Minosako Yoshihito, Nemoto Masahiro, Ino Sento, Shirakami Yoshifumi, Kurami Miki
Research Centre, Research & Development Division, Nihon Medi-physics Co., Ltd.
Kaku Igaku. 2003 Feb;40(1):23-30.
Fluorine-18-2-fluoro-2-deoxy-D-glucose (18F-FDG) injectable was developed as a tumor imaging agent reflecting glucose metabolism. In membrane transportation studies, the uptake of 14C-FDG into erythrocytes decreased with an increase in glucose concentration, and Cytochalasin B, inhibitor of glucose transporter (GLUT), blocked the uptake about 75%. The results means FDG is transported into tumor cells mainly by GLUT as glucose analogues. 18F-FDG is recognized to be phosphorylated to 18F-FDG-6-phosphate with hexokinase. We found that FDG-6-phosphate was further isomerized to 18F-FDM-6-phosphate by phosphoglucose isomerase (PGI) in vitro. About 27% 18F-FDM-6-phosphate was generated at the reaction with 70 U PGI for 90 min. These results show that the 18F-FDG injectable manufactured by the commercial supply system has equivalent properties; membrane transportation characteristic and enzyme affinity, to FDG synthesized at each PET institution.
氟-18-2-氟-2-脱氧-D-葡萄糖(18F-FDG)注射剂被开发用作一种反映葡萄糖代谢的肿瘤成像剂。在膜转运研究中,14C-FDG进入红细胞的摄取量随着葡萄糖浓度的增加而降低,并且葡萄糖转运蛋白(GLUT)的抑制剂细胞松弛素B可阻断约75%的摄取。这些结果表明,FDG作为葡萄糖类似物主要通过GLUT转运进入肿瘤细胞。18F-FDG被认为可被己糖激酶磷酸化为18F-FDG-6-磷酸。我们发现,在体外,FDG-6-磷酸可被磷酸葡萄糖异构酶(PGI)进一步异构化为18F-FDM-6-磷酸。在与70 U PGI反应90分钟时,约生成27%的18F-FDM-6-磷酸。这些结果表明,通过商业供应系统生产的18F-FDG注射剂具有与各PET机构合成的FDG等效的性质,即膜转运特性和酶亲和力。