Basic Science Investigation
Synthesis and biological evaluation of 68Ga-NODAGA-GE11
Li Huiqiang, Zhen Zhifei, Zhang Weifeng, Liao Shuguang, Xuan Ang, Fu Chang, You Yang, Gao Yongju, Xu Junling
Published 2021-11-25
Cite as Chin J Nucl Med Mol Imaging, 2021, 41(11): 676-679. DOI: 10.3760/cma.j.cn321828-20200519-00202
Abstract
ObjectiveTo prepare 68Ga-2-(4, 7-bis(carboxymethyl)-1, 4, 7-triazonan-1-yl)pentanedioic acid (NODAGA)-YHWYGYTPQNVI (GE11) and evaluate its feasibility of PET imaging for pancreatic cancer.
MethodsGE11 peptide was conjugated with NODAGA and then labeled with 68Ga. The labeling yield, radiochemical purity, hydrophilicity, stability and specificity in vitro were determined. Human pancreatic cancer BxPC3 nude mice models (n=9) were established. MicroPET imaging was then obtained after 30 and 90 min, and mice were sacrificed at 90 min to acquire the radioactivity distribution of main organs and tumors. Pair t test was used to analyze the data.
ResultsThe labeling yield was (73.5±5.4)% and radiochemical purity was more than 98%. After incubation 120 min in mouse serum at 37 ℃, radiochemical purity was more than 92%. The uptake was specific in BxPC3 cell lines. MicroPET images showed that 68Ga-NODAGA-GE11 could accumulate quickly in tumor. Value of tumor uptake was significantly higher than that of normal pancreas at 90 min ((1.38±0.25) vs (0.49±0.07) %ID/g; t=12.67, P<0.05), and the radio-uptake of blood, muscle and bone was lower than that of tumor.
Conclusions68Ga-NODAGA-GE11 is easy to be prepared with high radiochemical purity and good stability, and can specifically target BxPC3 xenograft tumor. However, due to the high uptake in the kidneys and liver, the value of 68Ga-NODAGA-GE11 in PET imaging for pancreatic tumor needs further study.
Key words:
GE11 peptide; Heterocyclic compounds, 1-ring; Gallium radioisotopes; Positron-emission tomography; Pancreatic neoplasms; Tumor cells, cultured; Mice, nude
Contributor Information
Li Huiqiang
Department of Nuclear Medicine, Henan Provincial People′s Hospital, People′s Hospital of Zhengzhou University, Zhengzhou 450003, China
Zhen Zhifei
Department of Nuclear Medicine, Henan Provincial People′s Hospital, People′s Hospital of Zhengzhou University, Zhengzhou 450003, China
Zhang Weifeng
Department of Nuclear Medicine, Henan Provincial People′s Hospital, People′s Hospital of Zhengzhou University, Zhengzhou 450003, China
Liao Shuguang
Department of Nuclear Medicine, Henan Provincial People′s Hospital, People′s Hospital of Zhengzhou University, Zhengzhou 450003, China
Xuan Ang
Department of Nuclear Medicine, Henan Provincial People′s Hospital, People′s Hospital of Zhengzhou University, Zhengzhou 450003, China
Fu Chang
Department of Nuclear Medicine, Henan Provincial People′s Hospital, People′s Hospital of Zhengzhou University, Zhengzhou 450003, China
You Yang
Department of Nuclear Medicine, Henan Provincial People′s Hospital, People′s Hospital of Zhengzhou University, Zhengzhou 450003, China
Gao Yongju
Department of Nuclear Medicine, Henan Provincial People′s Hospital, People′s Hospital of Zhengzhou University, Zhengzhou 450003, China
Xu Junling
Department of Nuclear Medicine, Henan Provincial People′s Hospital, People′s Hospital of Zhengzhou University, Zhengzhou 450003, China
