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Evaluation of 99m Tc-labeled glutathione as a colon cancer targeting probe
Journal of Radioanalytical and Nuclear Chemistry ( IF 1.5 ) Pub Date : 2021-01-20 , DOI: 10.1007/s10967-020-07563-1
Sumeera Sidiq , Ravi Ranjan Kumar , Neelima D. Passi , D. K. Dhawan , Jaya Shukla , B. R. Mittal , Vijayta D. Chadha

The present study was designed to unravel the bioevaluation of [99mTc]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 [99mTc]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 [99mTc]Tc-GSH radiocomplex has tumor delineating features and also exhibits selectivity for colon tumor.



中文翻译:

评价99m Tc标记的谷胱甘肽作为结肠癌靶向探针

本研究的目的是解开[的bioevaluation 99米锝]锝GSH在HT 29结肠癌细胞系,以及在实验性诱导的结肠癌。观察到放射化学产率为95.93±1.09%。在计算机对接研究中发现,[ 99m Tc] Tc-GSH可以很好地容纳在γ-谷氨酰转肽酶的结合口袋中,方向相当,估计结合能最低-81.90。毒性测定,即3-(4,5-二甲基噻唑基-2)-2,5-二苯基四唑溴化物和锥虫蓝排除测定表明,放射性复合物对HT 29细胞无毒。总之,体外和体内结果表明[ 99m Tc] Tc-GSH放射性复合物具有肿瘤勾画特征,并且还表现出对结肠肿瘤的选择性。

更新日期:2021-01-20
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