Abstract
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.
Highlights
Graphene quantum dots (GQDs) are nano-sized graphene slices
FAPEG-TNGs nanoparticles were developed through the construction of nucleus-targeting TAT peptidemodified GQDs, followed by disulfide bonding with folic acid (FA)-PEG for cancer cell targeting (e.g., HeLa cells rather than L929 cells), and selective cancer killing
targeting TAT peptides (TAT-NGs) were released from FAPEG-TNGs by the high level of intracellular GSH, and the released TAT-NGs entered into the cell nucleus
Summary
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. We developed GQDs that suppress the growth of tumor by selectively damaging the DNA of cancer cells. 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, . 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. The cell nucleus is an important target for chemotherapy drugs (e.g., cisplatin and doxorubicin) to induce the apoptosis of tumor cells through the DNA damage inside the nucleus[2,3]. Due to the lack of specific tumor targeting and the presence of intracellular biological barriers, carrier-free drugs cannot be efficiently and targeting inside the nucleus[4]
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