar, and sample stability was tested under various storage conditions. To demonstrate its utility, the method was applied to a preclinical pharmacokinetic study following coadministration of ondansetron and tariquidar in rats. The presented method will be valuable in pharmacokinetic studies of ondansetron and tariquidar in which simultaneous determination may be required. In addition, this is the first report of a bioanalytical method validated for quantification of tariquidar in plasma samples.     

Determination of acidic drugs in biological and environmental matrices by membrane‐based dual emulsification liquid‐phase microextraction followed by high‐performance liquid chromatography

A simple method is introduced providing a highly clean microextraction for the determination of some anti‐inflammatory drugs as the model analytes in human urine and environmental matrices. This method is based upon the implementation of two consecutive emulsification liquid‐phase microextractions, which are separated by a syringe filtration step. In this method, the organic extraction solvent (dihexyl ether) is dispersed into the aqueous sample solution (20 mL), and the resulting cloudy mixture is passed through a hydrophilic polytetrafluoroethylene syringe filter. By this action, the extraction phase containing the analytes and many interfering species that could be transferred into the organic phase is retained behind the hydrophilic membrane. The filter is then detached from the syringe and attached to another syringe containing an aqueous solution (pH 12.0, 150 μL), and by the in‐syringe dispersion of the organic phase into the aqueous phase, the analytes are selectively back‐extracted into the aqueous phase. The developed method is centrifuge‐free and very simple, and provides a high sample clean‐up in a few minutes. Under the optimized experimental conditions, the developed method provided a linearity in the range of 2.0–2000 ng/mL, a low limit of detection (0.5 ng/mL), and enrichment factors of 47–53.     

A rapid,sensitive, and widely applicable method for quantitative analysis of underivatized amino acids in different biological matrices by UHPLC‐MS/MS

A rapid, sensitive, and widely applicable method for the simultaneous quantitative analysis of 20 underivatized amino acids in different biological matrices, including serum, plasma, and tissue homogenates, using ultra high performance liquid chromatography with tandem mass spectrometry was developed and validated. Only 4 µL of serum, plasma, or tissue homogenate was extracted with 996 µL of solution (1.7 mM ammonium formate in 85% acetonitrile containing 0.1% formic acid) containing 100 ng/mL phenylalanine‐d5 as an internal standard without any further derivatization step. In addition, the matrix effects were small because a large volume of extraction solution was used. The total run time including reequilibration was 13 min. The results of linearity, accuracy, repeatability, precision, limits of detection, limits of quantification, and sample stability were sufficient to allow the measurement of the amino acids in different biological matrices. We conclude that our method is rapid, sensitive, and widely applicable and represents an improvement over other currently available technologies.     

基于Aerolysin纳米孔道对单个c-di-AMP分子的检测研究

环二腺苷酸(c-di-AMP)是原核细胞中普遍存在的第二信使, 不仅能够有效调控细胞生长、离子转运、细胞壁代谢平衡等多种生理过程, 还能引发I型干扰素应答, 激发机体天然免疫反应. 本实验使用单个气单胞菌溶素(Aerolysin)纳米孔道蛋白构建的单分子界面, 对c-di-AMP进行单分子测量研究. 为提高Aerolysin纳米孔对带负电小分子化合物的测量灵敏度, 本实验利用LiCl为支持电解质, 有效屏蔽Aerolysin孔口表面负电荷, 减小c-di-AMP与Aerolysin纳米孔之间的静电排斥, 从而显著增强了Aerolysin纳米孔道对单个c-di-AMP分子的检测能力. 实验结果显示, 在90 mV电压下, 每分钟在LiCl中获得的有效穿孔事件的数量最高可达同条件KCl支持电解质的30倍, 且有效穿孔事件占总体事件的比例在不同电压下提升了7~11倍. 进一步表明, 使用LiCl支持电解质, 可有效增强Aerolysin孔道对带负电小分子化合物的测量灵敏度. 因此, 本研究实现了Aerolysin纳米孔道对单个环二核苷酸的高灵敏免标记检测, 有望为单分子水平上阐明新型免疫干扰机制提供新的分析方法.