Synthesis,In Vitro,and Computational Studies of PTP1B Phosphatase Inhibitors Based on Oxovanadium(IV) and Dioxovanadium(V) Complexes

One of the main goals of recent bioinorganic chemistry studies has been to design and synthesize novel substances to treat human diseases. The promising compounds are metal-based and metal ion binding components such as vanadium-based compounds. The potential anticancer action of vanadium-based compounds is one of area of investigation in this field. In this study, we present five oxovanadium(IV) and dioxovanadium(V) complexes as potential PTP1B inhibitors with anticancer activity against the MCF-7 breast cancer cell line, the triple negative MDA-MB-231 breast cancer cell line, and the human keratinocyte HaCaT cell line. We observed that all tested compounds were effective inhibitors of PTP1B, which correlates with anticancer activity. [VO(dipic)(dmbipy)]·2 H₂O (Compound 4) and [VOO(dipic)](2-phepyH)·H₂O (Compound 5) possessed the greatest inhibitory effect, with IC₅₀ 185.4 ± 9.8 and 167.2 ± 8.0 nM, respectively. To obtain a better understanding of the relationship between the structure of the examined compounds and their activity, we performed a computer simulation of their binding inside the active site of PTP1B. We observed a stronger binding of complexes containing dipicolinic acid with PTP1B. Based on our simulations, we suggested that the studied complexes exert their activity by stabilizing the WPD-loop in an open position and limiting access to the P-loop.     

Al4B2O9纳米棒改性制备优异综合性能的固体聚合物电解质

随着储能设备和电力驱动产品的激增,特别是电动汽车的大规模推广应用,全固态电池被认为是最有可能解决电动设备日益严峻的安全问题和高能量密度需求的策略之一.本文报道了一种Al4B2O9纳米棒改性的聚环氧乙烷(PEO)基固体聚合物电解质(ASPE),其具有高离子电导率、宽电化学窗口、良好的机械性能和阻燃性能.具体来说,因为Al...     

Production of Lacto-N-biose I Using Crude Extracts of Bifidobacterial Cells

Lacto-N-biose I (LNB) is supposed to represent the bifidus factor in human milk oligosaccharides, and can be practically produced from sucrose and GlcNAc using four bifidobacterial enzymes, 1,3-β-galactosyl-N-acetylhexosamine phosphorylase, sucrose phosphorylase, UDP-glucose-hexose 1-phosphate uridylyltransferase, and UDP-glucose 4-epimerase, recombinantly produced by Escherichia coli. Here the production of LNB by the same enzymatic method without using genetically modified enzymes to consider the use of LNB for a food ingredient was reported. All four enzymes were produced as the intracellular enzymes of Bifidobacterium strains. The mixture of the crude extracts contained all four enzymes, with other enzymes interfering with the LNB production, namely, phosphoglucomutase, fructose 6-phosphate phosphoketolase, and glycogen phosphorylase. The first two interfering enzymes were selectively inactivated by heat treatment at 47 °C for 1 h in the presence of pancreatin, and glycogen phosphorylase was disabled by hydrolyzing its possible acceptor molecules using glucoamylase. Finally, 91 % of GlcNAc was converted into LNB in the 100-mL reaction mixture containing 300 mM GlcNAc.     

Webmenthods的设计与实现

为了更好地应用WebMethods,该文提供了一个基于B2B项目的环境,用于对WebMethods的设计,实现,从而大大提高WebMethods的管理和操作以及易用性和可维护性。     

基于特征断面的复杂巷道段三维建模

为解决巷道断面随工程需要及岩层变化不断改变,导致巷道三维建模程序复杂的问题,提出基于特征断面的巷道三维建模思想,通过建立巷道特征断面模型库,实现变化巷道段的三维建模,以期提高复杂巷道段的建模效率。首先阐述建模数据的采集方法,并对巷道断面进行了细化坐标分析;同时提出拐角处断面变化巷道段的平滑处理算法（通过圆弧来圆滑拐角处巷道中心线）,对普通巷道段采用三角剖分形成三角网完成巷道段的建模;而巷道断面发生变化的复杂巷道段存在简单曲面四边形,采用Bézier曲面及曲面的拼接完成巷道段的建模,并在实验中进行了验证     

化学灌浆技术在锦屏一级电站工程中的试验研究

介绍了锦屏一级水电站化学灌浆试验研究及施工情况,明确在此类地质条件下采用化学灌浆是完全必要且可行的,整个试验取得了成功,对今后工程的实施及类似工程项目的试验研究具有借鉴意义。     

信号转导和转录激活子5信号转导途径对受辐射KG-1细胞周期的调控作用

探讨信号转导和转录激活子５（ＳＴＡＴ５）信号转导途径在受辐射ＫＧ－１细胞中对细胞周期的调控作用。通过转染ＳＴＡＴ５基因的显性负突变体（ＤＮ－ＳＴＡＴ５）阻断ＪＡＫ／ＳＴＡＴ的信号传递后,瞬间转染ｃｙｃｌｉｎＤ１基因及ｃｙｃｌｉｎＢ１基因,观察ｃｙｃｌｉｎＤ１蛋白及ｃｙｃｌｉｎＢ１蛋白对受辐射细胞周期阻滞的影响作用。转染ＤＮ－ＳＴＳＡＴ５基因的受辐射ＫＧ－１细胞即使用粒－巨噬细胞集落刺激因子（ＧＭ－ＣＳＦ）刺激亦不能跳出Ｇ１期阻滞;瞬间转染ｃｙｃｌｉｎＤ１基因及ｃｙｃｌｉｎＢ１基因分别能促进受辐射细胞跳出Ｇ１期和Ｇ２期阻滞。ＧＭ－ＣＳ所激活的ＪＡＫ／ＳＴＡＴ信号转导途径通过促进周期蛋白ｃｙｃｌｉｎＤ１及ｃｙｃｌｉｎＢ１的表达而对受辐射细胞周期进行调控。     

基于B/S结构的服装销售管理系统的设计与实现

针对现有服装销售管理的现状及信息化需求,研究了基于B/S结构的服装销售管理系统,并利用asp加以实现。通过三层结构实现了系统的原型设计,介绍了基于B/S结构的服装销售管理系统的体系结构、功能及系统实现的关键技术。     

数字温度测量模块LTM8003及其应用

LTM8003是一种新型数字温度传感器模块，该模块具有管理512个数字温度传感器的能力，它可利用其自身的RS－485口来和上位机一起构成数字多点测温网络系统，可广泛应用于粮食、档案库等行业的温度监测系统中，文中介绍了该模块的特点、命令集及典型应用。