文献：

Construction of novel multifunctional luminescent nanoparticles based on DNA bridging and their inhibitory effect on tumor growth

文献链接：

作者： 

Qiaobei Pan,Jing Zhang, Xiang Li,cQian Zou, Peng Zhang,Ying Luo and Yi Jin

相关产品：

DSPE-PEG2000-cRGD（二硬脂酰基磷脂酰乙醇胺-聚乙二醇2000-cRGD肽）

原文摘要：

   Cyclic RGD peptide was introduced onto the surface of silver nanoparticle (AgNP)-single strand DNA (ssDNA)-graphene quantum dots (GQDs) (ADG) after coating with a hybrid phospholipid material (ADGDDPC) to be used for antitumor treatment. The Ag and ssDNA content was quantified. The morphology and properties of the nanoparticles were characterized by ultraviolet-visible absorption spectroscopy (UV-VIS), scanning electron microscopy (SEM), transmission electron microscopy (TEM), and atomic force microscopy (AFM). The etching effect of H2O2 on the AgNPs and the cleavage of DNA was observed. The cytotoxicity of the ADG-DDPC was investigated using the cell viability and LDH content. The cell uptake was evaluated by using the fluorescence recovery of the GQDs in the ADG-DDPC. The antitumor effects of ADG-DDPC were also evaluated. The content of the ssDNA was 15.3 mg mL 1. The content of the silver element in AgNPs was 3.75 mg mL 1 and 20.43 mg mL 1 in ADG-DDPC. ADG were distributed uniformly with the GQDs on the surface. After coating with hybrid phospholipid membranes containing DSPE-PEG2000-cRGD, ADG-DDPC was detected with an average size of 25.2 nm with a low IC50 of 209.68 ng mL 1 and showed LDH activity on HeLa cells. A better cellular uptake of ADG-DDPC was observed in HeLa cells, compared with cRGD-unmodified ADG nanoparticles (ADG-DDP), up to 6 and 12 h using the fluorescence recovery of GQDs as a measurement. Compared with ADG-DDP (3.6 mg of silver equivalent per kg body weight), ADG-DDPC at the same dose significantly halted 50.9% of tumor growth with little change to body weights when compared with a PTX Injection (10 mg kg 1). The novel nanoparticles, ADG-DDPC, could target tumor sites to exhibit multifunctional inhibition on tumor growth with little toxicity.

    DSPE-PEG2000-cRGD是一种生物分子修饰的磷脂质聚乙二醇（PEG）共聚物。结合cRGD多肽的纳米颗粒或胶囊可以用于分子成像。环RGD肽在用混合磷脂材料（AgNP）涂层后，被引入银纳米颗粒(单链DNA-单链DNA（ssDNA）-石墨烯量子点（GQDs）（ADG）表面进行用于抗tumour。由于cRGD多肽能够特异性结合tumour细胞的整合素受体，DSPE-PEG2000-cRGD常用于纳米化合物递送系统的构建，以提高化合物对tumour细胞的靶向性和吸收性，具体制备过程如下：

图：ADG-DDP或ADG-DDPC的制备工艺

涂有混合脂膜（ADG-DDPC）的ADG核的合成：

将TCEP（三(2-羧乙基)膦）和的巯基DNA（SH-DNA）在Britton-Robinson缓冲液（BR缓冲液）中孵育。然后，向银纳米粒子（AgNPs）溶液（通过加入BR缓冲液将AgNPs溶液调pH）中加入SH-DNA。将溶液孵育，使DNA吸附到AgNPs上。之后向AgNPs溶液中加入柠檬酸盐缓冲液调节浓度。再孵育，再次向溶液中加入柠檬酸盐缓冲液，达到柠檬酸盐的最终浓度。孵育后，通过离心去除多余DNA，然后用BR缓冲液将剩余的沉淀洗涤。将制备好的AgNP-DNA偶联物分散在BR缓冲液中以供后续使用。然后，将AgNP-DNA重新分散在BR缓冲液中，并加入石墨烯量子点（GQDs）。将溶液在室温下孵育以获得ADG核心。在透析袋中透析去除未吸附的GQDs收集备用。

将含有DOTAP和DSPE-PEG2000-cRGD甲醇的混合磷脂溶液缓慢注射到制备的ADG核中，在水浴中孵育。将磷脂吸附在ADG芯表面，将获得的悬浮液在透析液管中透析，以确保甲醇完全透析。将制备的磷脂纳米颗粒通过激光切割得到ADG-DDPC。

图：表征图

结论：DSPE-PEG2000-cRGD结合了磷脂质、聚乙二醇和靶向多肽的优势特性，在靶向化合物递送和生物成像研究中具有价值。以单链DNA（ssDNA）为“桥梁”，将银纳米粒子（AgNPs）与无poison发光材料石墨烯量子点（GQDs）连接起来，形成一个核心，该核心被无poison的混合磷脂膜包裹，这种膜在体内具有较长的循环时间和tumour靶向能力。