Design, BSA Binding, Stopped-Flow Kinetic, Mechanistic, Molecular Docking, and Biological Evaluation of Hy-droxychloroquine-Based Chitosan Nanoparticles for Enhancing Anticancer Activity in A549 Lung Cancer Cell Line DOI Open Access
Rudi van Eldik,

Fawzia I. Elshami,

Hadeer A. Shereef

et al.

Published: Aug. 2, 2023

The current study describes the preparation of chitosan nanoparticles (CNPs) using hydroxychloroquine (HCQ), widely used in traditional medicine due to its diverse phar-macological and medicinal uses. This work aims combine HCQ drug with CS NPs generate a novel nanocomposite improved characteristics bioavailability. HCQ@CS is roughly shaped like roadways has smooth surface an average size 159.3±7.1 nm, PdI 0.224±0.101, zeta potential +46.6±0.8 mV. To aid development pharmaceutical systems for use cancer therapy, binding mech-anism affinity interaction between BSA were ex-amined stopped-flow, other spectroscopic approaches, supplemented by molecular docking analysis. driven ground-state complex formation that may be accompanied non-radiative energy transfer process, constants indicated NPs-BSA was more stable than HCQ-BSA. stopped-flow analysis demonstrated that, addition increasing affinity, nano formulation NPS changes process open up new routes interaction. Docking experiments verified HCQ-BSA complex, site I on structure, primarily amino acids Thr 578, Gln 579, 525, Tyr 400, Asn 404. Furthermore, nano-formulation not only increased cytotoxicity against A549 lung cell line (IC50 = 28.57±1.72 g/ml) compared (102.21±0.67) g/ml), but also exhibited higher anti-bacterial activity both Gram-positive Gram-negative bacteria when chloramphenicol which agreement constants. developed this offer viable therapy option cancer.

Language: Английский

Design, BSA Binding, Stopped-Flow Kinetic, Mechanistic, Molecular Docking, and Biological Evaluation of Hy-droxychloroquine-Based Chitosan Nanoparticles for Enhancing Anticancer Activity in A549 Lung Cancer Cell Line DOI Open Access
Rudi van Eldik,

Fawzia I. Elshami,

Hadeer A. Shereef

et al.

Published: Aug. 2, 2023

The current study describes the preparation of chitosan nanoparticles (CNPs) using hydroxychloroquine (HCQ), widely used in traditional medicine due to its diverse phar-macological and medicinal uses. This work aims combine HCQ drug with CS NPs generate a novel nanocomposite improved characteristics bioavailability. HCQ@CS is roughly shaped like roadways has smooth surface an average size 159.3±7.1 nm, PdI 0.224±0.101, zeta potential +46.6±0.8 mV. To aid development pharmaceutical systems for use cancer therapy, binding mech-anism affinity interaction between BSA were ex-amined stopped-flow, other spectroscopic approaches, supplemented by molecular docking analysis. driven ground-state complex formation that may be accompanied non-radiative energy transfer process, constants indicated NPs-BSA was more stable than HCQ-BSA. stopped-flow analysis demonstrated that, addition increasing affinity, nano formulation NPS changes process open up new routes interaction. Docking experiments verified HCQ-BSA complex, site I on structure, primarily amino acids Thr 578, Gln 579, 525, Tyr 400, Asn 404. Furthermore, nano-formulation not only increased cytotoxicity against A549 lung cell line (IC50 = 28.57±1.72 g/ml) compared (102.21±0.67) g/ml), but also exhibited higher anti-bacterial activity both Gram-positive Gram-negative bacteria when chloramphenicol which agreement constants. developed this offer viable therapy option cancer.

Language: Английский

Citations

1