功能化石墨烯量子点体内外肿瘤抑制效果评价

Evaluation of the Anti-tumor Effect of Functionalized Graphene Quantum Dots in Vivo and in Vitro

关键词:  功能化  石墨烯量子点  肿瘤细胞抑制  效果评价

Key words:  functionalized  graphene quantum dots  tumor cell inhibition effect  evaluation

摘要:

目的 对前期制备的环肽（cRGD）修饰的、负载多柔比星（doxorubicin，DOX）的石墨烯量子点递药系统（cR-G@D）体内外抑制肿瘤效应进行考察。方法 以U87细胞为模型，采用CCK-8法对cR-G@D等样品的体外细胞毒性进行分析；以α_vβ₃不表达的MCF-7细胞和α_vβ₃过表达的U87细胞为模型，利用共聚焦显微技术进一步分析cR-G@D等样品在细胞内的摄取及成像情况；以Balb/c裸鼠（U87）为实验对象，分别考察cR-G@D等样品光热效应及体内肿瘤抑制情况。结果 细胞毒性结果显示cR-G@D在激光照射条件下有显著的肿瘤细胞抑制作用；细胞摄取试验结果显示在U87细胞中靶向修饰的石墨烯量子点摄取情况要远优于非靶向修饰的石墨烯量子点，而在MCF-7细胞中各测试样品摄取无明显区别；体内试验表明cR-G@D在激光照射下温度随时间推移而增加，cR-G@D与激光照射配合条件下肿瘤生长缓慢。结论 cR-G@D递药系统在激光照射下具有一定的光热效应，在体内外具有一定的肿瘤抑制效果。

Abstract:

OBJECTIVE To investigated the antitumor effect of cRGD modified graphene quantum dot with loading doxorubicin drug delivery system(cR-G@D). METHODS The cytotoxicity of cR-G@D in vitro was analyzed using U87 cells as model by CCK-8 method. Using MCF-7 cells(without αvβ3 expression) and U87 cells(with αvβ3 overexpression) as models, the intracellular uptake and imaging of cR-G@D and other samples were further analyzed by confocal microscopy. Balb/c nude mice(U87) were used to investigate the photothermal effect and tumor inhibition of cR-G@D and other samples in vivo. RESULTS The results of cytotoxicity showed that cR-G@D had a significant inhibitory effect on tumor cells under the condition of laser irradiation. The results of cell uptake assay showed that the uptake of targeted modified graphene quantum dots was much better than that of non-targeted modified graphene quantum dots. There was no significant difference among the tested samples in MCF-7 cells. In vivo experiments showed that the temperature of cR-G@D increased with the passage of time under laser irradiation. The tumor grew slowly under the condition of cR-G@D combined with laser irradiation. CONCLUSION The drug delivery system of cR-G@D have a certain photothermal and tumor inhibitory effect under laser irradiation in vivo and in vitro.