title: Synthesis and biodistribution of a new (99m) Tc-oxo complex with deoxyglucose dithiocarbamate for tumor imaging.
abstract: The deoxyglucose dithiocarbamate (DGDTC) was radiolabeled with (99m) Tc(V)-glucoheptonate (GH), for the potential use as radiopharmaceuticals for tumor imaging. For labeling, (99m) TcO-DGDTC was prepared by ligand-exchange reaction with (99m) Tc-GH. The radiochemical purity of the (99m) TcO-DGDTC complex was over 90% by thin-layer chromatography and high-performance liquid chromatography, without any notable decomposition at room temperature over a period of 6 h. Its partition coefficient indicated that it was a hydrophilic complex. The ligand-exchange reaction occured at neutral condition and under 100 °C for 15 min to achieve high radiochemical purity. In vitro cell studies showed there was an increase in the uptake of (99m) TcO-DGDTC as a function of incubation time and the cellular uptake of (99m) TcO-DGDTC was possibly mediated by way of a d-glucose mechanism. The biodistribution of (99m) TcO-DGDTC in mice bearing S 180 tumor showed that the complex accumulated in the tumor with good uptake and excellent retention. As compared with other reported (99m) Tc radiolabeled glucose derivatives, (99m) TcO-DGDTC showed the highest tumor uptake and good tumor/muscle ratios. The tumor/muscle ratio of (99m) TcO-DGDTC uptake was higher than that of [(18) F] FDG uptake. Single photon emission computed tomography (SPECT) image studies showed there was a visible accumulation in tumor sites, suggesting (99m) TcO-DGDTC would be a promising candidate for tumor imaging.
authors.affiliation: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing, China.
authors.forename: Xiao
authors.initials: X
authors.lastname: Lin
authors.forename: Zhonghui
authors.initials: Z
authors.lastname: Jin
authors.forename: Jialei
authors.initials: J
authors.lastname: Ren
authors.forename: Yan
authors.initials: Y
authors.lastname: Pang
authors.forename: Weifang
authors.initials: W
authors.lastname: Zhang
authors.forename: Jinfeng
authors.initials: J
authors.lastname: Huo
authors.forename: Xuebin
authors.initials: X
authors.lastname: Wang
authors.forename: Junbo
authors.initials: J
authors.lastname: Zhang
authors.forename: Yanyan
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D000818:Animals; D002219:Carbamates / Q000737:chemistry*; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D003847:Deoxyglucose / Q000031:analogs & derivatives* / Q000737:chemistry; D019788:Fluorodeoxyglucose F18 / Q000737:chemistry / Q000493:pharmacokinetics; D051379:Mice; D008819:Mice, Nude; D009369:Neoplasms / Q000000981:diagnostic imaging*; D015609:Organotechnetium Compounds / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D002219:Carbamates; D056831:Coordination Complexes; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C541546:deoxyglucose dithiocarbamate; D019788:Fluorodeoxyglucose F18; D003847:Deoxyglucose