99m 99m Tc‐labeled DTPA‐colchicine dimer with improved tumor uptake

摘要

This work reports the synthesis, radiolabeling, and biological studies of 99m Tc‐diethylene triamine pentaacetic acid (DTPA)‐colchicine dimer in tumor‐bearing mice. The novel colchicine dimer was successfully synthesized by conjugation of DTPA to 2 colchicine biomolecules. The ligand could be labeled by 99m Tc in high yield to get 99m Tc‐DTPA‐colchicine dimer, which was hydrophilic and stable at room temperature. Biodistribution and imaging studies in tumor‐bearing mice showed that 99m Tc‐DTPA‐colchicine dimer accumulated in the tumor with improved uptake and retention. The results indicate the need for synthetic modification of the parent colchicine derivative and the 99m Tc‐chelate with a view to improve the tumor‐targeting efficacy and in vivo kinetic profiles.