Key Laboratory of Drug Quality Control and Pharmacovigilance (Ministry of Education), China Pharmaceutical University, Nanjing 210009, China.
Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China.
ACS Nano. 2022 Sep 27;16(9):14827-14837. doi: 10.1021/acsnano.2c05715. Epub 2022 Aug 18.
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 (Ln = Tb, Eu, Dy, or Sm), metal ion quenchers (M = Cu or Co), and the organic ligand 2,2'-thiodiacetic acid (TDA). SA can competitively coordinate with Ln, resulting in the "signal-on" of the Ln. 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 Eu 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.
唾液酸（SA）在肿瘤细胞的细胞膜上过表达，并且在荷瘤患者中观察到血清 SA 浓度增加。在此，通过发光镧系离子（Ln = Tb、Eu、Dy 或 Sm）、金属离子猝灭剂（M = Cu 或 Co）和有机配体 2,2'-硫代二乙酸（TDA）之间的配位，制备了一系列含镧的双金属配合物（TDA-M-Lns）用于靶向 SA。SA 可以与 Ln 竞争配位，从而使 Ln 的“信号开启”。因此，TDA-M-Lns 可用于在血液样本中以节省成本的方式检测 SA。在 TDA-M-Lns 中，TDA-Co-Eu 对检测荷瘤小鼠血液中的 SA 具有最高的灵敏度。此外，TDA-Co-Eu 成功地用于靶向 SA 并在肿瘤细胞表面沉积 Eu 以抑制肿瘤细胞的生长和迁移。评估了 TDA-Co-Eu 对 Balb/c 小鼠肝癌模型的治疗效果。证明 TDA-Co-Eu 可用于 SA 检测以及抑制肿瘤生长。
