端基为肝靶向基团的聚谷氨酸苄酯的合成及表征

本文研究甘草次酸、 甘草酸和胆酸的二胺类衍生物的合成及其引发谷氨酸苄酯-N-羧酸酐的开环聚合, 合成了在端基具有不同肝靶向识别基团的聚谷氨酸苄酯. 该材料可能具有肝细胞主动靶向作用, 为进一步的肝靶向药物控释的研究奠定了基础.     

磁性脂质体的制备及在肿瘤诊断与靶向治疗中的应用进展

磁性脂质体是近年来发展起来的新型靶向制剂,能在外加磁场作用下大量滞留在靶部位.由于磁性脂质体具有良好的生物相容性、无毒、易生物降解,因而被广泛用于肿瘤诊断与靶向治疗等领域.本文作者综述了磁性脂质体的制备方法及其在肿瘤诊断与靶向治疗中的应用进展.     

核酸适配子与核酸适配子制药

近年来,分子靶向性治疗在临床实践中取得了显著的进展,尤其是在肿瘤治疗领域,开启了一个全新的时代.单克隆抗体和小分子靶向抑制剂是其中的两个支柱品种,而在更前期的研究中,一类被称作"化学抗体"的单链核酸分子也引起了人们的关注.这类新型靶向性制剂又被称作"核酸适配子",它们对性质各异的众多靶标分子均具有较高的靶向特异性和亲和性,是分子靶向治疗的新方向.本文针对核酸适配子的技术发展和成药性研究进行了综述.     

肿瘤靶向性高分子纳米载体研究现状与展望

综述了肿瘤靶向性高分子纳米载体在抗肿瘤药物的靶向性输送和控制释放方面的研究进展,并详细介绍了被动肿瘤靶向性、主动靶向性、生物可降解性、pH敏感性、还原敏感性、酶敏感性和温度敏感性高分子纳米载体的研究现状,展望了该研究领域的发展方向.     

DBAH-Tf靶向药物及其对乳腺癌细胞的杀伤作用分析

以转铁蛋白(Tf)为靶向载体,与双氢青蒿素(DHA)化学偶联制备一种新的双氢青蒿素衍生物-转铁蛋白靶向药物.以DHA为原料先合成了12β-对甲酰肼苯基双氢青蒿素(DBAH),并采用紫外、红外、核磁共振及电化学等手段对目标产物的结构进行了表征.利用高碘酸钠氧化Tf的C端的N-糖链上的邻位羟基,其氧化产物和DBAH通过希夫碱偶联合成了DBAH-Tf靶向药物,采用紫外吸收光谱法和电化学方法进行表征.四甲基氮唑蓝法(MTT)分析了DBAH-Tf及DHA对人乳腺癌细胞(MCF-7)和正常乳腺细胞的体外杀伤作用, 结果表明,DBAH-Tf对MCF-7的杀伤作用是正常乳腺癌细胞的286倍,体现出良好的靶向性.     

内质网荧光探针研究进展

内质网作为亚细胞器在哺乳细胞生命活动中发挥重要作用.将内质网可视化,进一步检测其活性物质、微环境及生理过程,对于疾病的诊治具有重要的指导价值.近年来,内质网靶向荧光探针的设计与合成受到了越来越多的关注.当前已报道的内质网靶向荧光探针涵盖了单纯内质网成像、金属离子、小分子物质、大分子物质、微环境等.总结并介绍了近期报道的内质网靶向荧光探针的设计与合成工作,分析了内质网荧光探针在研究细胞生理过程中的应用,并展望了内质网靶向荧光探针的发展趋势.     

核酸适体偶联药物的生物偶联构建技术与应用

核酸适体被称为“化学抗体”, 具有与抗体类似或更加优异的特异性和亲和力, 可以精准地靶向靶蛋白, 与靶蛋白特异性结合. 此外, 核酸适体还具有获取简单、 合成简便、 易于进行化学修饰、 不易变性、 靶标范围广、 免疫原性低及细胞内化快等优点, 已被广泛应用于众多研究领域. 在癌症治疗领域, 核酸适体作为一种优异的靶向识别工具和药物递送载体, 可实现抗肿瘤药物的精准递送. 将核酸适体与药物分子偶联, 可通过核酸适体的靶向作用使药物分子随核酸适体共同进入靶细胞, 实现药物分子在靶细胞内的富集, 进而促进靶细胞的死亡. 近年来, 核酸适体偶联药物已成为癌症靶向治疗的前沿新兴领域, 希望通过该领域的深入研究为癌症靶向治疗领域提供新思路. 本文综合评述了以生物偶联技术构建的核酸适体偶联药物及其应用研究.     

靶向性纳米金探针对宫颈癌细胞的激光扫描共聚焦散射成像

制备了粒径均一的纳米金颗粒, 再对其表面进行叶酸修饰, 制得具有靶向性的纳米金探针. 利用激光扫描共聚焦显微镜(LSCM), 对靶向性纳米金的细胞特异性散射成像进行研究. 实验结果表明, 人宫颈癌细胞(Hela)对纳米金-叶酸的摄取作用强于对纳米金的摄取, 但随着时间的延长, 两者的差别逐渐减小. 表明在适当的时间内纳米金-叶酸探针对宫颈癌细胞具有良好的靶向性.     

表面等离子体子共振传感器用于研究不同材质包裹的磁性纳米粒子性质

利用自行设计组装的以白色发光二极管为光源的表面等离子体子共振传感器实验装置, 检测了不同材质包裹的磁性纳米粒子连接靶向DNA与生物素化DNA探针的结合程度. 结果表明, 与聚苯乙烯磁性微球连接的靶向DNA相比, Fe3O4@SiO2核壳式纳米微球连接的靶向DNA与生物素化的DNA探针结合速率较快, 且其相对标准偏差较小.     

基于海藻酸钠衍生物的肝靶向纳米前药的构建及抗肿瘤活性研究

利用寡聚乙二醇(mOEG)修饰海藻酸钠(ALG), 有效降低了ALG的黏度, 提高了其对疏水性肝靶向配体甘草次酸(GA)的负载量. 结果表明, 靶向材料(GA-ALG-mOEG)的GA负载量为11.8%, 是对照组(GA-ALG)的1.97倍. 在此基础上, 以物理交联的方式引入pH响应的阿霉素前药(DOX-ALG-mOEG), 制备了肝靶向纳米前药(DOX-ALG-mOEG/GA-ALG-mOEG NPs). 细胞实验及抑瘤实验结果表明, 该前药较对照组(DOX-ALG/GA-ALG NPs)具有更高的肝靶向性和药物利用率, 其对肝癌细胞的半致死率浓度(IC₅₀)为58.1 ng/mL, 是对照组(IC₅₀=141.7 ng/mL)的41%; 动物实验结果显示, 该前药的抑瘤率达到了88.4%, 比对照组提高了11.5%.     

利用水相合成的量子点标记木瓜蛋白酶的研究

利用半导体纳米粒子 (也称半导体量子点 ,Quantum Dots,以下简称 QDs)和表面修饰技术制备的半导体荧光探针具有极其优良的光谱特征和光化学稳定性 [1] .自 1 997年以来 ,随着量子点制备技术的不断提高 ,量子点在生物医学方面已有应用 . 1 998年 ,Alivisatos[1] 和 Nie[2 ] 两个研究小组分别将结合了生物分子的 QDs作为荧光探针应用于生物体系 ,开创了纳米粒子应用的新领域 .最近 Nie等 [3 ]在利用量子点编码生物分子的研究中取得了突破性进展 .目前 ,纳米粒子与生物分子的连接以共价键方式相结合最为常见 [1,2 ,4 ,5] ,而且在这些应用中…     

Simple reductant concentration-dependent shape control of polyhedral gold nanoparticles and their plasmonic properties

We report a facile seed-mediated method for the synthesis of monodisperse polyhedral gold nanoparticles, with systematic shape evolution from octahedral to trisoctahedral structures. The control over the particle growth process was achieved simply by changing the concentration of the reductant in the growth solution, in the presence of small spherical seed nanoparticles. By progressively increasing the concentration of the reductant used in the growth solution (ascorbic acid), while keeping the amount and type of added surfactant constant, the morphology of the gold nanoparticles was varied from octahedral to truncated octahedral, cuboctahedral, truncated cubic, cubic, and finally trisoctahedral structures. These nanoparticles were monodisperse in size, possessed similar volumes, and were naturally oriented so that their larger crystal planes were face down on quartz substrates when deposited from the solution. By adjusting the volume of gold seed nanoparticle solution added to a growth solution, the size of the simplest gold nanoparticles (with a highly symmetric cubic morphology) could be tuned from 50 ± 2.1 to 112 ± 11 nm. When other seed nanoparticles were used, the size of the cubic Au nanoparticles reached 169 ± 7.0 nm. The nanoparticle growth mechanism and the plasmonic properties of the resulting polyhedral nanoparticles are discussed in this paper.     

Fabrication of PES-based nanofiltration membrane modified by composite PAA-co-PMMA-g-ZnA nanoparticles

In the current research, nanocomposite polyethersulfone-based nanofiltration membranes were prepared by composite PAA-co-PMMA-g-ZnA nanoparticles. NF membranes were fabricated by phase inversion through casting solution technique. The effect of composite PAA-co-PMMA-g-ZnA nanoparticles concentration into the casting solution on physicochemical characteristics of membrane was studied. Scanning optical microscopy images showed uniform particle distribution for the membranes. Scanning electron microscopy images also demonstrated that membrane porosity was enhanced by increase in nanoparticles content ratio. The membrane surface 3D images showed smooth surface for the membranes filled with 0.05, 0.1 and 0.5 wt% nanoparticles. The contact angle results exhibited that membrane hydrophilicity was improved significantly by using of NPs in membrane matrix. The contact angle was decreased from 65.38° for PES membrane to 48.33° for membrane filled with 0.5 wt% nanoparticles. The water permeability was reduced initially by addition of 0.05 wt% nanoparticles into the casting solution and then increased by more nanoparticles loading rate (0.1 wt%). The water permeability was decreased again by more increase in nanoparticles loading range from 0.5 to 1 wt%. The salt rejection was improved strongly from 68.4 % for PES to 88.58 % for membrane filled with 0.5 wt% nanoparticles. The membranes mechanical strength was increased sharply from 2835.5 to 3337.3 kPa with addition of nanoparticles into the casting solution.     

纳米银对表面吸附镝配合物的荧光增强效应研究

研究了不同粒径的纳米银对镝配合物(乙二胺四乙酸配合物)的光谱学性质影响。当配合物溶液的pH值范围为4.0～6.0时,加入纳米银,可观察到大量的纳米银聚集体形成,而在吸收光谱的长波处出现一个新的吸收峰,随着纳米银浓度的增加,该吸收峰逐渐红移,同时,镝配合物的荧光强度增强。实验结果表明,纳米银粒子对镝配合物的荧光增强效应及荧光增强因子与纳米银粒子的浓度和粒径密切相关。随着纳米银浓度的增加,配合物的荧光强度先增强而后又逐渐降低。小粒径的纳米银对镝配合物的荧光增强因子较小。本文从纳米银粒子的聚集效应、局部电磁场增强效应及光吸收效应等方面探讨了纳米银对表面吸附镝配合物的+荧光增强效应机理。     

Synthesis of metallic copper nanoparticles coated with polypyrrole

This paper describes a method for polypyrrole (PPy) coating of metallic Cu nanoparticles in aqueous solution in atmosphere. Colloid solution of Cu nanoparticles was prepared by reducing Cu ions with the use of hydrazine in an aqueous solution dissolving citric acid and cetyltrimethylammonium bromide as stabilizers. The PPy coating was performed by polymerizing pyrrole with the use of hydrogen peroxide as an initiator in an aqueous colloid solution of the Cu nanoparticles. Ultraviolet–visible extinction measurements, transmission electron microscopy observation, and X-ray diffraction measurements revealed that the metallic Cu nanoparticles with a size of 27.6 ± 11.1 nm were coated with PPy. The obtained PPy-coated Cu particles were chemically stable even in atmosphere.     

Fluorescent organic nanoparticles self-assembled from hexa[p-(carbonyl glycin methyl ester) phenoxy] cyclotriphosphazene in solution

Novel organic nanoparticles self-assembled from the hexa[p-(carbonyl glycin methyl ester) phenoxy] cyclotriphosphazene (HGPCP) were prepared by a simple solution method. The as-prepared nanoparticles were extensively characterized by SEM, TEM, XRD, TGA, and fluorescence spectrum. The size of nanoparticles was increased with increasing the HGPCP concentration in solution. The effect of reaction conditions on the particle size and stability was further investigated. Based upon the experimental results, a growth mechanism was proposed for the formation of the nanoparticles. The obtained nanoparticles were highly thermal stable and exhibited strong fluorescent emission, which could be potential candidates for drug-loading carriers and tracer drug delivery.     

水溶液中Mn2+对硫化锌纳米粒子形貌的调控作用

利用硫代乙酰胺在水溶液中缓慢释放的S2-与Zn2+反应制备了ZnS纳米颗粒,ZnS纳米颗粒沉积吸附在3-磺酸基丙基三甲氧基硅烷自组装单层膜上。 实验发现,溶液中添加少量Mn2+,可以显著影响ZnS纳米颗粒的形貌,对ZnS纳米晶的生长方向也有重要影响。 EDS和XRD谱证实Mn2+并没有掺杂到纳米颗粒中去。 这为纳米粒子形貌的调控提供了新途径。 并对ZnS的形成过程进行了探讨,并提出了可能的影响纳米材料形貌的机制。     

Pre-concentration of trace amounts of manganese in water samples based on (1-(2-pyridylazo)-2-naphthol) modified magnetic nanoparticles

A simple procedure based on magnetic nanoparticles has been developed for analytical purposes. In this method, 1-(2-pyridylazo)-2-naphthol (PAN)-modified magnetic nanoparticles (MNPs) were used for separation and pre-concentration of manganese(II) ions from aqueous samples. This method combines the use of a solution solvent with separation of magnetic nanoparticles from sample solution using a magnet. The influence of different parameters, such as amount of extractant (PAN) loaded on the nanoparticles, pH of solution, adsorption time, amount of modified nanoparticle, type and amount of eluents for desorption of manganese from magnetic nanoparticles were evaluated. The effect of various cationic and anionic interferences on the percentage recovery of manganese was also studied. Manganese ions were adsorped from a solution at pH 9.5 and desorbed from nanoparticles with 10?mL of DMSO?:?HNO₃ (1?:?1, v/v). The detection limit of the proposed method was found to be 0.11?µg?L^?1. The method was employed to recover and determine the level of manganese in different water samples.     

Ultrasonic Synthesis of Gold Nanoparticles and Its Use in Immunochromatographic Assay for Detection of Kanamycin

An ultrasonic method to synthesize gold nanoparticles with uniform size was reported. Effects of ethanol concentration, solution pH, ultrasonic irradiation power, and time on the formation of gold nanoparticles were investigated. The obtained gold nanoparticles were characterized by ultraviolet-visible (UV-vis) absorption spectra and scanning electron microscope (SEM). The method performed in ethanol solution under ultrasonic irradiation is friendly to the environment. Furthermore, a nanogold-labeled probe was used to develop an immunochromatographic method for detection of kanamycin.     

Analysis of peptides and proteins affinity-bound to iron oxide nanoparticles by MALDI MS

Iron oxide nanoparticles modified with oleate have been employed for the extraction of peptides and proteins from aqueous solution before matrix-assisted laser desorption/ionization (MALDI) mass spectrometric (MS) analysis. Adsorption of peptides and proteins onto the nanoparticles were mainly through electrostatic attraction and hydrophobic interaction. The analyte-adsorbed iron oxide nanoparticles could be efficiently collected from solution using a magnet. No elution step was needed. With this preconcentration strategy, the lowest detectable concentration of angiotensin I, insulin, and myoglobin in 500 microL of aqueous solution were 0.1 nM, 0.1 nM, and 10.0 nM, respectively. In addition, the nanoparticles could extract the analytes from solution with a high content of salt and surfactant, thus eliminating suppression effect during MALDI MS analysis. This method was successfully applied to concentrate the tryptic digest products of cytochrome c. In addition, the tryptic digestion of cytochrome c can be directly conducted on the iron oxide nanoparticles.