In vivo Study of Chalcone Loaded Carbon Dots for Enhancement of Anticancer and Bioimaging Potencies.

The fluorescent imaging and drug delivery utilizing carbon dots nanomaterials (CDs) have attracted tremendously due to their unique optical ability and outstanding biocompatibility. Herein, we reported a new design of chalcone-loaded carbon dots (Chalcone-APBA-CDs) to serve chalcone transport onto cancer cells and enhance the CDs bioimaging and antitumor activity. The boronic acid was directly introduced to carbon dots (CDs) via pyrolysis process to drive CDs specifically to the cancer cell, and chalcone was mediated on CDs by ultrasonication to perform facile release of the drug delivery model. The successfully synthesized Chalcone-APBA-CDs were proved by their chemical structure, fluorescent activities, in vitro and in vivo analyses, and drug release systems using different pH. In addition, flow cytometry and confocal fluorescent imaging proved CDs' cellular uptake and imaging performance. In vitro analyses further proved that the Chalcone-APBA-CDs exhibited a higher toxicity value than bare CDs and efficiently inhibited the proliferation of the HeLa cells depending on their dose-response. Finally, the performance of Chalcone-APBA-CDs on cancer healing capability was examined in vivo with fibrosarcoma cancer-bearing mice, which showed a remarkable ability to reduce the tumor volume compared with saline (control). This result strongly suggested that the Chalcone-APBA-CDs appear promising simultaneously as cancer cell imaging and drug delivery.

A Perspective on Using Organic Molecules Composing Carbon Dots for Cancer Treatment.

Fluorescent Carbon dots (CDs) derived from biologically active sources have shown enhanced activities compared to their precursors. With their prominent potentiality, these small-sized (<10nm) nanomaterials could be easily synthesized from organic sources either by bottom-up or green approach. Their sources could influence the functional groups present on the CDs surfaces. A crude source of organic molecules has been used to develop fluorescent CDs. In addition, pure organic molecules were also valuable in developing practical CDs. Physiologically responsive interaction of CDs with various cellular receptors is possible due to the robust functionalization on their surface. In this review, we studied various literatures from the past ten years that reported the potential application of carbon dots as alternatives in cancer chemotherapy. The selective cytotoxic nature of some of the CDs towards cancer cell lines suggests the role of surface functional groups towards selective interaction, which results in over-expressed proteins characteristic of cancer cell lines. It could be inferred that cheaply sourced CDs could selectively bind to overexpressed proteins in cancer cells with the ultimate effect of cell death induced by apoptosis. In most cases, CDs-induced apoptosis directly or indirectly follows the mitochondrial pathway. Therefore, these nanosized CDs could serve as alternatives to the current kinds of cancer treatments that are expensive and have numerous side effects.

Boronic-Acid-Modified Nanomaterials for Biomedical Applications.

Boronic-acid-modified nanomaterials have inspired significant research interest owing to their unique biocompatibility and excellent reversible interaction with diol groups containing saccharides, protein, DNA, and other related glucose compounds. However, the different sources and methods change the application of nanomaterials. Thus, surface-functionalized nanomaterials are of interest as one of the best ways to improve the application of the biomedical field. In this mini-review, we summarize recent studies on boronic-acid-modified nanomaterials, based on the carbon dot group and graphene oxides, which have been used in the fields of bioimaging, biosensing, antiviral inhibitors, etc. Moreover, the multivalent interaction on boronic-acid-modified materials has become the main key improvement for targeting treatment in the future. We mainly focused on any previously reported papers for synergistic future opportunities of superior biomedical applications of carbon dots (CDs) in the management and diagnostics of nanomedicine fields.

Comparison Direct Synthesis of Hyaluronic Acid-Based Carbon Nanodots as Dual Active Targeting and Imaging of HeLa Cancer Cells.

The present study explores the potential of carbon nanodots (CDs) synthesized from hyaluronic acid using microwave-assisted and furnace-assisted methods as bioimaging agents for cancer cells. The investigation on the effect of microwave-assisted and furnace-assisted times (2 min and 2 h) on determining CD character is dominantly discussed. Various CDs, such as HA-P1 and HA-P2 were, respectively, synthesized through the furnace-assisted method at 270 °C for 2 min and 2 h, whereas HA-M1 and HA-M2 were synthesized with the microwave-assisted method for 2 min and 2 h, respectively. Overall, various CDs were produced with an average diameter, with the maximum absorption of HA-P1, HA-P2, HA-M1, and HA-M2 at 234, 238, 221, and 217 nm, respectively. The photoluminescence spectra of these CDs showed particular emissions at 320 nm and excitation wavelengths from 340 to 400 nm. Several characterizations such as X-ray photoelectron spectroscopy, Fourier-transform infrared spectroscopy, X-ray diffraction, and Raman spectroscopy reveal the CD properties such as amorphous structures, existence of D bands and G bands, and hydrophilic property supported with hydroxyl and carboxyl groups. The quantum yields of HA-M1, HA-M2, HA-P1, and HA-P2 were 12, 7, 9, and 23%, respectively. The cytotoxicity and in vitro activity were verified by a cell counting kit-8 assay and confocal laser scanning microscopy, which show a low toxicity with the percentage of living cells above 80%.

Inactivation of HIV-1 Infection through Integrative Blocking with Amino Phenylboronic Acid Attributed Carbon Dots.

Current antiretroviral HIV therapies continue to have problems related to procedural complications, toxicity, and uncontrolled side effects. In this study, amino phenylboronic acid-modified carbon dots (APBA-CDs) were introduced as a new nanoparticle-based on gp120 targeting that inhibits HIV-1 entry processes. Prolonged by simple pyrolysis for preparing carbon dots, this report further explores attributing amino phenylboronic acid on carbon dots, which prove the formation of graphene-like structures on carbon dots and boronic acid sites, thereby enabling the enhancement of positive optical properties through photoluminescent detection. Aside from performing well in terms of biocompatibility and low cytotoxicity (the CC50 reach up to 11.2 mg/mL), APBA-CDs exhibited superior capabilities in terms of prohibiting HIV-1 entry onto targeted MOLT-4 cells recognized by the delimitations of syncitia formation and higher ATP signal rather than bare carbon dots. The modified carbon dots also promote dual-action on HIV-1 treatment by both intracellularly and extracellularly viral blocking by combining with the Duviral drug, along with compressing p24 antigen signals that are better than APBA-CDs and Duviral itself.