Protein-Based Delivery Systems for Anticancer Metallodrugs: Structure and Biological Activity of the Oxaliplatin/β-Lactoglobulin Adduct

β-lactoglobulin is the major component of whey. Here, the adduct formed upon the reaction of the protein with oxaliplatin (OXA) has been prepared, structurally characterized by X-ray crystallography and electrospray ionization-mass spectrometry, and evaluated as a cytotoxic agent. The data demonstra...

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Published in:Pharmaceuticals (Basel, Switzerland) Switzerland), 2022-03, Vol.15 (4), p.425
Main Authors: Monti, Daria Maria, Loreto, Domenico, Iacobucci, Ilaria, Ferraro, Giarita, Pratesi, Alessandro, D'Elia, Luigi, Monti, Maria, Merlino, Antonello
Format: Article
Language:English
Subjects:
anticancer
Apoptosis
Cancer
Communication
Cytotoxicity
delivery system
Experiments
Ligands
Mass spectrometry
metallodrug
Molecular weight
protein
protein metalation
Proteins
Scientific imaging
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Summary:β-lactoglobulin is the major component of whey. Here, the adduct formed upon the reaction of the protein with oxaliplatin (OXA) has been prepared, structurally characterized by X-ray crystallography and electrospray ionization-mass spectrometry, and evaluated as a cytotoxic agent. The data demonstrate that OXA rapidly binds β-lactoglobulin via coordination with a Met7 side chain upon release of the oxalate ligand. The adduct is significantly more cytotoxic than the free drug and induces apoptosis in cancer cells. Overall, our results suggest that metallodrug/β-lactoglobulin adducts can be used as anticancer agents and that the protein can be used as a metallodrug delivery system.
ISSN:1424-8247
1424-8247
DOI:10.3390/ph15040425