石墨烯量子点通过增加顺铂的细胞摄取和核摄取来增强其抗癌活性。
Graphene quantum dots enhance anticancer activity of cisplatin via increasing its cellular and nuclear uptake.
作者信息
Sui Xin, Luo Chao, Wang Chong, Zhang Fangwei, Zhang Jingyan, Guo Shouwu
机构信息
State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai, P.R. China.
Department of Electronic Engineering, School of Electronic Information and Electrical Engineering, Shanghai Jiao Tong University, Shanghai, P.R. China.
出版信息
Nanomedicine. 2016 Oct;12(7):1997-2006. doi: 10.1016/j.nano.2016.03.010. Epub 2016 Apr 13.
Using assistant reagents to improve the pharmaceutical performance of cisplatin (CDDP) has been one of promising strategies. Owing to their extraordinary properties, graphene quantum dots (GQDs) have shown great potentials in biomedical applications. Here we demonstrate that the combination of GQDs with CDDP can effectively enhance the cytotoxicity, cell cycle arrest, and DNA fragmentation that induced by CDDP. We also found that the GQDs improved the interaction of CDDP with DNA. Combing these results with our previous finding that graphene oxide could enhance the permeability of the cells, we believe GQDs improve the pharmaceutical performance of CDDP via first increasing its cellular uptake through improving the cell permeability, and then reinforcing its interaction with DNA once it is inside cells. The remarkable enhancement to CDDP cellular uptake in CDDP resistant cells further specifies that GQDs can increase chemotherapy efficacy of anticancer drugs that are suboptimal due to the drug resistance.
使用辅助试剂来改善顺铂（CDDP）的药物性能一直是一种很有前景的策略。由于其非凡的特性，石墨烯量子点（GQDs）在生物医学应用中显示出巨大潜力。在此我们证明，GQDs与CDDP的组合可有效增强CDDP诱导的细胞毒性、细胞周期阻滞和DNA片段化。我们还发现GQDs改善了CDDP与DNA的相互作用。将这些结果与我们之前发现的氧化石墨烯可增强细胞通透性相结合，我们认为GQDs通过首先提高细胞通透性来增加其细胞摄取，然后在其进入细胞后加强其与DNA的相互作用，从而改善了CDDP的药物性能。CDDP耐药细胞中CDDP细胞摄取的显著增强进一步表明，GQDs可以提高因耐药性而效果欠佳的抗癌药物的化疗疗效。
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