Cargando…

Biocompatibility, Cytotoxicity, Antimicrobial and Epigenetic Effects of Novel Chitosan-Based Quercetin Nanohydrogel in Human Cancer Cells

BACKGROUND: Previous studies have reported that quercetin (Q) has a potential antibacterial and anticancer activity. However, its application is limited by many important factors including high hydrophobicity and low absorption. METHODOLOGY: In the current study, we synthesized and characterized (Pa...

Descripción completa

Detalles Bibliográficos
Autores principales: Abbaszadeh, Saber, Rashidipour, Marzieh, Khosravi, Peyman, Shahryarhesami, Soroosh, Ashrafi, Behnam, Kaviani, Mozhgan, Moradi Sarabi, Mostafa
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7441583/
https://www.ncbi.nlm.nih.gov/pubmed/32884259
http://dx.doi.org/10.2147/IJN.S263013
_version_ 1783573321085878272
author Abbaszadeh, Saber
Rashidipour, Marzieh
Khosravi, Peyman
Shahryarhesami, Soroosh
Ashrafi, Behnam
Kaviani, Mozhgan
Moradi Sarabi, Mostafa
author_facet Abbaszadeh, Saber
Rashidipour, Marzieh
Khosravi, Peyman
Shahryarhesami, Soroosh
Ashrafi, Behnam
Kaviani, Mozhgan
Moradi Sarabi, Mostafa
author_sort Abbaszadeh, Saber
collection PubMed
description BACKGROUND: Previous studies have reported that quercetin (Q) has a potential antibacterial and anticancer activity. However, its application is limited by many important factors including high hydrophobicity and low absorption. METHODOLOGY: In the current study, we synthesized and characterized (Patent) a novel chitosan-based quercetin nanohydrogel (ChiNH/Q). Encapsulation efficiency was confirmed by UV/VIS spectrophotometer. Physicochemical characterization of ChiNH/Q was assessed by PDI, DLS, SEM, FTIR, and XRD. The toxicity of the ChiNH/Q against five strains of the pathogen and HepG2 cells was examined. Moreover, the quantification of ChiNH/Q on genomic global DNA methylation and expression of DNMTs (DNMT1/3A/3B) in HepG2 cancer cells were evaluated by ELISA and real-time PCR, respectively. RESULTS: Under the SEM-based images, the hydrodynamic size of the ChiNH/Q was 743.6 nm. The changes in the PDI were 0.507, and zeta potential was obtained as 12.1 mV for ChiNH/Q. The FTIR peak of ChiNH/Q showed the peak at 627 cm(−1) corresponded to tensile vibrational of NH(2)-groups related to Q, and it is the indication of Q loading in the formulation. Moreover, XRD data have detected the encapsulation of ChiNH/Q. The ChiNH/Q showed a potent antimicrobial inhibitory effect and exerted cytotoxic effects against HepG2 cancer cells with IC(50) values of 100 µg/mL. Moreover, our data have shown that ChiNH/Q effectively reduced (65%) the average expression level of all the three DNMTs (p<0.05) and significantly increased (1.01%) the 5-methylated cytosine (5-mC) levels in HepG2 cells. CONCLUSION: Our results showed for the first time the bioavailability and potentiality of ChiNH/Q as a potent antimicrobial and anticancer agent against cancer cells. Our result provided evidence that ChiNH/Q could effectively reduce cellular DNMT expression levels and increase genomic global DNA methylation in HepG2 cancer cells. Our results suggest a potential clinical application of nanoparticles as antimicrobial and anticancer agents in combination cancer therapy.
format Online
Article
Text
id pubmed-7441583
institution National Center for Biotechnology Information
language English
publishDate 2020
publisher Dove
record_format MEDLINE/PubMed
spelling pubmed-74415832020-09-02 Biocompatibility, Cytotoxicity, Antimicrobial and Epigenetic Effects of Novel Chitosan-Based Quercetin Nanohydrogel in Human Cancer Cells Abbaszadeh, Saber Rashidipour, Marzieh Khosravi, Peyman Shahryarhesami, Soroosh Ashrafi, Behnam Kaviani, Mozhgan Moradi Sarabi, Mostafa Int J Nanomedicine Original Research BACKGROUND: Previous studies have reported that quercetin (Q) has a potential antibacterial and anticancer activity. However, its application is limited by many important factors including high hydrophobicity and low absorption. METHODOLOGY: In the current study, we synthesized and characterized (Patent) a novel chitosan-based quercetin nanohydrogel (ChiNH/Q). Encapsulation efficiency was confirmed by UV/VIS spectrophotometer. Physicochemical characterization of ChiNH/Q was assessed by PDI, DLS, SEM, FTIR, and XRD. The toxicity of the ChiNH/Q against five strains of the pathogen and HepG2 cells was examined. Moreover, the quantification of ChiNH/Q on genomic global DNA methylation and expression of DNMTs (DNMT1/3A/3B) in HepG2 cancer cells were evaluated by ELISA and real-time PCR, respectively. RESULTS: Under the SEM-based images, the hydrodynamic size of the ChiNH/Q was 743.6 nm. The changes in the PDI were 0.507, and zeta potential was obtained as 12.1 mV for ChiNH/Q. The FTIR peak of ChiNH/Q showed the peak at 627 cm(−1) corresponded to tensile vibrational of NH(2)-groups related to Q, and it is the indication of Q loading in the formulation. Moreover, XRD data have detected the encapsulation of ChiNH/Q. The ChiNH/Q showed a potent antimicrobial inhibitory effect and exerted cytotoxic effects against HepG2 cancer cells with IC(50) values of 100 µg/mL. Moreover, our data have shown that ChiNH/Q effectively reduced (65%) the average expression level of all the three DNMTs (p<0.05) and significantly increased (1.01%) the 5-methylated cytosine (5-mC) levels in HepG2 cells. CONCLUSION: Our results showed for the first time the bioavailability and potentiality of ChiNH/Q as a potent antimicrobial and anticancer agent against cancer cells. Our result provided evidence that ChiNH/Q could effectively reduce cellular DNMT expression levels and increase genomic global DNA methylation in HepG2 cancer cells. Our results suggest a potential clinical application of nanoparticles as antimicrobial and anticancer agents in combination cancer therapy. Dove 2020-08-11 /pmc/articles/PMC7441583/ /pubmed/32884259 http://dx.doi.org/10.2147/IJN.S263013 Text en © 2020 Abbaszadeh et al. http://creativecommons.org/licenses/by-nc/3.0/ This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms (https://www.dovepress.com/terms.php).
spellingShingle Original Research
Abbaszadeh, Saber
Rashidipour, Marzieh
Khosravi, Peyman
Shahryarhesami, Soroosh
Ashrafi, Behnam
Kaviani, Mozhgan
Moradi Sarabi, Mostafa
Biocompatibility, Cytotoxicity, Antimicrobial and Epigenetic Effects of Novel Chitosan-Based Quercetin Nanohydrogel in Human Cancer Cells
title Biocompatibility, Cytotoxicity, Antimicrobial and Epigenetic Effects of Novel Chitosan-Based Quercetin Nanohydrogel in Human Cancer Cells
title_full Biocompatibility, Cytotoxicity, Antimicrobial and Epigenetic Effects of Novel Chitosan-Based Quercetin Nanohydrogel in Human Cancer Cells
title_fullStr Biocompatibility, Cytotoxicity, Antimicrobial and Epigenetic Effects of Novel Chitosan-Based Quercetin Nanohydrogel in Human Cancer Cells
title_full_unstemmed Biocompatibility, Cytotoxicity, Antimicrobial and Epigenetic Effects of Novel Chitosan-Based Quercetin Nanohydrogel in Human Cancer Cells
title_short Biocompatibility, Cytotoxicity, Antimicrobial and Epigenetic Effects of Novel Chitosan-Based Quercetin Nanohydrogel in Human Cancer Cells
title_sort biocompatibility, cytotoxicity, antimicrobial and epigenetic effects of novel chitosan-based quercetin nanohydrogel in human cancer cells
topic Original Research
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7441583/
https://www.ncbi.nlm.nih.gov/pubmed/32884259
http://dx.doi.org/10.2147/IJN.S263013
work_keys_str_mv AT abbaszadehsaber biocompatibilitycytotoxicityantimicrobialandepigeneticeffectsofnovelchitosanbasedquercetinnanohydrogelinhumancancercells
AT rashidipourmarzieh biocompatibilitycytotoxicityantimicrobialandepigeneticeffectsofnovelchitosanbasedquercetinnanohydrogelinhumancancercells
AT khosravipeyman biocompatibilitycytotoxicityantimicrobialandepigeneticeffectsofnovelchitosanbasedquercetinnanohydrogelinhumancancercells
AT shahryarhesamisoroosh biocompatibilitycytotoxicityantimicrobialandepigeneticeffectsofnovelchitosanbasedquercetinnanohydrogelinhumancancercells
AT ashrafibehnam biocompatibilitycytotoxicityantimicrobialandepigeneticeffectsofnovelchitosanbasedquercetinnanohydrogelinhumancancercells
AT kavianimozhgan biocompatibilitycytotoxicityantimicrobialandepigeneticeffectsofnovelchitosanbasedquercetinnanohydrogelinhumancancercells
AT moradisarabimostafa biocompatibilitycytotoxicityantimicrobialandepigeneticeffectsofnovelchitosanbasedquercetinnanohydrogelinhumancancercells