Yang David J, Kim Chang-Guhn, Schechter Naomi R, Azhdarinia Ali, Yu Dong-Fang, Oh Chang-Sok, Bryant Jerry L, Won Jong-Jin, Kim E Edmund, Podoloff Donald A
Division of Diagnostic Imaging, University of Texas M.D. Anderson Cancer Center, 1515 Holcombe Blvd, Houston, TX 77030, USA.
Radiology. 2003 Feb;226(2):465-73. doi: 10.1148/radiol.2262011811.
To evaluate the feasibility of technetium 99m ((99m)Tc) ethylenedicysteine-deoxyglucose (ECDG) imaging in tumor-bearing rodents.
ECDG was synthesized by means of reacting ethylenedicysteine with glucosamine, with carbodiimide as the coupling agent. Hexokinase assays were performed at an ultraviolet wavelength of 340 nm. To determine whether blood glucose level could be altered, ECDG or glucosamine was injected into six rats. In a separate study, ECDG followed by insulin was administered to three rats. To determine biodistribution, lung tumor cells were intramuscularly injected into the hind legs of 18 nude mice. The animals were then injected with (99m)Tc ECDG or fluorine 18 ((18)F) fluorodeoxyglucose (FDG) (0.037-0.074 MBq per mouse). Radioactivity was measured in tissue excised from the animals. Scintigraphy was performed in three groups: in group 1 to demonstrate that different-sized tumors could be imaged after (99m)Tc ECDG administration, in group 2 to ascertain whether tumor uptake of (99m)Tc ECDG was perfusion related, and in group 3 to demonstrate that tumor uptake of (99m)Tc ECDG occurred by means of a glucose-mediated process.
ECDG was positive for phosphorylation at hexokinase assay. Blood glucose level increased with ECDG injection and decreased with insulin administration. Tumor-to-brain tissue and tumor-to-muscle tissue ratios of (99m)Tc ECDG uptake were higher than those of (18)F FDG uptake. Scintigraphic results demonstrated the feasibility of (99m)Tc ECDG imaging.
There are similarities between (99m)Tc ECDG uptake and (18)F FDG uptake in tumors, and study findings supported the potential use of (99m)Tc ECDG as a functional imaging agent.
评估锝99m（99mTc）乙二半胱氨酸 - 脱氧葡萄糖（ECDG）成像在荷瘤啮齿动物中的可行性。
以碳二亚胺为偶联剂，通过乙二半胱氨酸与葡糖胺反应合成ECDG。在340nm的紫外波长下进行己糖激酶测定。为确定血糖水平是否会改变，将ECDG或葡糖胺注射到6只大鼠体内。在另一项研究中，给3只大鼠先注射ECDG，随后注射胰岛素。为确定生物分布，将肺肿瘤细胞肌肉注射到18只裸鼠的后腿中。然后给这些动物注射99mTc ECDG或氟18（18F）氟脱氧葡萄糖（FDG）（每只小鼠0.037 - 0.074MBq）。测量从动物身上切除的组织中的放射性。在三组中进行闪烁显像：第1组用于证明给予99mTc ECDG后不同大小的肿瘤均可成像，第2组用于确定99mTc ECDG的肿瘤摄取是否与灌注有关，第3组用于证明99mTc ECDG的肿瘤摄取是通过葡萄糖介导的过程发生的。
在己糖激酶测定中，ECDG的磷酸化呈阳性。注射ECDG后血糖水平升高，注射胰岛素后血糖水平降低。99mTc ECDG摄取的肿瘤与脑组织及肿瘤与肌肉组织的比值高于18F FDG摄取的比值。闪烁显像结果证明了99mTc ECDG成像的可行性。
肿瘤中99mTc ECDG摄取与18F FDG摄取存在相似性，研究结果支持99mTc ECDG作为一种功能成像剂的潜在用途。
