Characterization of 99mTc-Resveratrol as a Cancer Targeting Radiopharmaceutical: An In Vitro study
| Autor: | Sohini Walia, Rozy Kamal, Vijayta Dani Chadha, D. K. Dhawan |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
endocrine system diseases media_common.quotation_subject Resveratrol Bioinformatics 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine medicine Internalization Cytotoxicity media_common chemistry.chemical_classification business.industry organic chemicals Phytoalexin Pinocytosis Cancer medicine.disease In vitro Cytosol 030104 developmental biology chemistry 030220 oncology & carcinogenesis Biophysics business |
| Zdroj: | Journal of Carcinogenesis & Mutagenesis. |
| ISSN: | 2157-2518 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|