Radio-labeling and Micro-PET Study of 64Cu Labeled D-Glucose for Tumor Imaging†

doi:10.7503/cjcu20130718

Abstract

Abstract:

2-(4-Isothiocyanatobenzyl)-1,4,7,10-tetraazacyclo-dodecane-1,4,7,10-tetraacetic acid-D-glucose(DOTA-DG) was synthesized and radiolabeled with ⁶⁴Cu. The DOTA-DG dissolved in sodium acetate buffer(pH=5.5) was added to the eluent of ⁶⁴Cu. The solution was stirred and placed at 25 ℃ for 30 min. The labeling efficiency and radiochemical purity of ⁶⁴Cu-DOTA-DG were all over 95%, as determined by radio-HPLC. The in vitro stability of the conjugates was analyzed in 0.1 mol/L PBS and 0.1 mol/L NaAc and it showed excellent in vitro stability. 14.8 MBq of ⁶⁴Cu-DOTA-DG was injected to Hep-G2 xenograft models via tale vein. Positron emission tomography images were taken 1 and 3 h after the injection. These images suggested that there was high tumor uptake of ⁶⁴Cu-DOTA-DG. The results suggested that ⁶⁴Cu-DOTA-DG could provide images much clearer than the DG labeled with ^99mTc, ¹¹¹In and ⁶⁸Ga, and observation of the metabolism of DG much longer. These preliminary data show that ⁶⁴Cu-DOTA-DG appears to be useful in PET imaging.

Key words: 2-Amino-deoxy-D-glucose, ⁶⁴Cu, Positron emission tomography(PET), Tumor

CLC Number:

O615.3

TrendMD:

HONG Ye, ZHU Hua, HU Ji, LIN Xinfeng, QING Jing, YANG Zhi. Radio-labeling and Micro-PET Study of ⁶⁴Cu Labeled D-Glucose for Tumor Imaging^†[J]. Chem. J. Chinese Universities, 2014, 35(4): 724.

Figures/Tables 4

Scheme 1 Synthesis and radiolabeling of 64Cu-DOTA-DG

Fig.1 Influences of the temperature(A) and reaction time(B) on the labeling efficiency (A) Reaction time: 30 min; (B) temperature: 25 ℃.

Fig.2 In vitro stability of 64Cu-DOTA-DG conjugate in PBS(a) and NaAc(b) solutions

Fig.3 PET images of 64Cu-DOTA-DG 1 h(A—C) and 3 h(D—F) after intravenious injection (A, D) Transverse plane; (B, E) coronal plane; (C, F) sagittal plane.

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Radio-labeling and Micro-PET Study of ⁶⁴Cu Labeled D-Glucose for Tumor Imaging^†

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