99mTc-labeled 1-thio-β-D-glucose as a new tumor-seeking agent:: Synthesis and tumor cell uptake assay

被引:28
作者
Oh, SJ
Ryu, JS
Yoon, EJ
Bae, MS
Choi, SJ
Park, KB
Moon, DH
机构
[1] Univ Ulsan, Coll Med, Asan Med Ctr, Dept Nucl Med, Seoul 138736, South Korea
[2] Ewha Womans Univ, Mokdong Hosp, Dept Radiol, Div Nucl Med, Seoul, South Korea
[3] Hanaro Ctr, Korea Atom Energy Res Inst, Div Radioisotope Prod & Applicat, Taejon 305600, South Korea
关键词
Tc-99m; 1-thio-beta-D-glucose; tumor imaging; glucose derivatives; tumor cell uptake assay;
D O I
10.1016/j.apradiso.2005.07.022
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
Tc-99m-labeled 1-thio-beta-D-glucose (Tc-99m-1-TG) was synthesized under different ligand concentrations. 1-Thio-beta-D-glucose (1-TG) showed different chemical properties and higher stability at acid pH as compared to neutral and basic pH. Under different ligand concentrations, Tc-99m-1-TG was obtained with high labeling efficiency of > 97%, but the HPLC chromatogram varied with the ligand concentration. The results of a tumor cell uptake assay also depended on the ligand concentration. With the lowest ligand concentration tested (0.5 mg/ml of 1-TG), we obtained the highest uptake. With different glucose and insulin concentrations, Tc-99m-1-TG uptake was not significantly different from that of [F-18]FDG. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:207 / 215
页数:9
相关论文
共 14 条
[1]   DISTRIBUTION OF VARIOUS LABELED THIOGLUCOSES IN RODENTS [J].
ATKINS, HL ;
LAMBRECHT, RM ;
WOLF, AP ;
ANSARI, AN ;
GUILLAUME, M .
RADIOLOGY, 1975, 115 (03) :723-725
[2]  
BALLINGER JR, 1993, J NUCL MED, V34, P242
[3]   PET and [F-18]-FDG in oncology: A clinical update [J].
Conti, PS ;
Lilien, DL ;
Hawley, K ;
Keppler, J ;
Grafton, ST ;
Bading, JR .
NUCLEAR MEDICINE AND BIOLOGY, 1996, 23 (06) :717-735
[4]   SPECIFICITY OF GOLD THIOGLUCOSE FOR VENTROMEDIAL HYPOTHALAMIC LESIONS AND HYPERPHAGIA [J].
MAYER, J ;
MARSHALL, NB .
NATURE, 1956, 178 (4547) :1399-1400
[5]   CYCLOTRON PRODUCTION OF PB-203 FOR RADIOPHARMACEUTICAL APPLICATIONS .11. [J].
MERRILL, JC ;
LAMBRECHT, RM ;
WOLF, AP .
INTERNATIONAL JOURNAL OF APPLIED RADIATION AND ISOTOPES, 1973, 24 (12) :701-702
[6]   Biodistribution of 99Tcm-labelled 5-thio-D-glucose [J].
Ozker, K ;
Collier, BD ;
Lindner, DJ ;
Kabasakal, L ;
Liu, Y ;
Krasnow, AZ ;
Hellman, RS ;
Edwards, SD ;
Bourque, CR ;
Crane, PD .
NUCLEAR MEDICINE COMMUNICATIONS, 1999, 20 (11) :1055-1058
[7]   FDG accumulation and tumor biology [J].
Pauwels, EKJ ;
Ribeiro, MJ ;
Stoot, JHMB ;
McCready, VR ;
Bourguignon, M ;
Maziere, B .
NUCLEAR MEDICINE AND BIOLOGY, 1998, 25 (04) :317-322
[8]   Oncological applications of positron emission tomography with fluorine-18 fluorodeoxyglucose [J].
Rigo, P ;
Paulus, P ;
Kaschten, BJ ;
Hustinx, R ;
Bury, T ;
Jerusalem, G ;
Benoit, T ;
FoidartWillems, J .
EUROPEAN JOURNAL OF NUCLEAR MEDICINE, 1996, 23 (12) :1641-1674
[9]   DISTRIBUTION OF TC-99M 1-THIOGLUCOSE IN RATS - EFFECT OF ADMINISTRATION ROUTE ON PANCREATIC SPECIFICITY [J].
RISCH, VR ;
HONDA, T ;
HEINDEL, ND ;
EMRICH, JL ;
BRADY, LW .
RADIOLOGY, 1977, 124 (03) :837-838
[10]   Synthesis and in vitro characterization of organometallic rhenium and technetium glucose complexes against glut 1 and hexokinase [J].
Schibli, R ;
Dumas, C ;
Petrig, J ;
Spadola, L ;
Scapozza, L ;
Garcia-Garayoa, E ;
Schubiger, PA .
BIOCONJUGATE CHEMISTRY, 2005, 16 (01) :105-112