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Increased ROS scavenging and antioxidant efficiency of chlorogenic acid compound delivered via a chitosan nanoparticulate system for efficient in vitro visualization and accumulation in human renal adenocarcinoma cells

Naturally existing Chlorogenic acid (CGA) is an antioxidant-rich compound reported to act a chemopreventive agent by scavenging free radicals and suppressing cancer-causing mechanisms. Conversely, the compound's poor thermal and pH (neutral and basic) stability, poor solubility, and low cellula...

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Main Authors: Rajan, Revathi Kavi, Hussein, Mohd Zobir, Fakurazi, Sharida, Yusoff, Khatijah
Format: Article
Language:English
Published: Multidisciplinary Digital Publishing Institute (MDPI) 2019
Online Access:http://psasir.upm.edu.my/id/eprint/80235/1/Increased%20ROS%20scavenging%20and%20antioxidant%20efficiency%20of%20chlorogenic%20acid%20compound%20delivered%20via%20a%20chitosan%20nanoparticulate%20system%20for%20efficient%20in%20vitro%20visualization%20and%20accumulation%20in%20human%20renal%20adenocarcinoma%20cells.pdf
http://psasir.upm.edu.my/id/eprint/80235/
https://pubmed.ncbi.nlm.nih.gov/31547100/
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spelling my.upm.eprints.802352020-10-18T18:08:24Z http://psasir.upm.edu.my/id/eprint/80235/ Increased ROS scavenging and antioxidant efficiency of chlorogenic acid compound delivered via a chitosan nanoparticulate system for efficient in vitro visualization and accumulation in human renal adenocarcinoma cells Rajan, Revathi Kavi Hussein, Mohd Zobir Fakurazi, Sharida Yusoff, Khatijah Naturally existing Chlorogenic acid (CGA) is an antioxidant-rich compound reported to act a chemopreventive agent by scavenging free radicals and suppressing cancer-causing mechanisms. Conversely, the compound's poor thermal and pH (neutral and basic) stability, poor solubility, and low cellular permeability have been a huge hindrance for it to exhibit its efficacy as a nutraceutical compound. Supposedly, encapsulation of CGA in chitosan nanoparticles (CNP), nano-sized colloidal delivery vector, could possibly assist in enhancing its antioxidant properties, in vitro cellular accumulation, and increase chemopreventive efficacy at a lower concentration. Hence, in this study, a stable, monodispersed, non-toxic CNP synthesized via ionic gelation method at an optimum parameter (600 µL of 0.5 mg/mL of chitosan and 200 µL of 0.7 mg/mL of tripolyphosphate), denoted as CNP°, was used to encapsulate CGA. Sequence of physicochemical analyses and morphological studies were performed to discern the successful formation of the CNP°-CGA hybrid. Antioxidant property (studied via DPPH (1,1-diphenyl-2-picrylhydrazyl) assay), in vitro antiproliferative activity of CNP°-CGA, and in vitro accumulation of fluorescently labeled (FITC) CNP°-CGA in cancer cells were evaluated. Findings revealed that successful formation of CNP°-CGA hybrid was reveled through an increase in particle size 134.44 ± 18.29 nm (polydispersity index (PDI) 0.29 ± 0.03) as compared to empty CNP°, 80.89 ± 5.16 nm (PDI 0.26 ± 0.01) with a maximal of 12.04 μM CGA loaded per unit weight of CNP° using 20 µM of CGA. This result correlated with Fourier-Transform Infrared (FTIR) spectroscopic analysis, transmission Electron Microscopy (TEM) and field emission scanning (FESEM) electron microscopy, and ImageJ evaluation. The scavenging activity of CNP°-CGA (IC50 5.2 ± 0.10 µM) were conserved and slightly higher than CNP° (IC50 6.4±0.78 µM). An enhanced cellular accumulation of fluorescently labeled CNP°-CGA in the human renal cancer cells (786-O) as early as 30 min and increased time-dependently were observed through fluorescent microscopic visualization and flow cytometric assessment. A significant concentration-dependent antiproliferation activity of encapsulated CGA was achieved at IC50 of 16.20 µM as compared to CGA itself (unable to determine from the cell proliferative assay), implying that the competent delivery vector, chitosan nanoparticle, is able to enhance the intracellular accumulation, antiproliferative activity, and antioxidant properties of CGA at lower concentration as compared to CGA alone. Multidisciplinary Digital Publishing Institute (MDPI) 2019 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/80235/1/Increased%20ROS%20scavenging%20and%20antioxidant%20efficiency%20of%20chlorogenic%20acid%20compound%20delivered%20via%20a%20chitosan%20nanoparticulate%20system%20for%20efficient%20in%20vitro%20visualization%20and%20accumulation%20in%20human%20renal%20adenocarcinoma%20cells.pdf Rajan, Revathi Kavi and Hussein, Mohd Zobir and Fakurazi, Sharida and Yusoff, Khatijah (2019) Increased ROS scavenging and antioxidant efficiency of chlorogenic acid compound delivered via a chitosan nanoparticulate system for efficient in vitro visualization and accumulation in human renal adenocarcinoma cells. International Journal of Molecular Sciences, 20 (19). pp. 1-29. ISSN 1422-0067; ESSN: 1661-6596 https://pubmed.ncbi.nlm.nih.gov/31547100/ 10.3390/ijms20194667
institution Universiti Putra Malaysia
building UPM Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Putra Malaysia
content_source UPM Institutional Repository
url_provider http://psasir.upm.edu.my/
language English
description Naturally existing Chlorogenic acid (CGA) is an antioxidant-rich compound reported to act a chemopreventive agent by scavenging free radicals and suppressing cancer-causing mechanisms. Conversely, the compound's poor thermal and pH (neutral and basic) stability, poor solubility, and low cellular permeability have been a huge hindrance for it to exhibit its efficacy as a nutraceutical compound. Supposedly, encapsulation of CGA in chitosan nanoparticles (CNP), nano-sized colloidal delivery vector, could possibly assist in enhancing its antioxidant properties, in vitro cellular accumulation, and increase chemopreventive efficacy at a lower concentration. Hence, in this study, a stable, monodispersed, non-toxic CNP synthesized via ionic gelation method at an optimum parameter (600 µL of 0.5 mg/mL of chitosan and 200 µL of 0.7 mg/mL of tripolyphosphate), denoted as CNP°, was used to encapsulate CGA. Sequence of physicochemical analyses and morphological studies were performed to discern the successful formation of the CNP°-CGA hybrid. Antioxidant property (studied via DPPH (1,1-diphenyl-2-picrylhydrazyl) assay), in vitro antiproliferative activity of CNP°-CGA, and in vitro accumulation of fluorescently labeled (FITC) CNP°-CGA in cancer cells were evaluated. Findings revealed that successful formation of CNP°-CGA hybrid was reveled through an increase in particle size 134.44 ± 18.29 nm (polydispersity index (PDI) 0.29 ± 0.03) as compared to empty CNP°, 80.89 ± 5.16 nm (PDI 0.26 ± 0.01) with a maximal of 12.04 μM CGA loaded per unit weight of CNP° using 20 µM of CGA. This result correlated with Fourier-Transform Infrared (FTIR) spectroscopic analysis, transmission Electron Microscopy (TEM) and field emission scanning (FESEM) electron microscopy, and ImageJ evaluation. The scavenging activity of CNP°-CGA (IC50 5.2 ± 0.10 µM) were conserved and slightly higher than CNP° (IC50 6.4±0.78 µM). An enhanced cellular accumulation of fluorescently labeled CNP°-CGA in the human renal cancer cells (786-O) as early as 30 min and increased time-dependently were observed through fluorescent microscopic visualization and flow cytometric assessment. A significant concentration-dependent antiproliferation activity of encapsulated CGA was achieved at IC50 of 16.20 µM as compared to CGA itself (unable to determine from the cell proliferative assay), implying that the competent delivery vector, chitosan nanoparticle, is able to enhance the intracellular accumulation, antiproliferative activity, and antioxidant properties of CGA at lower concentration as compared to CGA alone.
format Article
author Rajan, Revathi Kavi
Hussein, Mohd Zobir
Fakurazi, Sharida
Yusoff, Khatijah
spellingShingle Rajan, Revathi Kavi
Hussein, Mohd Zobir
Fakurazi, Sharida
Yusoff, Khatijah
Increased ROS scavenging and antioxidant efficiency of chlorogenic acid compound delivered via a chitosan nanoparticulate system for efficient in vitro visualization and accumulation in human renal adenocarcinoma cells
author_facet Rajan, Revathi Kavi
Hussein, Mohd Zobir
Fakurazi, Sharida
Yusoff, Khatijah
author_sort Rajan, Revathi Kavi
title Increased ROS scavenging and antioxidant efficiency of chlorogenic acid compound delivered via a chitosan nanoparticulate system for efficient in vitro visualization and accumulation in human renal adenocarcinoma cells
title_short Increased ROS scavenging and antioxidant efficiency of chlorogenic acid compound delivered via a chitosan nanoparticulate system for efficient in vitro visualization and accumulation in human renal adenocarcinoma cells
title_full Increased ROS scavenging and antioxidant efficiency of chlorogenic acid compound delivered via a chitosan nanoparticulate system for efficient in vitro visualization and accumulation in human renal adenocarcinoma cells
title_fullStr Increased ROS scavenging and antioxidant efficiency of chlorogenic acid compound delivered via a chitosan nanoparticulate system for efficient in vitro visualization and accumulation in human renal adenocarcinoma cells
title_full_unstemmed Increased ROS scavenging and antioxidant efficiency of chlorogenic acid compound delivered via a chitosan nanoparticulate system for efficient in vitro visualization and accumulation in human renal adenocarcinoma cells
title_sort increased ros scavenging and antioxidant efficiency of chlorogenic acid compound delivered via a chitosan nanoparticulate system for efficient in vitro visualization and accumulation in human renal adenocarcinoma cells
publisher Multidisciplinary Digital Publishing Institute (MDPI)
publishDate 2019
url http://psasir.upm.edu.my/id/eprint/80235/1/Increased%20ROS%20scavenging%20and%20antioxidant%20efficiency%20of%20chlorogenic%20acid%20compound%20delivered%20via%20a%20chitosan%20nanoparticulate%20system%20for%20efficient%20in%20vitro%20visualization%20and%20accumulation%20in%20human%20renal%20adenocarcinoma%20cells.pdf
http://psasir.upm.edu.my/id/eprint/80235/
https://pubmed.ncbi.nlm.nih.gov/31547100/
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score 13.211869

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