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Updated: Aug 12, 2025
Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics
Published on: May 14, 2016
Cancer cells inhibition by cationic carbon dots targeting the cellular nucleus
Jiuyan Chen1, Fang Li2, Jun Gu3
1Department of Chemistry, University of Miami, Coral Gables, FL 33146, USA.
Abstract:
Nucleus targeting is tremendously important in cancer therapy. Cationic carbon dots (CCDs) are potential nanoparticles which might enter cells and penetrate nuclear membranes. Although some CCDs have been investigated in nucleus targeting and applied in nuclear imaging, the CCDs derived from drugs, that are able to target the nucleus, bind with DNA and inhibit the growth of cancer cells have not been reported. In this project, 1, 2, 4, 5-benzenetetramine (Y15, a focal adhesion kinase inhibitor) derived cationic carbon dots (Y15-CDs) were prepared via a hydrothermal approach utilizing Y15, folic acid and 1,2-ethylenediamine as precursors. Based on the structural, optical, and morphologic characterizations, Y15-CDs possess rich amine groups and nitrogen in structure, an excitation-dependent photoluminescence emission, and a small particle size of 2 to 4 nm. The DNA binding experiments conducted through agarose gel electrophoresis, UV-vis absorption, fluorescence emission, and circular dichroism spectroscopies, prove that Y15-CDs might bind with DNA via electrostatic interactions and partially intercalative binding modes. In addition, the cell imaging and cytotoxicity studies in human foreskin fibroblasts (HFF), prostate cancer (PC3) and osteosarcoma cells (U2OS) indicate the nucleus targeting and anticancer abilities of Y15-CDs. Most interestingly, Y15-CDs exhibit a higher cytotoxicity to cancer cells (PC3 and U2OS) than to normal cells (HFF), inferring that Y15-CDs might be potentially applied in cancer therapy.
Insights
Novel drug-derived cationic carbon dots (CCDs) show promise for cancer therapy by targeting cell nuclei. These Y15-carbon dots bind DNA and exhibit selective toxicity towards cancer cells, offering a new avenue for treatment.
Area of Science:
- Nanotechnology
- Biomedical Engineering
- Oncology
Background:
- Nucleus targeting is crucial for effective cancer therapy.
- Cationic carbon dots (CCDs) are nanoparticles with potential for cellular entry and nuclear penetration.
- Drug-derived CCDs for nucleus targeting, DNA binding, and cancer inhibition are underexplored.
Purpose of the Study:
- To synthesize and characterize 1,2,4,5-benzenetetramine (Y15) derived cationic carbon dots (Y15-CDs).
- To investigate the DNA binding capabilities and modes of Y15-CDs.
- To evaluate the nucleus targeting efficacy and anticancer potential of Y15-CDs in vitro.
Main Methods:
- Hydrothermal synthesis of Y15-CDs using Y15, folic acid, and 1,2-ethylenediamine.
- Structural, optical, and morphological characterization of Y15-CDs.
- DNA binding assays (agarose gel electrophoresis, UV-vis, fluorescence, circular dichroism).
- Cellular imaging and cytotoxicity studies in human foreskin fibroblasts (HFF), prostate cancer (PC3), and osteosarcoma cells (U2OS).
Main Results:
- Y15-CDs were successfully synthesized, exhibiting rich amine/nitrogen content, excitation-dependent photoluminescence, and small particle size (2-4 nm).
- Y15-CDs demonstrated DNA binding through electrostatic interactions and partial intercalation.
- Y15-CDs effectively targeted cell nuclei and showed higher cytotoxicity against cancer cells (PC3, U2OS) than normal cells (HFF).
Conclusions:
- Y15-derived cationic carbon dots possess favorable characteristics for nucleus targeting.
- Y15-CDs exhibit DNA binding affinity and anticancer properties.
- These novel Y15-CDs show potential for development as targeted cancer therapeutics.
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