新型Ebselen类似物的合成研究

在已知具有很强抗氧化作用的2-苯基-1，2-苯并异硒唑-3（2H）酮（Ebselen）的基础上，将其2-位苯环更换为不同杂环或取代苯环，设计并合成了5种Ebselen类似物，其抗肿瘤生物活性体外筛选试验正在进行中．     

翻译中的文化障碍

翻译工作的实质是不同语言、文字的文化转换,其最高境界就是“通、达、顺”。要很好地做到这一点,必须克服翻译中的文化障碍。本文从中英文化差异入手,探讨文化障碍的主要表现与突破文化障碍的途径。     

学校学生信息管理系统的设计与实现

本论文介绍了学校学生信息管理系统的实现过程:包括系统分析、系统调查、系统功能设计、系统实现、数据库设计等。本系统主要功能有对学生信息、学生选课信息、学生成绩、教师信息的录入、修改、删除、查询等。     

SU5416 sensitizes ovarian cancer cells to cisplatin through inhibition of nucleotide excision repair

SU5416 is reported to be a selective inhibitor of vascular endothelial growth factor, and it has metwith limited success in the clinic. In the present study, we investigated whether SU5416 could augment cisplatin-induced cytotoxicity in human ovarian cancer cells. When used as a single agent, 2-h exposures to SU5416 were not harmful to the cells up to doses of 100 microM. For 48-h exposures, the SU5416 IC20 and IC50 were 17 and 34 microM, respectively. When used with cisplatin, the effect of SU5416 was sequence dependent. SU5416 given first was subadditive, whereas cisplatin given first was supraadditive. Cisplatin was given as a 1-h exposure. Augmented cisplatin cytotoxicity was seen with 2-h exposures to SU5416 at doses of 17-34 microM. This was associated with a decrease in cisplatin-DNA adduct repair, as measured by atomic absorbance spectrometry. Treatment of the ovarian carcinoma cells with SU5416 was also associated with a reduced expression of ERCC-1 protein and c-jun mRNA, as well as a decrease in c-Jun and JNK activities. We conclude that SU5416 can be used to augment cisplatin-induced cell killing at doses that are non-toxic. This effect may occur through direct or indirect reduction of the activity of AP-1 and DNA repair.     

Multiple flavonoid-binding sites within multidrug resistance protein MRP1

Recombinant nucleotide-binding domains (NBDs) from human multidrug resistance protein MRP1 were overexpressed in bacteria and purified to measure their direct interaction with high-affinity flavonoids, and to evaluate a potential correlation with inhibition of MRP1-mediated transport activity and reversion of cellular multidrug resistance. Among different classes of flavonoids, dehydrosilybin exhibited the highest affinity for both NBDs, the binding to N-terminal NBD1 being prevented by ATP. Dehydrosilybin increased vanadate-induced 8-N₃-[-³²P]ADP trapping, indicating stimulation of ATPase activity. In contrast, dehydrosilybin strongly inhibited leukotriene C₄ (LTC₄) transport by membrane vesicles from MRP1-transfected cells, independently of reduced glutathione, and chemosensitized cell growth to vincristine. Hydrophobic C-isoprenylation of dehydrosilybin increased the binding affinity for NBD1, but outsite the ATP site, lowered the increase in vanadate-induced 8-N₃-[-³²P]ADP trapping, weakened inhibition of LTC₄ transport which became glutathione dependent, and induced some cross-resistance. The overall results indicate multiple binding sites for dehydrosilybin and its derivatives, on both cytosolic and transmembrane domains of MRP1.Received 1 May 2003; received after revision 18 June 2003; accepted 24 June 2003     

Comparative analyses of multi-species sequences from targeted genomic regions

The systematic comparison of genomic sequences from different organisms represents a central focus of contemporary genome analysis. Comparative analyses of vertebrate sequences can identify coding and conserved non-coding regions, including regulatory elements, and provide insight into the forces that have rendered modern-day genomes. As a complement to whole-genome sequencing efforts, we are sequencing and comparing targeted genomic regions in multiple, evolutionarily diverse vertebrates. Here we report the generation and analysis of over 12 megabases (Mb) of sequence from 12 species, all derived from the genomic region orthologous to a segment of about 1.8 Mb on human chromosome 7 containing ten genes, including the gene mutated in cystic fibrosis. These sequences show conservation reflecting both functional constraints and the neutral mutational events that shaped this genomic region. In particular, we identify substantial numbers of conserved non-coding segments beyond those previously identified experimentally, most of which are not detectable by pair-wise sequence comparisons alone. Analysis of transposable element insertions highlights the variation in genome dynamics among these species and confirms the placement of rodents as a sister group to the primates.     

鲢鱼的同工酶研究

采用聚丙烯酰胺垂直板状连续电泳的方法,对鲢鱼的六种组织进行了十种同工酶的电泳研究,并对各种酶的同工酶位点及酶谱表型进行了分析,其中,鲢鱼的α＿ＡＭＹ和ＰＯＸ以前未见报道。结果表明,除ＧＯＴ外,其余酶均存在不同程度的组织特异性;鲢鱼的酶谱模式表现为总体特征简单化,这可能和鲢鱼种质的衰退有关。     

Theoretical Calculation for the Oscillator Strength of A~3Π-X~3Π Band System of BN Molecule

选用ＳＴＯ４Ｇ双ζ扩展基组,采用单组态自洽场方法计算了分子轨道,然后再作较大规模的组态相互作用计算,得到ＢＮ分子基电子态和第一激发电子态的能量及波函数．两电子态的能量差与实验值相符甚好．在偶极近似下,计算了ＢＮ分子Ａ３ΠＸ３Π带系的振子强度,其值为０．０５６４．     

90年代特大城市发展与流动人口关系探析

以上海为例,通过对流动人口的抽样调查分析,探讨人口流动与特大城市的经济结构及空间扩散效应之间的相关性,以期寻求人口流动与特大城市经济发展之间的内在规律性,为中国特大城市发展和制订人口政策提供参考。     

钢丝绳隔震器三向性能试验研究

对三种类型的钢丝绳隔震器进行了三向性能试验研究,重点研究了钢丝绳隔震器直径比D／d与其三向刚度和阻尼的关系,并研究了不同径向负载对其纵向、横向性能的影响．研究结果表明：钢丝绳隔震器具有三向非线性软化刚度和迟滞阻尼特性,并可简化成双线性迟滞模型,其阻尼比在0．2以上．