High-level expression of soluble human β-defensin-2 fused with green fluorescent protein in Escherichia coli cell-free system

Human β-defensin-2 (hBD2), a small cationic peptide, exhibits a broad range of antimicrobial activity and does not acquire any microbial resistance. To produce this uneasily detectable, degradable, and toxic polypeptide efficiently, an alternative approach based on the Escherichia coli cell-free biosynthesis system was proposed. The approach implies that a polypeptide of interest is synthesized as a fusion protein linked to a green fluorescent protein (GFP) through a cleavable spacer. With batch-mode operation, a significant amount of hBD2 fused with GFP (0.25 mg/mL) can be expressed in this cell-free system. The productivity of the fusion protein can be improved up to 1.2 mg/mL by employing a continuous-exchange cell-free system. Furthermore, the GFP moiety provides directly visible and quantitative monitoring of the polypeptide synthesis, and the product is soluble and stable. This work will be helpful in allowing the rapid and visible expression of other similar defensins using an in vitro cell-free system.     

共轭高分子的研究——Ⅶ.脂肪腈类的聚合

<正> 聚腈作为新的一类共轭高分子而引起注意。本文在前报的基础上进一步选择了一系列脂肪腈(乙腈、丙腈、戊腈、庚腈和苯乙腈),系统地研究它们在络合能力较强的付氏试剂(BF_3和TiCl_4等)作用下的聚合反应与机理,同时测定了各聚腈的物理性能。 1.腈的络合聚合 腈类与付氏试剂可形成定组成的络合物结晶:     

Highly efficient nitration of phenolic compounds in solid phase or solution using Bi(NO3)3.5H2O as nitrating reagent

[reaction: see text] Bi(NO(3))(3).5H(2)O was used as an efficient nitrating reagent in the nitration of phenolic compounds to give nitrated phenols in good to high yields. The nitration reaction proceeded smoothly by grinding 1 equiv of phenol, 2-methylphenol, 4-methylphenol, or 4-chlorophenol and Bi(NO(3))(3).5H(2)O, and the nitration of other phenolic compounds could be performed in acetone at ambient temperature (22-30 degrees C).     

Palladium-catalyzed amination of aryl bromides with hindered N-alkyl-substituted anilines using a palladium(I) tri-tert-butylphosphine bromide dimer

An efficient palladium-catalyzed amination of aromatic bromides with hindered N-alkyl-substituted anilines is described, either using the combination of Pd(OAc)(2) and P(t-Bu)(3) or a palladium(I) tri-tert-butylphosphine bromide dimer, [Pd(mu-Br)(t-Bu(3)P)](2), a new, commercially available, and easily handled catalyst.     

Addressing the metabolic activation potential of new leads in drug discovery: a case study using ion trap mass spectrometry and tritium labeling techniques

Metabolic activation of drug candidates to electrophilic reactive metabolites that can covalently modify cellular macromolecules may result in acute and/or idiosyncratic immune system-mediated toxicities in humans. This presents a significant potential liability for the future development of these compounds as safe therapeutic agents. We present here an example of an approach where sites of metabolic activation within a new drug candidate series were rapidly identified using online liquid chromatography/multi-stage mass spectrometry on an ion trap mass spectrometer. This was accomplished by trapping the reactive intermediates formed upon incubation of compounds with rat and human liver microsomes as their corresponding glutathione conjugates and mass spectral characterization of these thiol adducts. Based on the structures of the GSH adducts identified, potential sites and mechanisms of bioactivation within the chemical structure were proposed. These metabolism studies were interfaced with iterative structural modifications of the chemical series in order to block these bioactivation sites within the molecule. This strategy led to a significant reduction in the propensity of the compounds to undergo metabolic activation as evidenced by reductions in the irreversible binding of radioactivity to liver microsomal material upon incubation of tritium-labeled compounds with this in vitro system. With the efficiency and throughput achievable with such an approach, it appears feasible to identify and address the metabolic activation potential of new drug leads during routine metabolite identification studies in an early drug discovery setting.     

钴膦簇合物的催化环丙烷化反应

本文首次利用碳基钴簇合物ＰｈＰＣｏ_３（ＣＯ）_９催化剂，在常压和－２０℃－０℃，用苯乙烯和重氮乙酸乙酯进行环丙烷化反应，合成了菊酸酯，重氮乙酸乙酯可全部转化，酯的选择性可达８５％。产物经减压分馏后，由ＩＲ和￣１ＨＮＭＲ分析，确证了产物为菊酸酯，表明了羰基钴簇合物对苯乙烯的环丙烷化反应有良好的催化性能，为四面体异核簇合物用于不对称催化反应打下了基础。     

由聚苯胺粒子组成的电流变液的研究

由经碱处理的掺杂态聚苯胺（ＰＡｎ）制得高介电常数的半导体ＰＡｎ粒子，将其悬浮于电绝缘油可组成电流变液，讨论了电流变（ＥＲ）液的静态屈服应力（τ＿ｓ），电流密度等性能与ＰＡｎ的介电常数（ε＿ｐ），导电率（σ），体积分数和应用电场强度的关系。对导电率相同的ＰＡｎ粒子，用氨水处理的ＰＡｎ粒子ε＿ｐ较用ＮａＯＨ液处理的高，前者在σ足够低如σ≤１．０×１０￣（－７）／ｃｍ时，ＥＲ液的τ＿ｓ随偶极系数的平方（β￣２）的增大而呈现非线性增加；后者ＥＲ液的τ＿ｓ随β￣２的增大出现一最大值．结果表明：由聚苯胺粒子可组成高电流变活性的无水ＥＲ液．     

In Situ Monitoring of Generation and Precipitation of Ferric Hydroxide Sol with a Piezoelectric Quartz Crystal Impedance Analyzer

The piezoelectric quartz crystal (PQC) impedance technique was applied to monitor in situ generation and precipitation of the ferric hydroxide sol in aqueous solutions at 90 degrees C. Equivalent circuit parameters and resonant frequencies as well as the half-peak width of the electroacoustic conductance spectrum deltaf(G1/2) for the PQC resonance were obtained and analyzed. Three stages, sol generation and simultaneous adsorption, adsorption equilibrium, and precipitation of ferric hydroxide sol could be identified in the process of adding the ferric nitrate solution into the hot water. A scheme of two consecutive reactions occurring at the electrode/solution interface was used to analyze the adsorption kinetics of ferric hydroxide sol onto the Au electrode. In addition, the electrolyte-induced precipitation of the colloid was monitored and discussed. Temperature effect on the PQC resonance behavior in liquid was also investigated. Since the PQC impedance technique provides multidimensional piezoelectric information in situ, it is highly recommended for studying the process of sol-gel generation and precipitation. Copyright 2001 Academic Press.     

硅胶担载四核羰基钴催化剂的EXAFS和IR研究

本文以透射法EXAFS和IR等手段研究了四核羰基钴金属簇Co_4(CO)_(10)(PPh)_2担载在SiO_2上以后及用于烯烃醛化反应前后的变化,确定了相应的结构参数并探讨了催化活性与结构的关系。