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Preliminary Biological Evaluation of Novel 99mTc-Cys-Annexin A5 as a Apoptosis Imaging Agent
Key Laboratory of Nuclear Medicine, Ministry of Health & Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China
Jiangsu Target Pharma Laboratories Inc., Changzhou High-Tech Research Institute of Nanjing University, Changzhou 213164, China
The State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, China
* Authors to whom correspondence should be addressed.
Received: 15 May 2013; in revised form: 24 May 2013 / Accepted: 5 June 2013 / Published: 10 June 2013
Abstract: A novel annexin A5 derivative (cys-annexin A5) with a single cysteine residue at its C-terminal has been developed and successfully labeled in high labeling yield with 99mTc by a ligand exchange reaction. Like the 1st generation 99mTc-HYNIC-annexin A5, the novel 99mTc-cys-annexin A5 derivative shows in normal mice mainly renal and, to a lesser extent, hepatobiliary excretion. In rat models of hepatic apoptosis there was 283% increase in hepatic uptake of 99mTc-cys-annexin A5 as compared to normal mice. The results indicate that the novel 99mTc-cys-annexin A5 is a potential apoptosis imaging agent.
Keywords: cys-annexin A5; 99mTc-labelled; biodistribution; apoptosis imaging
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MDPI and ACS Style
Lu, C.; Jiang, Q.; Hu, M.; Tan, C.; Ji, Y.; Yu, H.; Hua, Z. Preliminary Biological Evaluation of Novel 99mTc-Cys-Annexin A5 as a Apoptosis Imaging Agent. Molecules 2013, 18, 6908-6918.
Lu C, Jiang Q, Hu M, Tan C, Ji Y, Yu H, Hua Z. Preliminary Biological Evaluation of Novel 99mTc-Cys-Annexin A5 as a Apoptosis Imaging Agent. Molecules. 2013; 18(6):6908-6918.
Lu, Chunxiong; Jiang, Quanfu; Hu, Minjin; Tan, Cheng; Ji, Yu; Yu, Huixin; Hua, Zichun. 2013. "Preliminary Biological Evaluation of Novel 99mTc-Cys-Annexin A5 as a Apoptosis Imaging Agent." Molecules 18, no. 6: 6908-6918.