Graphene quantum dots (GQDs) are nano-sized graphene slices. With their small size, lamellar and aromatic-ring structure, GQDs tend to enter into the cell nucleus and interfere with DNA activity. Thus, GQD alone is expected to be an anticancer reagent. Herein, we developed GQDs that suppress the growth of tumor by selectively damaging the DNA of cancer cells. The amine-functionalized GQDs were modified with nucleus targeting TAT peptides (TAT-NGs) and further grafted with cancer-cell-targeting folic acid (FA) modified PEG via disulfide linkage (FAPEG-TNGs). The resulting FAPEG-TNGs exhibited good biocompatibility, nucleus uptake, and cancer cell targeting. They adsorb on DNA via the π–π and electrostatic interactions, which induce the DNA damage, the upregulation of the cell apoptosis related proteins, and the suppression of cancer cell growth, ultimately. This work presents a rational design of GQDs that induce the DNA damage to realize high therapeutic performance, leading to a distinct chemotherapy strategy for targeted tumor therapy.

石墨烯量子点 (GQD) 是纳米级石墨烯切片。由于它们的小尺寸、层状和芳香环结构，GQD 倾向于进入细胞核并干扰 DNA 活性。因此，单独的 GQD 有望成为一种抗癌试剂。在此，我们开发了 GQD，通过选择性破坏癌细胞的 DNA 来抑制肿瘤的生长。胺功能化的 GQDs 用细胞核靶向 TAT 肽 (TAT-NGs) 修饰，并通过二硫键 (FAPEG-TNGs) 进一步嫁接癌细胞靶向叶酸 (FA) 修饰的 PEG。由此产生的 FAPEG-TNG 表现出良好的生物相容性、细胞核摄取和癌细胞靶向性。它们通过π-π和静电相互作用吸附在DNA上，诱导DNA损伤，上调细胞凋亡相关蛋白，抑制癌细胞生长，最终。这项工作提出了一种合理的 GQD 设计，可诱导 DNA 损伤以实现高治疗性能，从而为靶向肿瘤治疗提供独特的化疗策略。