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

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 ChinaCorrespondence: Mei-Xia ZhaoKey Laboratory of Natural Medicine and Immune Engineer...

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Main Authors: Qiao LL, Yao WJ, Zhang ZQ, Yang X, Zhao MX
Format: Article
Language:English
Published: Dove Medical Press 2020-04-01
Series:International Journal of Nanomedicine
Subjects:
Online Access:https://www.dovepress.com/the-biological-activity-research-of-the-nano-drugs-based-on-5-fluorour-peer-reviewed-article-IJN
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author Qiao LL
Yao WJ
Zhang ZQ
Yang X
Zhao MX
author_facet Qiao LL
Yao WJ
Zhang ZQ
Yang X
Zhao MX
author_sort Qiao LL
collection DOAJ
description 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 ChinaCorrespondence: Mei-Xia ZhaoKey Laboratory of Natural Medicine and Immune Engineering of Henan Province, Henan University, Jinming Road, Kaifeng 475004, People’s Republic of ChinaEmail zhaomeixia2011@henu.edu.cnPurpose: 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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spelling doaj.art-23361e01e63a46faa282452e7d171a822022-12-21T20:36:28ZengDove Medical PressInternational Journal of Nanomedicine1178-20132020-04-01Volume 152765277653259The Biological Activity Research of the Nano-Drugs Based on 5-Fluorouracil-Modified Quantum DotsQiao LLYao WJZhang ZQYang XZhao MXLu-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 ChinaCorrespondence: Mei-Xia ZhaoKey Laboratory of Natural Medicine and Immune Engineering of Henan Province, Henan University, Jinming Road, Kaifeng 475004, People’s Republic of ChinaEmail zhaomeixia2011@henu.edu.cnPurpose: 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 activityhttps://www.dovepress.com/the-biological-activity-research-of-the-nano-drugs-based-on-5-fluorour-peer-reviewed-article-IJNquantum dots5-fluorouracilnano drugsapoptosisantitumor activity
spellingShingle Qiao LL
Yao WJ
Zhang ZQ
Yang X
Zhao MX
The Biological Activity Research of the Nano-Drugs Based on 5-Fluorouracil-Modified Quantum Dots
International Journal of Nanomedicine
quantum dots
5-fluorouracil
nano drugs
apoptosis
antitumor activity
title The Biological Activity Research of the Nano-Drugs Based on 5-Fluorouracil-Modified Quantum Dots
title_full The Biological Activity Research of the Nano-Drugs Based on 5-Fluorouracil-Modified Quantum Dots
title_fullStr The Biological Activity Research of the Nano-Drugs Based on 5-Fluorouracil-Modified Quantum Dots
title_full_unstemmed The Biological Activity Research of the Nano-Drugs Based on 5-Fluorouracil-Modified Quantum Dots
title_short The Biological Activity Research of the Nano-Drugs Based on 5-Fluorouracil-Modified Quantum Dots
title_sort biological activity research of the nano drugs based on 5 fluorouracil modified quantum dots
topic quantum dots
5-fluorouracil
nano drugs
apoptosis
antitumor activity
url https://www.dovepress.com/the-biological-activity-research-of-the-nano-drugs-based-on-5-fluorour-peer-reviewed-article-IJN
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