致癌与突变杂志

抽象的

Characterization of ^99mTc-Resveratrol as a Cancer Targeting Radiopharmaceutical: An In Vitro study

Rozy Kamal, Vijayta D Chadha, Sohini Walia and Dhawan DK

Introduction: The present study describes the radio-synthesis, chemical characterization and bio-evaluation of 99mTc-resveratrol as a diagnostic imaging probe in radionuclide imaging of cancer using single photon emission computed tomography (SPECT).
Methods: Resveratrol, a potent chemopreventive natural phytoalexin was labeled with Technetium (99mTc).Radiolabeling efficiency, stability in vitro, cytotoxicity in rat RBCs and in HT29 colon cancer cells along with cellular internalization and binding characteristics were investigated.
Results: The radiochemical purity of synthesized radio-complex, 99mTc-resveratrol was >85%. 99mTcresveratrol was stable upto 2 hours at room temperature between pH ranges 5-7. 99mTc-resveratrol, containing resveratrol up to a concentration of 20 μM was found to be nontoxic to both HT 29 cells and rat blood cells. Binding sites for 99mTc-resveratrol in HT 29 cells were found to be specific to native resveratrol and were concentrated in the cytosolic subcellular fraction of these cells. Cellular internalization of 99mTc-resveratrol was mainly through passive mode however active internalization via macropinocytosis was also observed.
Conclusion: The study, therefore reports the successful radio-synthesis of 99mTc-resveratrol complex, characterized as a stable, non-toxic and a potent cancer targeting probe.