药学学报, 2014, 49(10): 1457-1465
朱红艳, 朱景平, 谢爱梅, 袁静, 花烨, 张伟. 肿瘤靶向高分子碲化镉量子点复合纳米粒的制备及其表征[J]. 药学学报, 2014, 49(10): 1457-1465.
ZHU Hong-yan, ZHU Jing-ping, XIE Ai-mei, YUAN Jing, HUA Ye, ZHANG Wei. Preparation and characterization of tumor targeted CdTe quantum dots modified with functional polymer[J]. Acta Pharmaceutica Sinica, 2014, 49(10): 1457-1465.

朱红艳, 朱景平, 谢爱梅, 袁静, 花烨, 张伟
南通大学药学院, 江苏 南通 226001
本文采用水热法合成N-乙酰-L-半胱氨酸稳定的碲化镉量子点(CdTe quantum dots,CdTe QDs),采用配体置换的方法制备得到氨基脱氧葡萄糖(2-amino-2-deoxy-D-glucose,DG)、聚乙二醇(polyethylene glycol,PEG)与9聚精氨酸(9-D-arginine,9R)共同修饰的碲化镉量子点(9R/DG-CdTe QDs)。通过紫外、荧光光谱、傅里叶红外光谱、核磁共振氢谱、高效液相-质谱联用、聚丙烯酰胺凝胶电泳和透射电子显微镜等手段对该复合量子点进行表征,并对该复合纳米粒的生物相容性、肿瘤靶向性及穿细胞膜的效果进行考察。结果表明,通过配体置换的方法可以成功构建DG、9R、PEG修饰的CdTe QDs复合纳米粒。TEM结果显示,该纳米粒分散性较好,粒径约为8~10 nm。化学修饰后的CdTe QDs吸收峰从480 nm红移至510 nm,发射峰从627 nm红移至659 nm。通过DG、9R、PEG的修饰还能进一步改善量子点的生物相容性,提高对葡萄糖转运体1高表达的肿瘤细胞的靶向性,增加量子点穿过细胞膜进入细胞浆的作用。
关键词:    量子点      氨基葡萄糖      聚乙二醇      精氨酸      肿瘤     
Preparation and characterization of tumor targeted CdTe quantum dots modified with functional polymer
ZHU Hong-yan, ZHU Jing-ping, XIE Ai-mei, YUAN Jing, HUA Ye, ZHANG Wei
School of Pharmacy, Nantong University, Nantong 226001, China
N-acetyl-L-cysteine (NAC) capped quantum dots (QDs) were synthesized by a hydrothermal method and coated with 2-amino-2-deoxy-D-glucose (DG), polyethylene glycol (PEG), and 9-D-arginine (9R). The optical properties, morphology and structure of 9R/DG-coated CdTe QDs were characterized by ultraviolet-visible spectrometry, fluorescence spectrum, fourier transform infrared (FTIR), proton nuclear magnetic resonance (1H NMR), liquid chromatography-mass spectrometer (LC-MS), sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) and transmission electron micrographs (TEM). Furthermore, the biocompatibility, tumor targeted ability and transmembrane action of 9R/DG-coated CdTe QDs were studied. Results indicated that 9R/DG-coated CdTe QDs was constructed successfully by ligand exchange. The 9R/DG-coated CdTe QDs with the size of 8-10 nm had good dispersity and the absorbance and fluorescence peaks of CdTe QDs after modification were red shifted from 480 nm to 510 nm and 627 nm to 659 nm, respectively. In addition, the CdTe QDs modified by PEG, DG and 9R displayed good biocompatibility, high targeted ability to the cancer cells with glucose transporter type 1 (GLUT1) receptor high expression and obvious transmembrane ability.
Key words:    quantum dot    glucosamine    polyethylene glycol    arginine    neoplasm   
收稿日期: 2014-04-10
基金项目: 国家自然科学青年基金项目(81202467);江苏省青年科学基金项目(BK2012232);江苏省教育厅高校自然科学研究面上项目(11KJB350004);江苏省高校优势学科建设工程资助项目
通讯作者: 张 伟,Tel/Fax:86-513-85051728,E-mail:zhangwntu@163.com
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