功能化石墨烯负载冬凌草甲素抗肿瘤制剂的研究

doi:10.6023/cjoc201211033

有机化学 ›› 2013, Vol. 33 ›› Issue (03): 573-580.DOI: 10.6023/cjoc201211033 上一篇下一篇

研究论文

功能化石墨烯负载冬凌草甲素抗肿瘤制剂的研究

徐志远^a,b,c, 李永军^c,d, 史萍^b, 王博婵^b, 黄晓宇^c

a 华东理工大学材料科学与工程学院上海 200237;
b 生物反应器工程国家重点实验室上海 200237;
c 中国科学院上海有机化学研究所上海 200032;
d 聚合物分子工程国家重点实验室(复旦大学) 上海 200043

收稿日期:2012-11-16 修回日期:2012-12-01 发布日期:2012-12-07
通讯作者: 史萍, 黄晓宇 E-mail:ship@ecust.edu.cn; xyhuang@mail.sioc.ac.cn
基金资助:
国家自然科学基金(Nos. 31100549, 21204098)、上海市青年科技启明星跟踪计划(No. 11QH1402800)和上海市生物医药科技重点(No. 10431903000)资助项目.

Functionalized Graphene Oxide as a Nanocarrier for Loading and Delivering of Oridonin

Xu Zhiyuan^a,b,c, Li Yongjun^c,d, Shi Ping^b, Wang Bochan^b, Huang Xiaoyu^c

a School of Materials Science and Engineering, East China University of Science and Technology, Shanghai 200237;
b The State Key Laboratory of Bioreactor Engineering, Shanghai 200237;
c Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032;
d State Key Laboratory of Molecular Engineering of Polymers (Fudan University), Shanghai 200043

Received:2012-11-16 Revised:2012-12-01 Published:2012-12-07
Supported by:
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).

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摘要/Abstract

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.

关键词: 氧化石墨烯, 冬凌草甲素, 药物传输

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 nanocarrier shows higher cytotoxicity in A549 and MCF-7 cells.

Key words: graphene oxide, oridonin, drug delivery

引用此文

徐志远, 李永军, 史萍, 王博婵, 黄晓宇. 功能化石墨烯负载冬凌草甲素抗肿瘤制剂的研究[J]. 有机化学, 2013, 33(03): 573-580.

Xu Zhiyuan, Li Yongjun, Shi Ping, Wang Bochan, Huang Xiaoyu. Functionalized Graphene Oxide as a Nanocarrier for Loading and Delivering of Oridonin[J]. Chin. J. Org. Chem., 2013, 33(03): 573-580.

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功能化石墨烯负载冬凌草甲素抗肿瘤制剂的研究

Functionalized Graphene Oxide as a Nanocarrier for Loading and Delivering of Oridonin

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