以聚酰胺-胺树形分子为模板制备AgI纳米簇

本文以聚酰胺-胺(PAMAM)树形分子为模板,原位制备AgI纳米簇.系统地研究了AgI纳米簇制备过程中各种反应条件如树形分子端基、反应时间、Ag 与PAMAM摩尔比等对AgI纳米簇粒径的影响,分别用紫外-可见光谱、荧光光谱、透射电镜等对所制备的纳米簇进行表征.在相同的条件下,以G4.5-COOH3为模板较以G5.0-NH2为模板制备的AgI纳米簇粒径小、分布均匀,这主要取决于G4.5-COOCH3PAMAM树形分子所起的“内模板”作用.G4·5-COOH3树形分子浓度为1×10-5mol/L,Ag 与树形分子摩尔比为30∶1时所制备的AgI纳米簇的粒径分布均匀、稳定性好,室温避光可稳定存在两个月以上.     

钛合金在汽车轻量化中的应用

以SmCl3为原料，硼氢化钠为还原剂，低代（2．0G3．0G,4．0G）PAMAM树形分子为模板兼稳定剂、制备出纳米颗粒。实验发现，其他条件相同时，树形分子代数越高，所起的模板作用越显著，即Sm／4．0GPAMAM的复合纳米颗粒粒度均匀，分散度好。应用Virtual Materiale（VM）软件对Sm／PAMAM纳米颗粒进行分子动力学模拟。从分子结构和能量变化角度研究了正则（恒定的NVT）系中复合体系的稳定性及其机理。分子动力学模拟结果显示：4．0GPAMAM更适合于作为模板剂和稳定剂，表明动力学模拟结论与实验结果一致。     

PAMAM/PA6共混合金的结晶结构与性能

研究了不同代数和不同份量的PAMAM树形分子对PAMAM／PA6共混合金力学性能的影响，并用DSC、WAXD对PAMAM／PA6共混合金的结晶结构进行了分析．结果表明，PAMAM在低用量时，可提高PAMAM／PA6的结晶速度，使微晶尺寸变大，对共混合金起增塑作用；而在高用量时则对PAMAM／PA6的结晶过程起抑制作用，使微晶尺寸变小，对共混合金起增强作用．     

Improved tumor targetability of Tat-conjugated PAMAM dendrimers as a novel nanosized anti-tumor drug carrier

The generation 4-poly-amidoamine-dendrimers (PAMAM G4 dendrimer, P) was conjugated to Tat peptide (Tat, T), a cell-penetrating peptide, in search of an efficient anti-tumor drug delivery vehicle for cancer therapy. In this study, we synthesized BODIPY-labeled Tat-Conjugated PAMAM dendrimers (BPTs) as a novel nanosized anticancer drug carriers and systemically investigated their biodistribution and the tumor accumulation in Sarcoma 180-bearing mice. In addition, the uptake and the cytotoxicity to S180 cells of BPTs thereof were evaluated. The unmodified dendrimer (BP) showed a soon clearance from the blood stream and nonspecific accumulation in tumor. In contrast, the Tat-modified dendrimer, BPT(64) with appropriate particle size showed a better retention in blood and could be accumulated effectively in tumor tissue via the enhanced permeability and retention (EPR) effect. Moreover, BPTs with a high Tat modification rate was accumulated more effectively in tumor tissue. In vitro experiments, these BPTs displayed low cytotoxicity on S180 cells and high uptake to S180 cells. These findings indicate that the nanoparticulate system on the basis of Tat-conjugated PAMAM dendrimers is safer and effective in the concentration range (below 20?μg/ml) to be used as a carrier of anti-tumor drugs for tumor targeting by intravenous administration.     

Dendrimer as nanocarrier for drug delivery

Dendrimers are novel three dimensional, hyperbranched globular nanopolymeric architectures. Attractive features like nanoscopic size, narrow polydispersity index, excellent control over molecular structure, availability of multiple functional groups at the periphery and cavities in the interior distinguish them amongst the available polymers. Applications of dendrimers in a large variety of fields have been explored. Drug delivery scientists are especially enthusiastic about possible utility of dendrimers as drug delivery tool. Terminal functionalities provide a platform for conjugation of the drug and targeting moieties. In addition, these peripheral functional groups can be employed to tailor-make the properties of dendrimers, enhancing their versatility. The present review highlights the contribution of dendrimers in the field of nanotechnology with intent to aid the researchers in exploring dendrimers in the field of drug delivery.     

二代PAMAM树型高分子的荧光现象及其荧光标记应用

首次发现不含荧光团的二代poly(amido amine) (PAMAM) 树型高分子的荧光现象,研究结果表明在无荧光基团的PAMAM树型高分子中,胺类官能团是产生荧光的关键.不同酸度条件下,生成荧光中心的速度不同,而且荧光的稳定性也不相同.同时发现当反复变换酸碱性时PAMAM树型高分子的荧光强度逐渐变弱.由于低代PAMAM树型高分子的良好生物相容性和低廉价格,其有可能成为新型生物荧光标记物.     

聚氧乙烯链封端的聚酰胺-胺树状聚合物的合成与表征

采用酰氯法,用丙烯酰氯和不同相对分子质量的聚乙二醇为原料,制备出一系列具有丙烯酰端基的聚氧乙烯大单体(PEO-A)。实验证明,较佳的原料摩尔比n(PEG)∶n(CH2CHCOCl)∶n〔(CH3CH2)3N〕=2∶1∶1。然后以聚氧乙烯大单体为端基改性剂,在氮气保护下50℃四氢呋喃溶液中分别与G1.0～G4.0聚酰胺-胺树状聚合物进行Michael加成反应96h,合成出了聚氧乙烯(PEO)链封端的非离子型聚酰胺-胺树状聚合物,并用傅立叶变换红外光谱(FTIR)、核磁共振波谱(1HNMR,13CNMR)对其组成和结构进行了表征。     

Synergistic inhibition of human glioma cell line by temozolomide and PAMAM‐mediated miR‐21i

Temozolomide (TMZ) is a promising chemotherapeutic agent for treating glioblastomas. However, resistance develops quickly and with a high frequency. Efforts to overcome chemoresistance are, therefore, critically needed. In present study, a poly(amidoamine; PAMAM) dendrimer was used as a vector to deliver microRNA‐21 inhibitor (miR‐21i) into U87 cells and the chemosensitivity of the combination effect of miR‐21i and TMZ for glioma therapy was investigated. Flow cytometry analysis showed the uptake efficiency of microRNA‐21 inhibitor after complexation with PAMAM. Real‐time PCR and in situ hybridization indicated that, compared with TMZ or miR‐21i treated cells, cells simultaneously treated with miR‐21i and TMZ showed a remarkable decrease in the microRNA‐21 (miR‐21) level. The transfection of miR‐21i enhanced the chemosensitivity by significantly decreasing the IC50 value of TMZ to glioma cells. Knockdown of miR‐21 promoted the cells' apoptosis, and at the same time, inhibited cell invasion. In conclusion, the combination treatment of glioma cells with TMZ and miR‐21i could yield a synergistic effect in inhibition of human glioma cell line. © 2012 Wiley Periodicals, Inc. J. Appl. Polym. Sci., 2013     

Mechanism of Anticancer Action of Novel Imidazole Platinum(II) Complex Conjugated with G2 PAMAM-OH Dendrimer in Breast Cancer Cells

Transition metal coordination compounds play an important role in the treatment of neoplastic diseases. However, due to their low selectivity and bioavailability, as well as the frequently occurring phenomenon of drug resistance, new chemical compounds that could overcome these phenomena are still being sought. The solution seems to be the synthesis of new metal complexes conjugated with drug carriers, e.g., dendrimers. Numerous literature data have shown that dendrimers improve the bioavailability of the obtained metal complexes, solving the problem of their poor solubility and stability in an aqueous environment and also breaking down inborn and acquired drug resistance. Therefore, the aim of this study was to synthesize a novel imidazole platinum(II) complex conjugated with and without the second-generation PAMAM dendrimer (PtMet2–PAMAM and PtMet2, respectively) and to evaluate its antitumor activity. Cell viability studies indicated that PtMet2–PAMAM exhibited higher cytotoxic activity than PtMet2 in MCF-7 and MDA-MB-231 breast cancer cells at relatively low concentrations. Moreover, our results indicated that PtMet2–PAMAM exerted antiproliferative effects in a zebrafish embryo model. Treatment with PtMet2–PAMAM substantially increased apoptosis in a dose-dependent manner via caspase-9 (intrinsic pathway) and caspase-8 (extrinsic pathway) activation along with pro-apoptotic protein expression modulation. Additionally, we showed that apoptosis can be induced by activating POX, which induces ROS production. Furthermore, our results also clearly showed that the tested compounds trigger autophagy through p38 pathway activation and increase Beclin-1, LC3, AMPK, and mTOR inhibition. The high pro-apoptotic activity and the ability to activate autophagy by the imidazole platinum(II) complex conjugated with a dendrimer may be due to its demonstrated ability to reverse multidrug resistance (MDR) and thereby increase cellular accumulation in breast cancer cells.