Research Papers:

Preliminary biological evaluation of 18F-AlF-NOTA-MAL-Cys-Annexin V as a novel apoptosis imaging agent

Chunxiong Lu _, Quanfu Jiang, Minjin Hu, Cheng Tan, Huixin Yu and Zichun Hua

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Oncotarget. 2017; 8:51086-51095. https://doi.org/10.18632/oncotarget.16994

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Chunxiong Lu1, Quanfu Jiang1, Minjin Hu2, Cheng Tan1, Huixin Yu1 and Zichun Hua2,3

1Key Laboratory of Nuclear Medicine, Ministry of Health & Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China

2Jiangsu Target Pharma Laboratories Inc., Changzhou High-Tech Research Institute of Nanjing University, Changzhou 213164, China

3The State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, China

Correspondence to:

Huixin Yu, email: [email protected]

Zichun Hua, email: [email protected]

Keywords: site-specific labeling, 18F-AlF-NOTA-MAL-Cys-Annexin V, apoptosis imaging

Received: November 08, 2016    Accepted: February 12, 2017    Published: April 10, 2017


A novel annexin V derivative (Cys-Annexin V) with a single cysteine residue at its C-terminal has been successfully labeled site-specifically with NOTA-maleimide aluminum [18F]fluoride complexation and evaluated it as a novel apoptosis agent in vitro and in vivo. The total synthesis time of 18F-AlF-NOTA-MAL-Cys-Annexin V from [18F]fluoride was about 65 min. The tracer was stable in vitro and it was excreted through renal in normal mice. The rate of the tracer bound to erythrocytes with exposed phosphatidylserine was 89.36±0.61% and this binding could be blocked by unlabeled Cys-Annexin V. In rats treated with cycloheximide, there were 6.23±0.23 times (n=4) increase in hepatic uptake of the tracer as compared to normal rats at 1h p.i. The uptake of the tracer in liver also could be blocked by co-injection of unlabeled Cys-Annexin V. These results indicated the favorable characterizations such as convenient synthesis and specific apoptotic cells targeting of18F-AlF-NOTA-MAL- Cys-Annexin V were suitable for its further investigation in clinical apoptosis imaging.

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