Monti Daria Maria, Loreto Domenico, Iacobucci Ilaria, Ferraro Giarita, Pratesi Alessandro, D'Elia Luigi, Monti Maria, Merlino Antonello
Department of Chemical Sciences, University of Naples Federico II, Complesso Universitario di Monte Sant'Angelo, Via Cintia, 21, 80126 Napoli, Italy.
CEINGE Advanced Biotechnologies s.c.a.r.l., Via G. Salvatore 486, 80145 Napoli, Italy.
Pharmaceuticals (Basel). 2022 Mar 30;15(4):425. doi: 10.3390/ph15040425.
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.
β-乳球蛋白是乳清的主要成分。在此，已制备了该蛋白质与奥沙利铂（OXA）反应形成的加合物，通过X射线晶体学和电喷雾电离质谱对其进行了结构表征，并将其评估为一种细胞毒性剂。数据表明，OXA在草酸盐配体释放后通过与Met7侧链配位迅速结合β-乳球蛋白。该加合物的细胞毒性明显高于游离药物，并能诱导癌细胞凋亡。总体而言，我们的结果表明金属药物/β-乳球蛋白加合物可作为抗癌剂，且该蛋白质可作为金属药物递送系统。
