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Assay Drug Dev Technol ; 18(6): 249-260, 2020.
Article in English | MEDLINE | ID: mdl-32941071

ABSTRACT

The main challenging aspect in the management of tuberculosis (TB) diseases is effective alveolar macrophages targeting. Macrophage mannose receptor plays a predominant role in stimulating immune systems by TB pathogen. Our earlier in silico computational studies revealed that O-stearoyl mannose (OSM) possesses a higher affinity with macrophage mannose receptors. Therefore, keeping this in view, we developed OSM with the association of stearic acid and d-mannose as initial reactants by the esterification process. Preliminary confirmation of reaction was assessed with thin-layer chromatography experimentation, whereas further confirmation followed by in vitro characterization with several analytical experimental tools such as fourier transform near-infrared, differential scanning calorimetry, and electrospray ionization-assisted mass spectrometry confirms the formation of the OSM. This synthesized and well-characterized OSM as a ligand was further incubated with surface-engineered lipid nanoarchitectonics to achieve OSM ligand-engineered lipid nanoarchitectonics and earlier explored for its safety study through hemolysis assay and potential in vitro triggering efficiency in human alveolar macrophages (THP-1 cells) to validate its active targeting efficiency. Graphical Abstract [Figure: see text].


Subject(s)
Lipids/chemistry , Macrophages, Alveolar/drug effects , Mannose/pharmacology , Nanostructures/chemistry , Stearic Acids/pharmacology , Tuberculosis/drug therapy , Humans , Ligands , Mannose/chemical synthesis , Mannose/chemistry , Molecular Structure , Nanotechnology , Stearic Acids/chemical synthesis , Stearic Acids/chemistry
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