Modeling of protein adsorption to DEAE sepharose FF: Comparison of data with model simulation

The equilibrium and kinetic characteristics of the adsorption of human serum albumin (HSA) and ovalbumin (OVA) to the DEAE Sepharose FF weak anion exchanger were experimentally determined. The rate for protein adsorption was simulated with two different models, the first being based on a single lumped kinetic parameter, while the second includes the individual mass transfer processes occurring prior to the adsorption intervention, i.e., diffusion across the liquid film surrounding individual particles and diffusion within the ion exchanger particle itself. The actual adsorption of OVA to DEAE Sepharose FF in fully mixed stirred vessels and in packed bed columns was consistent with both models. In the case of HSA, however, the adsorption profile in an agitated vessel was consistent only with the pore diffusion model and neither model could correctly predict the latter part of the breakthrough profile observed in packed bed experiments.     

基于IHSA_LSSVM的供应链绩效评估研究

为有效评估供应链绩效,结合和声搜索算法(IHSA)与最小二乘支持向量机,提出一种评估算法(IHS_LSSVM)。研究和声搜索算法的原理,对基音调整概率和基音调整步长进行动态调整,给出一种改进的和声搜索算法。利用该算法的全局搜索能力优化选取LSSVM的惩罚因子r和高斯核函数的半径σ。采用供应链绩效评估实例,构建供应链评估模型。仿真实验结果表明,与已有的BP神经网络和LSSVM等评估算法相比,IHS_LSSVM具有更小的预测误差和更高的预测精度。     

Efficient loading and entrapment of tamoxifen in human serum albumin based nanoparticulate delivery system by a modified desolvation technique

Herein, the poorly water-soluble drug, Tamoxifen (Tmx), was loaded in the amphipathic matrix of human serum albumin (HSA) nanoparticles by a modified desolvation method. In order to enhance the drug loading (DL) and drug entrapment efficiency (DEE) (<2% and 10%, respectively), ultrasonication of Tmx-HSA mixture was performed prior to desolvation process. Tmx loading and entrapment efficiency were optimized by employment of the response surface methodology (RSM)-central composite design (CCD) of experiments. Under the optimum conditions of 1.59 mg Tmx/ml concentration, 7.76 pH and 5 h incubation of HSA-Tmx, the DL of 6.7% and DEE of 74% are achievable. Particles with the average size of 195 nm, zeta potential of −21 mV and polydispersity index of 0.09 were produced under these conditions. A more sustained Tmx release behavior was observed from polyethylene glycol (PEG) conjugated nanoparticles in comparison to the non-PEGylated ones. The short-term stability investigation showed no alteration in physicochemical properties of nanoparticles at 4 and 37 °C, but small increase in nanoparticles size was observed after three months of storage at room temperature. This is the first report for efficient production of a Tmx delivery system based on HSA nanoparticles.     

一种噻菁染料的合成及其在HSA检测中应用

研究设计合成一种新型噻菁染料Dyel,在PBS缓冲溶液中实现对人血清白蛋白(HSA)高选择性检测.向Dyel-PBS体系中加入HSA后,通过检测荧光,发现Dyel在444 nm处的荧光强度显著增加,说明此体系可应用于HSA检测.优化检测条件后,在HSA浓度为3-30 mg/L时,HSA与Dyel有良好的线性关系(R2 ...     

Incorporation of HSA Microparticles Within the Taxol-Loaded In Situ Forming PLGA Microspheres: Synthesis,Characterization, and Drug Release

Taxol-loaded poly(lactic acid-co-glycolic acid) (PLGA) microspheres containing different portions of human serum albumin microparticles (mHSA) were prepared via an in situ forming method. mHSA was obtained using a freezing-induced phase separation method and further surface modified via PLGA chains (g-mHSA). Surface modification of mHSA improved their dispersion within microspheres. Incorporation of 3% mHSA within microspheres increased their size and surface porosity, while g-mHSA decreased their size. Addition of 1.5% and 3% mHSA into microspheres decreased their initial burst release from 40.7% to 21.1% and 10.2%, respectively. Microspheres consisting 1.5% and 3% g-mHSA displayed 29.9% and 33.1% initial burst release, respectively.     

羟基肉桂酸衍生物的合成及其与人血清白蛋白的相互作用

以咖啡酸、间羟基肉桂酸为母体,分别与止血芳酸反应,设计合成两种羟基肉桂酸衍生物I、II,并用MS、IR、1H-NMR、13C-NMR进行结构表征。采用荧光光谱法、同步荧光光谱法、紫外可见光谱法结合分子对接技术研究其在体外生理条件下与HSA之间的相互作用机制。光谱实验结果表明,衍生物I和II都可以使HSA的内源荧光发生静态猝灭,相互作用力主要是氢键和范德华力,且对HSA的构象产生一定的影响。分子对接结果表明衍生物I、II与HSA中的结合位于亚结构域IIA（即site I）中,作用力主要是氢键和范德华力,同时还存在着疏水作用,且衍生物距色氨酸残基(Trp214)很近,很好地解释了衍生物有效猝灭HSA内源荧光的实验现象。分子对接与实验获得了一致性的结果,二者相互作证,提高了实验结果推断的准确度。     

Synthesis of Novel Tetra(µ3-Methoxo) Bridged with [Cu(II)-O-Cd(II)] Double-Open-Cubane Cluster: XRD/HSA-Interactions,Spectral and Oxidizing Properties

A new double-open-cubane core Cd(II)-O-Cu(II) bimetallic ligand mixed cluster of type [Cl₂Cu₄Cd₂(NNO)₆(NN)₂(NO₃)₂].CH₃CN was made available in EtOH/CH₃CN solution. The 1-hydroxymethyl-3,5-dimethylpyrazole (NNOH) and 3,5-dimethylpyrazole (NNH) act as N,O-polydentate anion ligands in coordinating the Cu(II) and Cd(II) centers. The structure of the cluster in the solid state was proved by XRD study and confirmed in the liquid state by UV-vis analysis. The XRD result supported the construction of two octahedral and one square pyramid geometries types around the four Cu(II) centers and only octahedral geometry around Cd(II) two centers. Interestingly, NNOH ligand acts as a tetra-µ³-oxo and tri-µ²-oxo ligand; meanwhile, the N-N in NNH acts as classical bidentate anion/neutral ligands. The interactions in the lattice were detected experimentally by the XRD-packing result and computed via Hirschfeld surface analysis (HSA). The UV-vis., FT-IR and Energy Dispersive X-ray (EDX), supported the desired double-open cubane cluster composition. The oxidation potential of the desired cluster was evaluated using a 3,5-DTB-catechol 3,5-DTB-quinone as a catecholase model reaction.     

液压液芯压下技术的应用实践

马钢薄板坯连铸连轧是目前世界上最先进的热轧板卷生产线之一，其连铸机设计为4个扇形段，使用了液压液芯压下技术。该文重点介绍液压液芯压下系统组成、工作原理以及实践经验。     

药物小分子与人血清白蛋白作用的研究手段进展

随着药物的普遍使用,研究药物与人血清白蛋白的作用机理不仅可了解药物的运输、代谢过程;而且对临床用药、药物设计、新药开发具有重要指导意义。文章综述了药物小分子与人血清白蛋白相互作用的研究手段。