Novel liver-specific nitric oxide（NO） releasing drugs with bile acid as both NO carrier and targeting ligand

Novel liver-specific nitric oxide（NO） releasing drugs with bile acid as both the NO carrier and targeting ligand were designed and synthesized by direct nitration of the hydroxyl group in bile acids or the 3-Ohydroxyl alkyl derivatives,with the intact 24-COOH being preserved for hepatocyte specific recognition.Preliminary biological evaluation revealed that oral administrated targeted conjugates could protect mice against acute liver damage induced by acetaminophen or carbon tetrachloride.The nitrate level in the liver significantly increased after oral administration of 1e while nitrate level in the blood did not significantly change.Co-administration of ursodeoxycholic acid（UDCA） significantly antagonized the increase of nitrate in the liver resulted by administration of 1e.     

Fabrication of flame-retardant and smoke-suppressant isocyanate-based polyimide foam modified by silica aerogel thermal insulation and flame protection layers

Because of containing urea groups, flame resistance and smoke releasing behaviors of isocyanate-based polyimide foam (IBPIF) produced using free foaming technology require further improvement. In this work, silica aerogel layers were incorporated into cells of IBPIF through an in situ growth process of silica sol (SS). Compared with silica aerogel particles directly mixed into the foaming slurry, the silica aerogel layers that firmly attached to the pores and surfaces of cells not only provided exceptional thermal insulation and flame protection, but also kept original cellular structure. With increase in ratio of SS mass to IBPIF volume, silica aerogel incorporation dosage was gradually increased. Accompanied by flame resistance was obviously improved and smoke releasing behavior was effectively suppressed. Those were indicated by the improved limiting oxygen index (LOI), decreased heat release rate (HRR), peak of HRR, and specific optical density of smoke (Ds) in trials with pilot flames. Compared with pure IBPIF, when the ratio reached to 5/15 g/cm³, it resulted in LOI increasing from 22.0% to 33.0%, peak of HRR, total smoke production (TSP), and maximum value of Ds decreasing from 174 to 72 kW/m², 1.11 to 0.37 m²/m², 45.90 to 17.45, respectively.     

基于碳点多功能纳米载药体系的制备及pH响应释药性能研究

采用一步微波法成功制备了表面带氨基的荧光纳米碳点CDots, 并通过酰胺化反应将靶向基团叶酸接枝到碳点表面, 成功获得中间产物CDots-FA. 在此基础上, 通过已合成四臂端酰肼基化合物2与抗肿瘤药物阿霉素(DOX)连接, 实现在碳点表面的阿霉素药物分子的化学键合, 最终获得多功能纳米载药体系DOX-CDots-FA. 利用原子力显微镜(AFM)、高分辨透射电镜(HR-TEM)和荧光光谱仪对荧光纳米碳点CDots的性能进行表征, 并通过核磁共振、紫外-可见吸收光谱对DOX-CDots-FA结构、接枝率进行了表征. 同时对纳米载药体系DOX-CDots-FA体外药物释放行为、细胞毒性及细胞摄取成像进行了系统的研究. 结果表明, DOX-CDots-FA具有良好的pH响应性. 叶酸靶向基团能加速DOX-CDots-FA被HeLa (FR+)细胞摄取, 并表现出更强的细胞毒性. 同时细胞摄入成像实验表明, 在叶酸靶向作用下, DOX-CDots-FA通过内吞作用进入HeLa细胞, 随后阿霉素被释放出来并进入细胞核区域, 抑制细胞的生长, 从而实现靶向治疗, 降低毒副作用.     

5-氟尿嘧啶壳聚糖微球的制备及其释药性能

5-氟尿嘧啶壳聚糖微球的制备及其释药性能;药物缓释剂     

基于接触数引导的迭代多组独立分子动力学模拟实现配体-蛋白质结合与解离过程

配体的结合与解离过程在蛋白质实现其生物学功能方面非常关键,因此对这些高度动态过程的研究变得非常重要. 尽管已有实验方法可以确定蛋白质-配体复合物的三维结构,但一般仅可获得静态图片. 随着计算机算力的快速提高以及算法的优化,分子动力学模拟在探索配体的结合与解离过程方面具有诸多优势. 然而,当系统变得足够大时,分子动力学模拟的时间和空间尺度成为了巨大的挑战. 本工作提出了一种研究配体-蛋白质结合与解离的增强采样工具,它基于配体和蛋白质之间形成的接触数来引导迭代多组独立分子动力学模拟. 在腺苷酸激酶的模拟结果中,观测到配体的结合和解离过程,而使用传统分子动力学模拟在同一时间尺度下则无法实现这一过程.     

增韧环氧树脂的动态裂纹扩展研究

本文主要进行了环氧及增韧环氧树脂的断裂韧性及裂纹快速扩展的试验研究。试验过程中采用了ＧＬＣ－１型高速裂纹扩展测试仪来测试裂纹的扩展速度,得到在裂纹扩展过程中裂纹扩展速度曲线。本文结合不同的计算公式及有限元分析方法,讨论了各个确定断裂韧性公式的准确程度,发现传统的静态断裂韧性的分析方法所得到的结果偏大,有一定的危险性,建议使用试验与数值计算相结合的方法;同时还发现增韧不仅可以提高材料的静态和动态断裂性能,而且在裂纹扩展过程中可以起到减缓裂纹扩展的作用     

太湖白鱼和梅鲚的数量增长模型

太湖的主要肉食性鱼类是白鱼,它是捕食梅鲚的主要鱼类.在建立了反映两者相互关系的数学模型后,分析了模型的稳定性、稳健性,通过数值模拟得到了种群数量随时间变化的曲线和相应的轨线,并探讨了捕捞强度、增殖放流对种群数量的影响.     

Synthesis and characterization of novel fluoride‐releasing monomers. II. Dimethacrylates containing bis(aminodiacetic acid) and their ternary zirconium fluoride complexes

Novel dimethacrylate monomers containing bis(aminodiacetic acid) chelating ligands with or without additional hydroxyl groups were synthesized, starting from 2,2‐bis(4‐hydroxy‐3‐methylphenyl)propane. The structures of the monomers were characterized by electrospray mass spectrometry (ESMS), ¹H NMR, and ¹³C NMR. The structures and relative stability of fluoride‐releasing monomers containing one or more ternary zirconium fluoride complex moieties were studied by ESMS. The most stable ternary zirconium fluoride complex was in the form of [LZrF]^?, where H₄L is the monomer containing bis(aminodiacetic acid) without additional hydroxyl groups. The synthesized monomer was photopolymerized with camphorquinone and 1‐phenyl‐1,2‐propane‐dione as initiators and N,N‐dimethylaminoethyl methacrylate as the accelerator. The fluoride release, fluoride recharge, compressive strength, and flexure strength were tested on the experimental dental composite containing 13.7 wt % synthesized monomer and three commercial flowable dental composites. The results showed that the experimental composite has significantly higher fluoride release and recharge capabilities than the commercial flowable composites. The compressive strength was comparable to that of the commercial materials. The water sorption and solubility met the requirement of the ISO Specification 4049. © 2005 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 43: 3153–3166, 2005     

两阶段免费增值商业模式中的定价优化与时序研究

免费增值商业模式在信息产品和服务当中被广泛采用。针对企业首先推出免费产品再推出付费产品以充分利用两种产品推出的时间差来提升消费者学习效应、降低消费者使用成本的情形,本文首先建立两阶段模型,求解给定系统参数情况下的付费版产品最优定价问题并给出解析解,然后通过与企业应用单阶段免费增值模式时的利润进行比较,解析地得到企业选择两阶段模式可获得较高利润的条件,最后在数值计算基础上讨论了学习效应强度对企业利润的影响,和优化学习效应强度以拓展两阶段模式适用范围的问题。本文的研究成果为拟采用免费增值商业模式的企业提供了关于产品最优定价和模式选择的决策支持。     

控藻鲢鱼的捕捞策略

鲢鱼是一种以水中浮游动植物为食的滤食性鱼类,利用鲢鱼控制蓝藻数量是一种有效的纯生物手段.分析蠡湖鲢鱼资源稳定的条件,建立鱼量的基本方程式及利润模型,给出利润与捕捞强度的关系和鱼群数量的变化趋势.最后得到了鲢鱼的放流与回捕策略.