文献类型：期刊文献

中文题名：功能化石墨烯负载冬凌草甲素抗肿瘤制剂的研究

英文题名：Functionalized Graphene Oxide as a Nanocarrier for Loading and Delivering of Oridonin

作者：徐志远[1,2,3];李永军[3,4];史萍[2];王博婵[2];黄晓宇[3]

机构：[1]华东理工大学材料科学与工程学院,上海200237;[2]生物反应器工程国家重点实验室,上海200237;[3]中国科学院上海有机化学研究所,上海200032;[4]聚合物分子工程国家重点实验室(复旦大学),上海200043

年份：2013

卷号：33

期号：3

起止页码：573

中文期刊名：有机化学

外文期刊名：Chinese Journal of Organic Chemistry

收录：CSTPCD;;Scopus;WOS:【SCI-EXPANDED(收录号:WOS:000317638500019)】；北大核心:【北大核心2011】；CSCD:【CSCD2013_2014】；

基金：Project supported by the National Natural Science Foundation of China (Nos. 31100549, 21204098), the Shanghai Rising Star Program (No. 11QH1402800), and the Shanghai Scientific and Technological Innovation Project (No. 10431903000).

语种：中文

中文关键词：氧化石墨烯;冬凌草甲素;药物传输

外文关键词：graphene oxide; oridonin; drug delivery

摘要：通过改进的Hummers法制备氧化石墨烯(GO),利用酰胺化反应将端基为氨基的六臂聚乙二醇(PEG)连到氧化石墨烯表面,改善其水溶性和生物相容性.原子力显微镜(AFM)数据表明所制备的GO-PEG尺寸小于250 nm,稳定性试验证明GO-PEG在水和PBS缓冲液中可以很好地分散.利用制备的GO-PEG作为药物载体,通过物理共混的方法负载疏水性抗肿瘤药物——冬凌草甲素.紫外光谱法测得载药率高达105%,远高于一般其他的药物载体.选择肺癌细胞A549和乳腺癌细胞MCF-7对载药体系的细胞毒性进行了研究,结果表明即使在高达100 mg/L的浓度下培养48 h,载体GO-PEG对两种细胞仍然具有很小的毒性(相对细胞存活率>85%),而通过载体负载后冬凌草甲素的疗效有所增强,对细胞具有更大的杀伤作用.
Graphene oxide （GO） was prepared by modified Hummers method firstly. In order to improve its water solubility and biocompatibility, 6-armed PEG was grafted onto GO via an amidation process. The size of GO-PEG was less than 250 nm and stability test indicated excellent dispersibility of GO-PEG in water and PBS buffer. Furthermore, oridonin, a widely used cancer chemotherapy drug, is adsorbed onto GO-PEG via blending. The drug loading ratio was determined to be as high as 105%, which was much higher than other common drug carriers. A549 lung cancer cell and MCF-7 breast cancer cell were chosen to study the cytotoxicity of GO-PEG/oridonin, GO-PEG, and free oridonin. The results demonstrated that GO-PEG did not show obvious toxicity （relative cell viability〉85%）, even cultivated for 48 h at a relatively high concentration of 100 mg/L. Compared to oridonin, the GO-PEG/oridonin nanocarder shows higher cytotoxicity in A549 and MCF-7 cells.