Synthesis of 4-substituted-7-chloroquinoline derivatives and preliminary evaluation of their antitumor activity

目的:设计合成一系列4-取代-7-氯喹啉衍生物并测定其抗肿瘤活性。方法:4,7-二氯喹啉通过烃化反应及缩合反应得到目标化合物,并采用MTT法,评价了其对4种体外培养肿瘤细胞的生长抑制作用。结果:大多数化合物具有一定的抑制肿瘤细胞增殖的活性,其中化合物3,5和10A抑制人非小细胞肺癌A549,nCI-H446,HElA细胞生长的作用强于阳性对照,化合物5和10A对于人非小细胞肺癌A549的抑制活性是阳性对照药的4~5倍,明显优于阳性对照。结论:本文合成的该系列部分化合物具有较好的抗肿瘤活性,是潜在的抗肿瘤候选药物。Objective: To design and synthesize a series of 4-substituted-7-chloroquinoline derivatives,and to assay their antitumor activity.Methods: The compounds were synthesized through alkylation and condensation reaction using 4,7-dichloro-quinoline,and the antitumor activities were assayed by MTT.Results: Most synthesized compounds had the property of antiproliferation on tumor cell lines in vitro.It was obvious that the compounds of 3,5 and 10a had stronger effect on the growth of A549,NCI-H446 and Hela cancer cells than the positive control group does,and compounds 5 and 10a also showed 4 ~ 5 times more inhibition effect on the A549 cells than the positive control group in terms of antitumor activity.Conclusion: The series of synthesized compounds exhibit excellent antitumor activities and deserve consideration for potential candidate of antitumor drugs泉州市科技计划重点项目(2013Z35

重组人血管内皮生长抑制因子对人肺腺癌裸鼠移植瘤的放射效应影响

目的:探讨重组人血管内皮抑制因子(recombinant human vascular endothelial growth inhiloitor-192,rhVEGI-192)对人肺腺癌裸鼠移植瘤的放射增敏作用。方法:采用原核表达rhVEGI-192,获得目的蛋白。通过肿瘤倍增时间,计算药物的增敏系数。通过建立人肺腺癌裸鼠移植瘤模型,荷瘤裸鼠随机分为4组:对照组、10Gy、rhVEGI-192、rhVEGI-192+10Gy。采用6MV-X线进行照射,照射剂量为10Gy。获得移植瘤标本,利用免疫印迹法检测移植瘤中VEGF(vascular endothelial growth factor)的表达变化。结果:SDS电泳结果显示,目的蛋白位于22k D左右。10Gy照射时,重组人血管内皮抑制因子的EF(enhancement factor)值为1.5。和空白对照组相比,rhVEGI-192组和10Gy组移植瘤的生长受到抑制(P<0.001),rhVEGI-192+10Gy组移植瘤生长显著抑制(P<0.001),rhVEGI-192+10Gy组移植瘤较10Gy组有明显生长抑制。和空白组相比,rhVEGI-192组VEGF表达减少,而10Gy组VEGF表达变化不明显,rhVEGI-192+10Gy组VEGF表达明显减少。rhVEGI-192+10Gy和rhVEGI-192组相比,VEGF表达减少。结论:rhVEGI-192联合照射能够减少VEGF的表达。这可能是rhVEGI-192的增敏机制之一。中国人民解放军南京军区医学科技创新项目(编号:No.12MA061

Preparation and Properties of MnO_2 /polyaniline Composite

以δ-MnO2为前驱体,通过酸处理后引入苯胺并聚合,得到了MnO2/聚苯胺复合材料。经XRD分析表明,在本研究条件下,经酸处理后的δ-MnO2晶型由δ型转变为α型,而在随后的苯胺引入及其聚合步骤中MnO2晶型均不再改变。以200mA·g-1的电流进行恒电流充放电性能测试,结果显示,MnO2/聚苯胺复合材料的充放电容量达到160.2mA·g-1,与酸处理后得到的α-MnO2接近(160.9mA·g-1),但比前驱体δ-MnO2高(125.8mA·g-1);更为重要的是,MnO2/聚苯胺复合材料与前驱体及酸处理得到的样品相比,其循环性能得到了较大的提高。MnO2 /polyaniline composite was prepared by polymerization of aniline in α-MnO2 from the acid-treating precursor of δ-MnO2. XRD results showed that during acid treatment the precursor of δ-MnO2 was transformed into α-MnO2, and this in α-MnO2 polymorph kept unchanged in the subsequent processes, as intercalation and polymerization of aniline. Comparison of charge-discharge performances among the precursor, its acid-treated form and the final composite, showed that at current density of 200 mA·g-1 the discharge capacity of the composite was 160.2 mA·g-1, which is close to that of the acid-treated material (160.9 mA·g-1) but higher than that of the precursor (125.8 mA·g-1). More important, the MnO2 /polyaniline composite showed a much better cyclic performance than the precursor and its acid-treated form.福建省高新技术重点项目(No2005H071);; 三明市重点科技项目(No2005-G-9

Preparation and properties of MnO2/polyaniline composite

MnO2/polyaniline composite was prepared by polymerization of aniline in alpha-MnO2 from the acid-treating precursor of delta-MnO2. XRD results showed that during acid treatment the precursor of delta-MnO2 was transformed into alpha-MnO2, and this in alpha-MnO2 polymorph kept unchanged in the subsequent processes, as intercalation and polymerization of aniline. Comparison of charge-discharge performances among the precursor, its acid-treated form and the final composite, showed that at current density of 200 mA . g(-1) the discharge capacity of the composite was 160.2 mA.g(-1), which is close to that of the acid-treated material (160.9 mA . g(-1)) but higher than that of the precursor (125.8 mA . g(-1)). More important, the MnO2/polyaniline composite showed a much better cyclic performance than the precursor and its acid-treated form

输电线路工程高塔组立施工技术措施研究

输电线路施工是电力工程建设的重要项目，施工作业所面临的环境条件不同，所适应的技术方法也有所差异。尤其是高塔组立是杆塔施工的重要内容，存在较大的施工难度，现场作业风险系数大，必须要提前综合现场条件做全面分析，科学设计施工方案，预测施工阶段可能会遇到的问题，然后通过技术工艺的控制，来消除影响，达到与设计方案一致的施工效果，为输电线路的高质量建设提供保障。本次总结了以往输电线路工程高塔组立施工的实践经验，并对施工技术做了更进一步的分析，争取可以达到更好的施工效果。</jats:p

物流社会责任公众满意度评价

结合物流社会责任实际状况,构建物流社会责任公众满意度评价体系。该评价体系主要由物流社会责任的公众品牌形象、公众期望、公众质量感知、公众价值感知、公众满意度、公众信任、公众抱怨等组成,通过定性与定量相结合的方法对该评价体系指标进行细化,并对各项参数之间的相互关系进行分析比较,及时发现企业履行物流社会责任中存在的问题,从而为企业更有效地提供物流服务,提升物流社会责任并制定发展战略提供参考依据

论河西走廊地区实施生态保护修复的重要性

河西走廊地区处于北方防沙带功能区的关键位置，目前，正面临着土地沙化、水资源枯竭、生物多样性大幅度降低等严峻的生态问题。文中以位于河西走廊西端的酒泉为例，从生态区位、区域地位、实施山水工程的必要性和意义来论述在河西走廊地区实施山水林田湖草生态保护修复工程的重要性。</jats:p

Distribution characteristics of radium isotopes and their influence factors in the water of Jiaozhou Bay area

2012年4-5月以胶州湾地区为研究地点,分析和研究了该地区地下水、河水、海水中224rA和226rA的分布特征及其影响因素。结果表明,232TH和238u浓度较高的花岗岩地区地下水和河水中224rA和226rA的活度均比其他地区高;受到海水混合的影响,沿岸地区地下水和河水由于水体盐度升高,224rA和226rA从固体颗粒的解吸量增加,从而导致活度较高;受河流输入(溶解态和悬浮颗粒解吸)以及海底地下水排泄(SubMArInE grOundWATEr dISCHArgE,Sgd)影响,胶州湾近岸海水224rA活度相对较高,之后224rA自身衰变以及外海水的混合稀释,使224rA活度分布呈现随着离岸距离增加活度逐渐降低的特点;而226rA活度在胶州湾内则保持一个较高水平,只出现个别226rA低值分布区,主要原因是外海水与陆源淡水的226rA活度较为接近且226rA半衰期较长。Background: The interaction between continental and oceanic process is much intense in coastal region.The terrestrial freshwater mixes with seawater here which leads to the chemical constituents in water undergo rapid change.Purpose: The aim is to analyze and study the distribution characteristics of 224Ra and 226Ra and their influence factors in the water of Jiaozhou Bay area.Methods: The water samples of 224Ra and 226Ra were collected from groundwater, river water and seawater around the Jiaozhou Bay from April to May, 2012.In the laboratory, the activities of 224Ra absorbed on the Mn-fiber were measured through the continuous emanation method.Finally, the Mn-fiber was sealed for more than 7 days, and the activities of 226Ra absorbed on the Mn-fiber were measured through the direct emanation method.Results: The results show that the activities of 224Ra and 226Ra in groundwater and river water are much higher in the granitic area which has higher concentration of 232Th and 238U.Because of mixing with seawater, the salinity of groundwater and river water in coastal region rises which leads to the increasing amounts of 224Ra and 226Ra desorbed from the particles, resulting in higher activities of 224Ra and 226Ra in coastal region.Affected by the input of river(dissolved and desorbed from suspended particles) and submarine groundwater discharge(SGD), the activities of 224Ra and 226Ra are relatively higher in nearshore seawater, then with the decay of 224Ra and mixing dilution effect of the offshore seawater, the activities of 224Ra gradually decrease from nearshore region to the open ocean.The activities of 226Ra in the seawater of Jiaozhou Bay remain high-level values, and there are only a few zones of low 226Ra activities.The main reasons are that the activities of 226Ra from terrestrial freshwater are close to those from offshore seawater and the half-life of 226Ra is very long.Conclusion: The activities of 224Ra and 226Ra in groundwater relate to the rock around Jiaozhou Bay and the water salinity.In addition to rock and water salinity, the activities of 224Ra and 226Ra in river water are also concerned with human activities and the process of groundwater recharge.The activities of 224Ra and 226Ra in seawater depend on the sources and sinks of radium isotopes.国家自然科学基金项目(No.41072174)资