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Anticancer Efficacy of Photodynamic Therapy with Lung Cancer-Targeted Nanoparticles
Published on: December 1, 2016
Fighting Non-Small Lung Cancer Cells Using Optimal Functionalization of Targeted Carbon Quantum Dots Derived from
Hanaa Mohammed Elsayed Mohammed El-Brolsy1, Nemany A N Hanafy1, Maged A El-Kemary1
1Nanomedicine Group, Institute of Nanoscience and Nanotechnology, Kafrelsheikh University, Kafrelsheikh 33516, Egypt.
Abstract:
Non-small cell lung cancer (NSCLC) is an important sub-type of lung cancer associated with poor diagnosis and therapy. Innovative multi-functional systems are urgently needed to overcome the invasiveness of NSCLC. Carbon quantum dots (CQDs) derived from natural sources have received interest for their potential in medical bio-imaging due to their unique properties, which are characterized by their water solubility, biocompatibility, simple synthesis, and low cytotoxicity. In the current study, ethylene-diamine doped CQDs enhanced their cytotoxicity (98 ± 0.4%, 97 ± 0.38%, 95.8 ± 0.15%, 86 ± 0.15%, 12.5 ± 0.14%) compared to CQDs alone (99 ± 0.2%, 98 ± 1.7%, 96 ± 0.8%, 93 ± 0.38%, 91 ± 1.3%) at serial concentrations (0.1, 1, 10, 100, 1000 μg/mL). In order to increase their location in a specific tumor site, folic acid was used to raise their functional folate recognition. The apoptotic feature of A549 lung cells exposed to N-CQDs and FA-NCQDs was characterized by a light orange-red color under fluorescence microscopy. Additionally, much nuclear fragmentation and condensation were seen. Flow cytometry results showed that the percentage of cells in late apoptosis and necrosis increased significantly in treated cells to (19.7 ± 0.03%), (27.6 ± 0.06%) compared to untreated cells (4.6 ± 0.02%), (3.5 ± 0.02%), respectively. Additionally, cell cycle arrest showed a strong reduction in cell numbers in the S phase (14 ± 0.9%) compared to untreated cells (29 ± 0.5%). Caspase-3 levels were increased significantly in A549 exposed to N-CQDs (2.67 ± 0.2 ng/mL) and FA-NCQDs (3.43 ± 0.05 ng/mL) compared to untreated cells (0.34 ± 0.04 ng/mL). The functionalization of CQDs derived from natural sources has proven their potential application to fight off non-small lung cancer.
Insights
Ethylene-diamine doped carbon quantum dots (CQDs) show enhanced cytotoxicity against non-small cell lung cancer (NSCLC) cells. Functionalizing CQDs with folic acid improves tumor targeting and cancer cell apoptosis, offering a promising NSCLC therapy.
Area of Science:
- Biomedical Engineering
- Materials Science
- Oncology
Background:
- Non-small cell lung cancer (NSCLC) presents significant diagnostic and therapeutic challenges.
- There is a critical need for innovative, less invasive treatments for NSCLC.
- Carbon quantum dots (CQDs) offer potential due to their biocompatibility, water solubility, and low cytotoxicity.
Purpose of the Study:
- To investigate the efficacy of ethylene-diamine doped CQDs (N-CQDs) and folic acid-conjugated N-CQDs (FA-NCQDs) against NSCLC cells.
- To evaluate the impact of CQD functionalization on cytotoxicity, cellular uptake, and induction of apoptosis in lung cancer cells.
Main Methods:
- Synthesis and characterization of CQDs, N-CQDs, and FA-NCQDs.
- Assessment of cytotoxicity using serial concentrations on A549 lung cancer cells.
- Fluorescence microscopy to observe cellular uptake and morphological changes (apoptosis).
- Flow cytometry to quantify late apoptosis, necrosis, and cell cycle arrest.
- Measurement of Caspase-3 levels as an apoptosis marker.
Main Results:
- N-CQDs demonstrated enhanced cytotoxicity compared to unmodified CQDs.
- FA-NCQDs showed increased cellular localization and induced significant apoptosis and necrosis in A549 cells.
- Flow cytometry revealed increased late apoptosis/necrosis (19.7-27.6%) and cell cycle arrest in the S phase (14%) in treated cells versus controls (4.6-3.5% and 29%, respectively).
- Caspase-3 levels were significantly elevated in cells treated with N-CQDs and FA-NCQDs.
Conclusions:
- Functionalized CQDs derived from natural sources exhibit potent anti-cancer activity against NSCLC.
- FA-NCQDs demonstrate potential for targeted therapy by enhancing tumor site localization and inducing cancer cell death.
- This study highlights the therapeutic promise of functionalized CQDs for combating non-small cell lung cancer.

