The radioactive (103)Pd and (109)Pd palladium bipyridyl-bisphosphonate complexes for radionuclide therapy of bone metastatic tumor cells

用于骨转移肿瘤细胞放射性核素治疗的放射性(103)Pd和(109)Pd钯联吡啶双膦酸盐配合物

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Abstract

Two radioisotopes of palladium, (103)Pd and (109)Pd, are considered promising candidates for therapeutic applications because they emit Auger electrons, which are known for their effectiveness in targeting and destroying cancerous cells. We synthesized complexes of (103)Pd and (109)Pd with two bipyridyl and one alendronate molecule. The complexes demonstrated stability and a strong affinity for the surface of hydroxyapatite grains, the main mineral component of bones. Radioactive complexes show significantly higher cytotoxicity against human prostate (DU 145) and ovarian Her2 positive (SKOV-3) cancer cell lines compared to trastuzumab labeled with the Auger electron emitter (125)I and cisplatin. The biological studies showed that both (103)Pd, a pure Auger electron emitter, and (109)Pd, which emits both beta and Auger electrons, demonstrate high cytotoxicity. Furthermore, it was observed that in the tested complexes, (109m)Ag, a decay product of (109)Pd, was released from the complex following the decay of (109)Pd. In contrast, (103m)Rh, a decay product of (103)Pd, remained within the structure of the complex. The release of (103m)Rh from the (103)Pd complex is inhibited by the presence of delocalized electrons in the aromatic bipyridyl ligand. The concept of using a (109)Pd/(109m)Ag and (103)Pd/(103m)Rh generator encourages further exploration of this treatment strategy.

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