Evaluation of radioiodinated curcumin for its potential as a tumor-targeting radiopharmaceutical

Abstract

Introduction: Curcumin, a component of the spice turmeric has widely reported anticancer properties in several types of cancer. The differential accumulation and mechanism of its action in normal and cancer cells have proven its potential in targeting tumor. Therefore, it was of interest to label curcumin with a suitable radionuclide and explore its potential for use in nuclear medicine. Materials and Methods: Curcumin was labeled with 125I by iodogen method. The radiochemical purity was analyzed by paper electrophoresis and high-performance liquid chromatography (HPLC) method. Cell binding was carried out in murine lymphoma and melanoma cell lines. Bioevaluation and pharmacokinetics of radioiodinated curcumin was carried out in lymphoma-bearing mice for various time points (1, 3, 24, and 48 h). Results: The efficiency of labeling was >75% and the radiochemical purity postpurification was >95% The maximum uptake (~7% at 2 h, 37°C using 5 × 105 cells) was observed in EL4 cells. Significant tumor uptake in lymphoma-bearing mice was observed at 180 min (3.3 ± 0.76% ID/g). In addition, pharmacokinetics of radioiodinated curcumin is fast, with the majority of the preparation out of the bloodstream in 3 h. Conclusion: The results of these studies suggest that curcumin has the potential for targeting lymphomas, which may be used as diagnostic/therapeutic agent by labeling with other radionuclides.

Keywords

• 125I-curcumin
• anticancer
• curcumin
• lymphoma
• radiopharmaceutical