4.5 Article

Evaluation of 99mTc-labeled glutathione as a colon cancer targeting probe

Journal

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
Volume 327, Issue 2, Pages 673-689

Publisher

SPRINGER
DOI: 10.1007/s10967-020-07563-1

Keywords

Glutathione; Gamma-glutamyl transpeptidase; Radiolabeling; Molecular docking; Colon cancer; [Tc-99m]technetium

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The study demonstrated that [Tc-99m]Tc-GSH has a high radiochemical yield and good binding capability in HT 29 colon cancer cell line, while showing no toxicity to the cells. Both in vitro and in vivo results suggest that the radiocomplex has tumor delineating features and selectivity for colon tumor.
The present study was designed to unravel the bioevaluation of [Tc-99m]Tc-GSH in HT 29 colon cancer cell line as well as in experimentally induced colon cancer. The radiochemical yield was observed to be 95.93 +/- 1.09%. In silico docking studies revealed that [Tc-99m]Tc-GSH gets well accommodated in the binding pocket of gamma-glutamyl transpeptidase in comparable orientation with lowest estimated binding energy - 81.90. Toxicity assays i.e. 3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide and trypan blue exclusion assay showed that radiocomplex is non-toxic to HT 29 cells. In conclusion, in vitro and in vivo results indicated the [Tc-99m]Tc-GSH radiocomplex has tumor delineating features and also exhibits selectivity for colon tumor.

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