Lanthanide Complexes for Tumor Diagnosis and Therapy by Targeting Sialic Acid

• Published in: ACS nano 2022-09, Vol.16 (9), p.14827-14837
• Main Authors: Wang, Jia-Li, Hu, Xin-Yuan, Han, Cheng-Gang, Hou, Shao-Yuan, Wang, Huai-Song, Zheng, Feng
• Format: Article
• Language: English
• Subjects: Animals; Ions; Lanthanoid Series Elements; Ligands; Luminescence; Mice; N-Acetylneuraminic Acid
• ISSN: 1936-0851; 1936-086X
• DOI: 10.1021/acsnano.2c05715

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.