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The Biological Activity Research of the Nano-Drugs Based on 5-Fluorouracil-Modified Quantum Dots

Authors Qiao LL, Yao WJ, Zhang ZQ, Yang X, Zhao MX

Received 3 January 2020

Accepted for publication 1 April 2020

Published 23 April 2020 Volume 2020:15 Pages 2765—2776

DOI https://doi.org/10.2147/IJN.S244693

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Dr Phong A Tran


Lu-Lu Qiao, Wen-Jing Yao, Zhi-Qiang Zhang, Xiaojing Yang, Mei-Xia Zhao

Key Laboratory of Natural Medicine and Immune Engineering of Henan Province, Henan University, Kaifeng 475004, People’s Republic of China

Correspondence: Mei-Xia Zhao
Key Laboratory of Natural Medicine and Immune Engineering of Henan Province, Henan University, Jinming Road, Kaifeng 475004, People’s Republic of China
Email zhaomeixia2011@henu.edu.cn

Purpose: Over the past decades, quantum dots (QDs) have shown the broad application in diverse fields, especially in intracellular probing and drug delivery, due to their high fluorescence intensity, long fluorescence lifetime, strong light-resistant bleaching ability, and strong light stability. Therefore, we explore a kind of therapeutic potential against cancer with fluorescent imaging.
Methods: In the current study, a new type of QDs (QDs@L-Cys-TAEA-5-FUA) capped with L-cysteine (L-Cys) and tris(2-aminoethyl)amine (TAEA) ligands, and conjugated with 5-fluorouracil-1-acetic acid (5-FUA) has been synthesized. Ligands were characterized by electrospray ionization mass spectrometry and H-nuclear magnetic resonance (1H NMR) spectroscopy. The modified QDs were characterized by transmission electron microscopy, ultraviolet and visible spectrophotometry (UV-Vis), and fluorescence microscopy. And the biological activity of modified QDs was explored by using MTT assay with HeLa, SMMC-7721 HepG2, and QSG-7701 cells. The fluorescence imaging of modified QDs was obtained by fluorescence microscope.
Results: The modified QDs are of controllable sizes in the range of 4– 5 nm and they possess strong optical emission properties. UV-Vis and fluorescence spectra demonstrated that the L-Cys-TAEA-5-FUA was successfully incorporated into QD nanoparticles. The MTT results demonstrated that L-Cys-TAEA-5-FUA modified QDs could efficiently inhibit the proliferation of cancer cells as compared to the normal cells, illustrating their antitumor efficacy. The mechanistic studies revealed that the effective internalization of modified QDs inside cancer cells could inhibit their proliferation, through excessive production of intracellular reactive oxygen species, leading to apoptosis process.
Conclusion: The present study suggests that modified QDs can enter cells efficiently and could be employed as therapeutic agents for the treatment of various types of cancers with fluorescent imaging.

Keywords: quantum dots, 5-fluorouracil, nano-drugs, apoptosis, antitumor activity

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