Seidensticker M, Ulrich G, Muehlberg F L, Pethe A, Grosser O S, Steffen I G, Stiebler M, Goldschmidt J, Smalla K H, Seidensticker R, Ricke J, Amthauer H, Mohnike K
Klinik für Radiologie und Nuklearmedizin, Universitätsklinik Magdeburg, Leipziger Strasse 44, 39120, Magdeburg, Germany,
Mol Imaging Biol. 2014 Apr;16(2):189-98. doi: 10.1007/s11307-013-0690-3.
This study was conducted to investigate the capacity of (99m)Tc-labeled 1-thio-β-D-glucose ((99m)Tc-1-TG) and 5-thio-D-glucose ((99m)Tc-5-TG) to act as a marker for glucose metabolism in tumor cells in vitro.
We investigated the cellular uptake of (99m)Tc-1-TG, (99m)Tc-5-TG, and 2-deoxy-2-[(18)F]fluoro-D-glucose((18)F-FDG) in a human colorectal carcinoma and human lung adenocarcinoma cell line (HCT-116, A549) at different time points and varying glucose/insulin concentrations and under transporter blockage by cytochalasin-B and phloretin. Cell compartment analysis was performed.
A significant uptake and time dependency thereof, a significant uptake dependency on glucose and insulin and a significant uptake inhibition by cytochalasin-B for (99m)Tc-1-TG and (99m)Tc-5-TG, was shown. Albeit substantial, the uptake was less pronounced in (99m)Tc-1-TG and (99m)Tc-5-TG compared with (18)F-FDG. (99m)Tc-1-TG and (99m)Tc-5-TG showed a higher accumulation in the cell membranes compared with (18)F-FDG.
Tc-1-TG and (99m)Tc-5-TG showed an uptake in vitro with glucose analog characteristics but with membranous accumulation. Tumor imaging should be investigated in an animal model.
本研究旨在探讨（99m）Tc标记的1-硫代-β-D-葡萄糖（（99m）Tc-1-TG）和5-硫代-D-葡萄糖（（99m）Tc-5-TG）在体外作为肿瘤细胞葡萄糖代谢标志物的能力。
我们在不同时间点、不同葡萄糖/胰岛素浓度以及细胞松弛素B和根皮素转运体阻断的情况下，研究了（99m）Tc-1-TG、（99m）Tc-5-TG和2-脱氧-2-[(18)F]氟-D-葡萄糖（(18)F-FDG）在人结肠癌细胞系和人肺腺癌细胞系（HCT-116、A549）中的细胞摄取情况。进行了细胞区室分析。
结果显示，（99m）Tc-1-TG和（99m）Tc-5-TG有显著摄取及其时间依赖性、对葡萄糖和胰岛素的显著摄取依赖性以及细胞松弛素B对其摄取的显著抑制作用。尽管摄取量很大，但与（18）F-FDG相比，（99m）Tc-1-TG和（99m）Tc-5-TG的摄取不太明显。与（18）F-FDG相比，（99m）Tc-1-TG和（99m）Tc-5-TG在细胞膜中的积累更高。
Tc-1-TG和（99m）Tc-5-TG在体外表现出具有葡萄糖类似物特征的摄取，但有膜积累。应在动物模型中研究肿瘤成像。
