Lanthanide Complexes for Tumor Diagnosis and Therapy by Targeting Sialic Acid.

Abstract

Sialic acid (SA) is overexpressed on cell membranes of tumor cells, and increased serum SA concentration has been observed in tumor-bearing patients. Herein, a series of lanthanide-containing bimetallic complexes (TDA-M-Lns) for targeting SA were prepared via coordination among luminescent lanthanide ions (Ln³⁺ = Tb³⁺, Eu³⁺, Dy³⁺, or Sm³⁺), metal ion quenchers (M²⁺ = Cu²⁺ or Co²⁺), and the organic ligand 2,2'-thiodiacetic acid (TDA). SA can competitively coordinate with Ln³⁺, resulting in the "signal-on" of the Ln³⁺. Therefore, the TDA-M-Lns can be simply used for cost-saving detection of SA in the blood samples. Among the TDA-M-Lns, TDA-Co-Eu showed the highest sensitivity to detect SA in the blood of tumor-bearing mice. Furthermore, the TDA-Co-Eu was successfully used to target SA and deposit Eu³⁺ on the surfaces of tumor cells for the inhibition of tumor cell growth and migration. The therapeutic effect of TDA-Co-Eu on a Balb/c mouse liver tumor model was evaluated. It was proved that TDA-Co-Eu can be applied for SA detection as well as for inhibiting tumor growth.