Abstract:
:In this study, a d-glucosamine derivative with an isonitrile group (CN5DG) was synthesized and it was chosen to coordinate with 99mTc for preparing 99mTc-CN5DG. 99mTc-CN5DG could be readily obtained with high radiochemical purity (>95%) and had great in vitro stability and metabolic stability in urine. The radiotracer demonstrated a positive response to the administration of glucose and insulin in S180 and A549 tumor cells in vitro, suggesting the mechanism of 99mTc-CN5DG into tumor cells was related to glucose transporters. Biodistribution studies in mice bearing A549 xenografts showed 99mTc-CN5DG had a high tumor uptake and high tumor-to-background ratios. SPECT/CT images further supported its ability for tumor imaging. As a cheap, conveniently made and widely available probe, 99mTc-CN5DG would become a potential "working horse" and be a breakthrough in 99mTc-labeled radiopharmaceuticals for tumor detection.
journal_name
Mol Pharmjournal_title
Molecular pharmaceuticsauthors
Zhang X,Ruan Q,Duan X,Gan Q,Song X,Fang S,Lin X,Du J,Zhang Jdoi
10.1021/acs.molpharmaceut.8b00415subject
Has Abstractpub_date
2018-08-06 00:00:00pages
3417-3424issue
8eissn
1543-8384issn
1543-8392journal_volume
15pub_type
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