Enzymatic synthesis of 125/131I labeled 8-hydroxyquinoline glucuronide and in vitro/in vivo evaluation of biological influence

8-OHQ-Glu components were labeled using iodogen method with 125I and 131I. Structural analyses were performed with LC/MS/MS, 1H NMR and 13C-MMR for identify and measure chemical constituents. Results confirmed expected molecular structure. 8-OHQ-Glu could successfully radioiodinated with 125/131I according to iodogen method. 125I-8-OHQ-glucuronide incorporated with human gastrointestinal cancer cells such as Detroit-562 (human pharynx adenocarcinoma) (12.6%), Caco-2 (human colorectal adenocarcinoma) (7.8%), Hutu- 80 (human duodenum intestinal adenocarcinoma) (9.5%) and ACBRI 519 (primary human small intestine epithelial cells) (6.40%). 131I-8-OHQ-Glu was tested in mice bearing subcutaneously implanted Caco-2 colorectal adenocarcinoma cells. The results demonstrated that radioiodinated 8-OHQ-Glu may be promising anticancer prodrug.