Novel types of carborane-carrier hyaluronan derivatives via "click chemistry"

Two new HA derivatives bearing carborane rings were synthesized by click chemistry. The optimal conditions were assessed for the preparation of biocompatible boron carriers, potentially suitable for application in BNCT and capable of targeting the CD44 antigen. The new polymeric samples were characterized by means of NMR-spectroscopy techniques that gave degrees of 17 and 8% for HAAACB and HapACB, respectively. Both HAAACB and HApACB turned out to be nontoxic for colorectal, ovarian and bladder tumor cell lines, to disclose a specific interaction with the CD44 antigen as the native hyaluronan moiety, and to deliver boron-atom concentrations largely sufficient for BNCT therapy when accumulated in cancer cells.     

8-取代黄酮的合成及生理活性研究

设计合成了8-黄酮甲基氮芥和6种8-黄酮甲基多聚异戊二烯胺类化合物, 产物结构经¹H NMR, MS及元素分析确证. 合成的7个化合物与氮芥类抗肿瘤药物美法仑一起对白血病细胞(K562)、中国仓鼠卵巢细胞(CHO)、黑色素瘤细胞(B16)等3种肿瘤细胞进行了初步的体外生理活性测试. 结果表明, 对3种受测细胞, 8-黄酮甲基氮芥的体外活性均与美法仑接近; N,N-二(8-黄酮甲基)香叶基胺则表现出比美法仑更高的体外抗肿瘤活性.     

微波辐射合成N-(2-氯-1-氧-5-吡啶甲基)二甲酰亚胺类化合物和生物活性研究

以二甲酰亚胺钾3a～3g与2-氯-5-氯甲基吡啶的N原子氧化后得到的2-氯-1-氧-5-氯甲基吡啶发生亲核取代反应, 用传统和微波两种方法合成了7种未见文献报到的化合物N-(2-氯-1-氧-5-吡啶甲基)二甲酰亚胺类化合物4a～4g. 对比两种合成方法, 在常压下, 微波辐射作为反应热源具有用时少、环境友好、易纯化和产率高的特点. 这些目标化合物4a～4g的结构经元素分析结果, IR, GC-MS, ¹H NMR, ¹³C NMR确证. 初步的生物活性测定结果表明, N-(2-氯-1-氧-5-吡啶甲基)二甲酰亚胺类部分化合物具有良好的杀虫活性.     

2-(1-苯基-1H-四唑-5-硫基)-N-芳基乙酰胺的合成及其生物活性研究

采用微波法通过2-氯乙酰芳胺与1-苯基-1H-四唑-5-硫醇反应合成了一系列2-(1-苯基-1H-四唑-5-硫基)-N-芳基乙酰胺. 其结构经 IR, ¹H NMR, ¹³C NMR 和元素分析表征. 生物活性实验结果表明, 该类化合物在较低浓度下对油菜籽和小麦的生长表现出良好的促进作用.     

微波诱导下2-芳氧甲基苯并咪唑-1-水杨醛乙酰腙衍生物合成及生物活性研究

在微波辐射条件下, 通过2-芳氧甲基苯并咪唑-1-乙酰肼衍生物与水杨醛进行缩合反应, 合成了10种未见文献报道的2-芳氧甲基苯并咪唑-1-水杨醛乙酰腙衍生物. 它们的结构经元素分析, IR, ¹H NMR和¹³C NMR确证. 初步生物活性试验结果表明该系列化合物对小麦幼苗的生长具有明显的调节作用.     

中国大戟属植物中二萜成分的化学及生物活性

大约有80种大戟属植物广泛分布于我国,并在民间用来治疗皮肤病、水肿、结核或作为泻药和利尿剂使用.本文综述了近20年来中国产大戟属植物中14个骨架类型共150多个二萜类成分的化学研究,包括最近报道的4个具有新骨架的二萜和2个二聚体.中国产大戟属植物中的一些二萜类成分具有抗肿瘤、抗病毒、促进神经生长因子增长、皮肤刺激、致癌以及镇痛安神的活性.本文还就大戟属中二萜类成分可能的生源代谢途径提出了假设,并对该属未来的研究进行了展望.     

Neural Wave Representation in Early Vision

The neural wave representation which describes spatiotemporal information in early vision is proposed in terms of extended Gabor functions in this paper. Its reasonability, completeness and uncertainty in spatiotemporal domains and their frequency domains were investigated. The ranges of these parameters in this representation were estimated on electrophysiological and psychophysical data. We derived the partial differential equations which the neural wave satisfied. The general significance of 3D neural wave representation has been explored.     

Amphiphilic cationic [dendritic poly(L-lysine)]-block-poly(L-lactide)-block-[dendritic poly(L-lysine)]s in aqueous solution: self-aggregation and interaction with DNA as gene delivery carriers

A new series of triblock [dendritic poly(L-lysine)]-block-PLLA-block-[dendritic poly(L-lysine)]s (DL(2) -PLLA-DL(2) ) with PLLA block lengths of 11.5-26.5 and double 2-generation PLL dendrons DL(2) as model cationic amphiphiles were synthesized and characterized. Their CAC, self-aggregation and plasmid DNA binding affinities in pure water and PBS were studied. The PLLA block length dependence of particle size, morphology and ξ potential for organized pDNA/amphiphile polyplex aggregates were examined. Finally, toxicities of these DL(2) -PLLA-DL(2) amphiphiles and their polyplexes were assayed by MTT with HeLa, SMMC-7721 and COS-7 cells, and COS-7 cell luciferase and eGFP gene transfection efficacies with these amphiphiles as the delivery carriers were investigated.     

2,3-位稠杂环喹唑啉酮类化合物的合成研究进展

2,3-位稠环喹唑啉酮类化合物由于具有多种优良的生物和生理活性而广泛应用于药物领域,其合成方法是目前药物研究的热点领域之一.本文主要介绍了包括以2-氨基苯甲酸类化合物、2-氨基苯甲酸甲酯类化合物、靛红酸酐类化合物、喹唑啉酮类化合物等为原料合成2,3-位稠环喹唑啉酮类化合物的方法,并对这些方法进行了简单的评述.     

物像空间位姿表征模型及标定技术研究

从对单目视觉系统的空间定位技术着眼，本文研究了一种利用标准平面镜反射辅助三维空间测量的模型和方法。首先基于摄像机标定的基本原理，以条纹反射检测系统为初始结构，建立应用标准镜测量显示屏的空间位姿的物理模型，然后在对摄像机标定不确定度进行实验标定的基础上，进行了对条纹反射检测系统的三维空间位姿描述和测量。研究结果验证了本文技术方法模型有效、精度较高，扩大了单目视觉系统的测量范围，获得了更加紧凑的物像空间位姿测量系统结构。