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.

Purpose: Patients afflicted with dry eye disease (DED) experience significant discomfort. The underlying cause of DED is the excessive accumulation of ROS on the ocular surface. Here, we investigated the nitrogen doped-graphene quantum dots (NGQDs), known for their ROS-scavenging capabilities, as a treatment for DED. Methods: NGQDs were prepared by using citric acid and urea as precursors through hydrothermal method. The antioxidant abilities of NGQDs were evaluated through: scavenging the ROS both extracellular and intracellular, regulating the nuclear factor-erythroid 2-related factor (Nrf2) antioxidant pathway of human corneal epithelial cells (HCECs) and their transcription of inflammation related genes. Furthermore, NGQDs were modified by Arg-Gly-Asp-Ser (RGDS) peptides to obtain RGDS@NGQDs. In vivo, both the NGQDs and RGDS@NGQDs were suspended in 0.1% Pluronic F127 (w/v) and delivered as eye drops in the scopolamine hydrobromide-induced DED mouse model. Preclinical efficacy was compared to the healthy and DPBS treated DED mice. Results: These NGQDs demonstrated pronounced antioxidant properties, efficiently neutralizing free radicals and activating the intracellular Nrf2 pathway. In vitro studies revealed that treatment of H₂O₂-exposed HCECs with NGQDs induced a preservation in cell viability. Additionally, there was a reduction in the transcription of inflammation-associated genes. To prolong the corneal residence time of NGQDs, they were further modified with RGDS peptides and suspended in 0.1% Pluronic F127 (w/v) to create RGDS@NGQDs F127 eye drops. RGDS@NGQDs exhibited superior intracellular antioxidant activity even at low concentrations (10 μg/mL). Subsequent in vivo studies revealed that RGDS@NGQDs F127 eye drops notably mitigated the symptoms of DED mouse model, primarily by reducing ocular ROS levels. Conclusion: Our findings underscore the enhanced antioxidant benefits achieved by modifying GQDs through nitrogen doping and RGDS peptide tethering. Importantly, in a mouse model, our novel eye drops formulation effectively ameliorated DED symptoms, thereby representing a novel therapeutic pathway for DED management.

Arguments regarding the biocompatibility of graphene-based materials (GBMs) have never ceased. Particularly, the genotoxicity (e.g., DNA damage) of GBMs has been considered the greatest risk to healthy cells. Detailed genotoxicity studies of GBMs are necessary and essential. Herein, we present our recent studies on the genotoxicity of most widely used GBMs such as graphene oxide (GO) and the chemically reduced graphene oxide (RGO) toward human retinal pigment epithelium (RPE) cells. The genotoxicity of GO and RGOs against ARPE-19 (a typical RPE cell line) cells was investigated using the alkaline comet assay, the expression level of phosphorylated p53 determined via Western blots, and the release level of reactive oxygen species (ROS). Our results suggested that both GO and RGOs induced ROS-dependent DNA damage. However, the DNA damage was enhanced following the reduction of the saturated C–O bonds in GO, suggesting that surface oxygen-containing groups played essential roles in the reduced genotoxicity of graphene and had the potential possibility to reduce the toxicity of GBMs via chemical modification.

The widespread antibiotic resistance has called for alternative antimicrobial agents. Carbon nanomaterials, especially carbon quantum dots (CQDs), may be promising alternatives due to their desirable physicochemical properties and potential antimicrobial activity, but their antimicrobial mechanism remains to be investigated. In this study, nitrogen-doped carbon quantum dots (N-CQDs) were synthesized to inactivate antibiotic-resistant bacteria and treat bacterial keratitis. N-CQDs synthesized via a facile hydrothermal approach displayed a uniform particle size of less than 10 nm, featuring a graphitic carbon structure and functional groups including -OH and -NH₂. The N-CQDs demonstrated antimicrobial activity against Staphylococcus aureus (S. aureus) and methicillin-resistant S. aureus, which was both dose- and time-dependent, reducing the survival rate to below 1 %. The antimicrobial activity was confirmed by live/dead staining. In in vivo studies, the N-CQDs were more efficient in treating drug-resistant bacterial keratitis and reducing corneal damage compared to the common antibiotic levofloxacin. The N-CQDs were shown to generate intracellular and extracellular ROS, which potentially caused oxidative stress, membrane disruption, and cell death. This antimicrobial mechanism was supported by scanning and transmission electron microscopy, significant regulation of genes related to oxidative stress, and increased protein and lactate dehydrogenase leakage. This study has provided insight into the development, application, and mechanism of N-CQDs in antimicrobial applications.

To deal with tumor microenvironment, chemodynamic therapy has been developed, which uses nanocatalysts simulating peroxidase to convert high concentration hydrogen peroxide into toxic hydroxyl radicals in situ and effectively kills tumor cells.

Ce_1–xO₂:x%Cu²⁺ nanobelts were bioinspired, designed, and fabricated using commercial filter papers as scaffolds by adding Cu(NO₃)₂ in the original sol solution of CeO₂ nanobelts, which display excellent catalyst properties for CO oxidation and photocatalytic activity for organic dyes. Compared with pure CeO₂, CuO belts were synthesized using the same method and the corresponding Ce_0.5O₂:50%Cu²⁺ bulk materials were synthesized without filter paper as scaffolds; the synthesized Ce_1–xO₂:x%Cu²⁺ nanobelts, especially Ce_0.5O₂:50%Cu²⁺ nanobelts, can decrease the reaction temperature of CO to CO₂ at 100 °C with the conversion rate of 100%, much lower than the formerly reported kinds of Ce_1–xO₂:x%Cu²⁺ catalysts. Meanwhile, the synthesized Ce_1–xO₂:x%Cu²⁺ nanobelts also display better photocatalytic activity for organic dyes. All of these results provide useful information for the potential applications of the synthesized Ce_1–xO₂:x%Cu²⁺ nanobelts in catalyst fields.