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Am J Nucl Med Mol Imaging 2012;2(4):499-507
Original Article
Synthesis and evaluation of 68Ga-labeled DOTA-2-deoxy-D-glucosamine as a
potential radiotracer in μPET imaging
Zhi Yang, Chiyi Xiong, Rui Zhang, Hua Zhu, Chun Li
Department of Experimental Diagnostic Imaging, Unit 59, The University of Texas MD Anderson Cancer Center, 1515 Holcombe
Boulevard, Houston, TX 77030, USA; Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education),
Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing, People’s Republic of China.
Received August 29, 2012; Accepted September 27, 2012; Epub October 15, 2012; Published October 30, 2012
Abstract: The purposes of this study were to develop an efficient method of labeling D-glucosamine hydrochloride with gallium 68
(68Ga) and investigate the imaging properties of the resulting radiotracer in a human tumor xenograft model using micro-positron
emission tomography (μPET). The precursor compound 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid (DOTA)-2-deoxy-D-
glucosamine (DOTA-DG) was synthesized from D-glucosamine hydrochloride and 2-(4-isothiocyanatobenzyl)-DOTA. Radiolabeling
of DOTA-DG with 68Ga was achieved in 10 minutes using microwave heating. The labeling efficiency and radiochemical purity after
purification of 68Ga-DOTA-DG were ~85% and greater than 98%, respectively. In A431 cells, the percentages of 68Ga-DOTA-DG and
18F-FDG uptakes after 60 min incubation were 15.7% and 16.2%, respectively. In vivo, the mean ± standard deviation of 68Ga-
DOTADG uptake values in A431 tumors were 2.38±0.30, 0.75±0.13, and 0.39±0.04 percent of the injected dose per gram of tissue at
10, 30, and 60 minutes after intravenous injection, respectively. μPET imaging of A431-bearing mice clearly delineated tumors at 60
minutes after injection of 68Ga-DOTA-DG at a dose of 3.7 MBq. 68Ga-DOTA-DG displayed significantly higher tumor-to-heart, tumor-
to-brain, and tumor-to-muscle ratios than 18F-FDG did. Further studies are needed to identify the mechanism of tumor uptake of this
new glucosamine-based PET imaging tracer. (ajnmmi1208009).
Keywords: Gallium 68, 2-deoxy-D-glucose, μPET imaging, microwave heating-assisted synthesis
Address all correspondence to:
Dr. Chun Li
Department of Experimental Diagnostic Imaging, Unit 59
The University of Texas MD Anderson Cancer Center
Houston, TX 77030, USA.
Phone: 713-792-5182; Fax: 713-794-5456
Email: cli@mdanderson.org
Dr. Zhi Yang
Department of Nuclear Medicine
Peking University Cancer Hospital & Institute
Beijing, 100142, People’s Republic of China.
Phone: +86-10-88120970; Fax: +86-10-77196196
Email: pekyangzhi@yahoo.com
Original Article
Synthesis and evaluation of 68Ga-labeled DOTA-2-deoxy-D-glucosamine as a
potential radiotracer in μPET imaging
Zhi Yang, Chiyi Xiong, Rui Zhang, Hua Zhu, Chun Li
Department of Experimental Diagnostic Imaging, Unit 59, The University of Texas MD Anderson Cancer Center, 1515 Holcombe
Boulevard, Houston, TX 77030, USA; Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education),
Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing, People’s Republic of China.
Received August 29, 2012; Accepted September 27, 2012; Epub October 15, 2012; Published October 30, 2012
Abstract: The purposes of this study were to develop an efficient method of labeling D-glucosamine hydrochloride with gallium 68
(68Ga) and investigate the imaging properties of the resulting radiotracer in a human tumor xenograft model using micro-positron
emission tomography (μPET). The precursor compound 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid (DOTA)-2-deoxy-D-
glucosamine (DOTA-DG) was synthesized from D-glucosamine hydrochloride and 2-(4-isothiocyanatobenzyl)-DOTA. Radiolabeling
of DOTA-DG with 68Ga was achieved in 10 minutes using microwave heating. The labeling efficiency and radiochemical purity after
purification of 68Ga-DOTA-DG were ~85% and greater than 98%, respectively. In A431 cells, the percentages of 68Ga-DOTA-DG and
18F-FDG uptakes after 60 min incubation were 15.7% and 16.2%, respectively. In vivo, the mean ± standard deviation of 68Ga-
DOTADG uptake values in A431 tumors were 2.38±0.30, 0.75±0.13, and 0.39±0.04 percent of the injected dose per gram of tissue at
10, 30, and 60 minutes after intravenous injection, respectively. μPET imaging of A431-bearing mice clearly delineated tumors at 60
minutes after injection of 68Ga-DOTA-DG at a dose of 3.7 MBq. 68Ga-DOTA-DG displayed significantly higher tumor-to-heart, tumor-
to-brain, and tumor-to-muscle ratios than 18F-FDG did. Further studies are needed to identify the mechanism of tumor uptake of this
new glucosamine-based PET imaging tracer. (ajnmmi1208009).
Keywords: Gallium 68, 2-deoxy-D-glucose, μPET imaging, microwave heating-assisted synthesis
Address all correspondence to:
Dr. Chun Li
Department of Experimental Diagnostic Imaging, Unit 59
The University of Texas MD Anderson Cancer Center
Houston, TX 77030, USA.
Phone: 713-792-5182; Fax: 713-794-5456
Email: cli@mdanderson.org
Dr. Zhi Yang
Department of Nuclear Medicine
Peking University Cancer Hospital & Institute
Beijing, 100142, People’s Republic of China.
Phone: +86-10-88120970; Fax: +86-10-77196196
Email: pekyangzhi@yahoo.com
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