New potential anti-SARS-CoV-2 and anti-cancer therapies of chitosan derivatives and its nanoparticles: Preparation and characterization
Hemat Mostafa Mohamed Hassan; Mansoura I. Mohamed; Azza T. Taher; Sara H. Mahmoud; Ahmed Mostafa; Farag F. Sherbiny; Kandile, Nadia; Mai Ali;
Abstract
Chitosan (CS) is a biopolymer and has reactive amine/hydroxyl groups facilitated its
modifications. The purpose of this study is improvement of (CS) physicochemical properties and
its capabilities as antiviral and antitumor through modification with 1-(2-oxoindolin-3-ylidene)thio
semicarbazide (3A) or 1-(5-fluoro-2-oxoindolin-3-ylidene)thiosemicarbazide (3B) via crosslinking of
poly(ethylene glycol)diglycidylether (PEGDGE) using microwave-assisted as green technique gives
(CS-I) and (CS-II) derivatives. However, (CS) derivatives nanoparticles (CS-I NPs) and (CS-II NPs)
are synthesized via ionic gelation technique using sodium tripolyphosphate (TPP). Structures of
new (CS) derivatives are characterized using different tools. The anticancer, antiviral efficiencies
and molecular docking of (CS) and its derivatives are assayed. (CS) derivatives and its nanoparticlesshow enhancement in cell inhibition toward (HepG-2 and MCF-7) cancer cells in comparison with
(CS). (CS-II NPs) reveals the lowest IC50 values are 92.70 ± 2.64 lg/mL and 12.64 m g/mL against
(HepG-2) cell and SARS-CoV-2 (COVID-19) respectively and the best binding affinity toward cor ona virus protease receptor (PDB ID 6LU7) 5.71 kcal / mol. Furthermore, (CS-I NPs) shows the
lowest cell viability% 14.31 ± 1.48 % and the best binding affinity 9.98 kcal/moL against (MCF 7) cell and receptor (PDB ID 1Z11) respectively. Results of this study demonstrated that (CS)
derivatives and its nanoparticles could be potentially employed for biomedical applications
modifications. The purpose of this study is improvement of (CS) physicochemical properties and
its capabilities as antiviral and antitumor through modification with 1-(2-oxoindolin-3-ylidene)thio
semicarbazide (3A) or 1-(5-fluoro-2-oxoindolin-3-ylidene)thiosemicarbazide (3B) via crosslinking of
poly(ethylene glycol)diglycidylether (PEGDGE) using microwave-assisted as green technique gives
(CS-I) and (CS-II) derivatives. However, (CS) derivatives nanoparticles (CS-I NPs) and (CS-II NPs)
are synthesized via ionic gelation technique using sodium tripolyphosphate (TPP). Structures of
new (CS) derivatives are characterized using different tools. The anticancer, antiviral efficiencies
and molecular docking of (CS) and its derivatives are assayed. (CS) derivatives and its nanoparticlesshow enhancement in cell inhibition toward (HepG-2 and MCF-7) cancer cells in comparison with
(CS). (CS-II NPs) reveals the lowest IC50 values are 92.70 ± 2.64 lg/mL and 12.64 m g/mL against
(HepG-2) cell and SARS-CoV-2 (COVID-19) respectively and the best binding affinity toward cor ona virus protease receptor (PDB ID 6LU7) 5.71 kcal / mol. Furthermore, (CS-I NPs) shows the
lowest cell viability% 14.31 ± 1.48 % and the best binding affinity 9.98 kcal/moL against (MCF 7) cell and receptor (PDB ID 1Z11) respectively. Results of this study demonstrated that (CS)
derivatives and its nanoparticles could be potentially employed for biomedical applications
Other data
| Title | New potential anti-SARS-CoV-2 and anti-cancer therapies of chitosan derivatives and its nanoparticles: Preparation and characterization | Authors | Hemat Mostafa Mohamed Hassan ; Mansoura I. Mohamed; Azza T. Taher; Sara H. Mahmoud; Ahmed Mostafa; Farag F. Sherbiny; Kandile, Nadia ; Mai Ali | Keywords | Chitosan and chitosan NP’s derivatives;COVID-19;Anticancer;Molecular docking | Issue Date | 16-Feb-2023 | Publisher | King Saud University | Journal | Arabian Journal of Chemistry | Volume | 16 | Issue | 5 | Start page | 1 | End page | 15 | DOI | https://doi.org/10.1016/j.arabjc.2023.104676 |
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