Background: Osteosarcoma is an aggressive bone tumor. It represents the principal
cause of cancer-associated death in children. Considering the recent findings on the role of iron in
cancer, iron chelation has been investigated for its antineoplastic properties in many tumors. Deferasirox
is the most used iron chelator compound and in previous studies showed an anticancer effect
in hematologic and solid malignancies. Eltrombopag is a Thrombopoietin receptor used in
thrombocytopenia that also binds and mobilize iron. It demonstrated an effect on iron overload conditions
and also in contrasting cancer cell proliferation.
Objective: We analyzed the effects of deferasirox and eltrombopag in human osteosarcoma cells in
an attempt to identify other therapeutic approaches for this tumor.
Methods: We cultured and treated with deferasirox and Eltrombopag, alone and in combination,
two human osteosarcoma cell lines, MG63 and 143B. After 72h exposure, we performed RTqPCR,
Western Blotting, Iron Assay and cytofluorimetric assays to evaluate the effect on viability, apoptosis,
cell cycle progression and ROS production.
Results: The iron-chelating properties of the two compounds are also confirmed in osteosarcoma,
but we did not observe any direct effect on tumor progression.
Discussion: We tested deferasirox and eltrombopag, alone and in combination, in human osteosarcoma
cells for the first time and demonstrated that their iron-chelating activity does not influence
biochemical pathways related to cancer progression and maintenance.
Conclusion: Although further investigations on possible effects mediated by cells of the tumor microenvironment
could be of great interest, in vitro iron chelation in osteosarcoma does not impair