| Literature DB >> 29985620 |
Xuran Zhang1, Qing Ruan, Xiaojiang Duan, Qianqian Gan, Xiaoqing Song, Sian Fang, Xiao Lin, Jin Du1, Junbo Zhang.
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.Entities:
Keywords: SPECT; Tc-99m; glucosamine-derivate; isonitrile; tumor imaging
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Year: 2018 PMID： 29985620 DOI： 10.1021/acs.molpharmaceut.8b00415
Source DB: PubMed Journal: Mol Pharm ISSN： 1543-8384 Impact factor: 4.939