(R)-2-羟基-4-苯基丁酸乙酯的合成

综述了血管紧张素转化酶抑制剂类治疗高血压和充血性心力衰竭药物的关键中间体（R）－2－羟基－4－苯基丁酸乙酯的合成方法。参考文献25篇。     

Micro-Determination of Protein Containing SH– and –S–S– Groups Based on the Polarographic wave of an Electroactive Derivative

This paper presents a new simple and sensitive method for the micro-determination of protein containing SH– and –S–S– groups based on the single sweep polarographic wave of an electroactive derivative. In 0.04molL^–1 Na₃PO₄ and 0.2% ascorbic acid solution, protein is heated in a boiling water bath for 15min, the reaction product giving a sensitive reduction wave at –0.70V (vs. SCE). The wave height is linearly proportional to the concentration of protein. The calibration curves of bovine serum albumin (BSA), human serum albumin (HSA), ovalbumin (OVA) and lysozyme (Lyso) are constructed under the optimal conditions. For BSA and HSA, the linear ranges and detection limits are 0.05–24mgL^–1 and 0.02mgL^–1, respectively. The method has been applied to the determination of protein in human serum samples with satisfactory results. The mechanism of the polarographic wave was also studied, and the results show that S^2– ion is released from the protein molecule during the derivatization reaction, the wave being attributed to the reduction of HgS.     

Structure control within poly(amidoamine) dendrimers: size, shape and regio-chemical mimicry of globular proteins

This work describes the syntheses of a new poly(amidoamine) (PAMAM) dendrimer family possessing a disulfide function (cystamine) in its core. Traditional redox-chemistry associated with the disulfide core in these dendrimer structures, provides a versatile strategy for designing unique sizes, shapes and controlling the regio-disposition of chemical groups on the surface of these dendrimers. Various single site, sulfhydryl functionalized dendron reactants may be generated in situ, under standard reducing conditions (i.e. dithiothreitol (DTT)). Facile control of size, shape and chemical functionality placement involves covalent hybridization of these single point, sulfhydryl reactive dendron components. This is accomplished by re-oxidation in the presence of air, to yield generation/surface chemistry differentiated cross-over products which may be isolated by preparative thin layer or column chromatography. Differentiated cystamine core dendrimers derived from combination and permutation of lower generation (i.e. Gen.=0-3) sulfhydryl functionalized dendrons possessing amino, hydroxyl, acetamido or dansyl surface groups, were synthesized and isolated. They were characterized by a variety of methods including; ¹³C NMR, capillary electrophoresis (CE), gel electrophoresis (PAGE), thin layer chromatography (TLC) and electrospray (ES) or matrix assisted laser desorption ionization (MALDI-TOF) mass spectrometry. This general strategy has broad implications for the systematic size, shape and regio-chemical control of a wide range of dendritic nanostructures, many of which may be designed to mimic the sizes, shapes and regio specific chemo-domains observed for globular proteins.     

Preparation, characterization, and application of multistimuli-responsive microspheres with fluorescence-labeled magnetic cores and thermoresponsive shells

Novel functional microspheres with multistimuli-responsive properties have been prepared and characterized. The as-prepared microspheres respond to an external magnetic field, environmental temperature, and ultraviolet radiation. The in vitro drug-loading efficiency and drug-release behavior of these microspheres demonstrated that they could be used as drug carriers for drug controlled release. The results of in vivo distribution investigations of these microspheres showed that they exhibit a high magnetic-targeting effect, which holds promise for applications in various fields such as magnetic drug targeting and tissue labeling, among others.     

Rapid Protein Hydrolysis by Microwave Irradiation Using Heat-Resistant Teflon-Pyrex Tubes

A rapid peptide-bond hydrolysis by means of microwave irradiation is introduced for the facile preparation of protein hydrolysates used for amino acid analysis. The optimal hydrolysis condition has been determined using several enzymes with known amino acid compositions. The effects of hydrolysis time on the recovery of various labile and hydrophobic amino acids are also exemplified in the microwave heating of standard amino acids. The method has been applied to the complete amino acid analysis with a single nonvolatile solvent of methanesulfonic acid with good recovery of tryptophan and half-cystine. It provides a radical expedition of protein and peptide hydrolysis via commercial microwave ovens and specially-designed Teflon-Pyrex tubes, circumventing the tedious procedures using vacuum-sealed pyrex lubes heating at 110°C for more than 24 h. This novel type of microwave chemistry associated with rapid peptide-bond cleavage is of great potential in the automation of the complete process of amino acid analysis starting from the preparation of protein hydrolysates.     

功能液晶膜的新进展

论述了功能液晶膜的新近研究结果和发展动向,指出功能液晶膜具有优异的气体分离、液体分离和电光性能,可望作为高效气体分离膜、高效液体分离膜和大面积光控膜,具有较重大的理论与实际意义。     

Time‐resolved Fourier transform infrared/attenuated total reflection spectroscopy for the measurement of molecular diffusion in polymers

Over the past 2 decades, the use of time‐resolved Fourier transform infrared/attenuated total reflection (ATR) spectroscopy for the measurement of diffusion in polymers has grown. ATR is a powerful technique for the measurement of diffusion in polymers because it is an in situ technique that is relatively inexpensive, provides reliable short‐time data, and provides a wealth of information at the molecular level. This article highlights the technique and its application to numerous studies, ranging from the diffusion of drugs in human skin to chemical warfare agents in barrier materials. In addition to these topics, recent studies with ATR to quantify and model molecular interactions during the diffusion process are reviewed. In the future, the ATR technique may have an impact on a variety of emerging fields in which diffusion in polymers plays an important role, such as fuel cells, membrane separation, sensors, and drug delivery. © 2003 Wiley Periodicals, Inc. J Polym Sci Part B: Polym Phys 41: 2794–2807, 2003     

New methods for data analysis of isothermal titration calorimetry

Heat divided by ligand concentration vs. heat, similar to the Scatchard plot, was introduced to obtain the equilibrium constant (K) and the enthalpy of binding (DH) using isothermal titration calorimetry data. Values of K and DH obtained by this linear pseudo-Scatchard plot for a system with a set of independent binding sites (such as binding fluoride ions on urease and monosaccharide methyl a-D-mannopyranoside on concavalin A) were remarkably like that obtained from a normal fitting Wiseman method and other our technical methods. On applying this graphical method to study the binding of copper ion on myelin basic protein (MBP), a concave downward curve obtained was consistent with the positive cooperativity in the binding. A graphical fitting by simple method for determination of thermodynamic parameters was also introduced. This method is general, without any assumption and restriction made in previous method. This general method was applied to the product inhibition study of adenosine deaminase. This revised version was published online in July 2006 with corrections to the Cover Date.     

Concerning the Thermal Diastereomerization of the Green Fluorescent Protein Chromophore

Summary. Two model compounds for the green fluorescent protein chromophore were prepared. One of them incorporates the natural 4-hydroxybenzylidene group of the natural tyrosin derived chromophore, the other one bears a methyl group instead of the hydroxy group. Whereas the photochemically prepared (E)-diastereomer of the first compound very effectively reverted thermally (room temperature) to the thermodynamically stable (Z)-diastereomer, the (E)-diastereomer of the second derivative proved to be stable even at elevated temperatures for more than a day. This finding can be rationalized by constructing the appropriate resonance structures showing that only in the first case an effective delocalization enables partial single bond character of the benzylidene double bond. From the standpoint of chemical etiology, only Nature’s choice of the tyrosin derived chromophore of the green fluorescent protein provides an efficient radiationless thermal relaxation channel for the unwanted photo-diastereomerization product formed after excitation besides the dominating fluorescence channel of its chromophore.