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Molecules 2013, 18(6), 6908-6918; doi:10.3390/molecules18066908
Article

Preliminary Biological Evaluation of Novel 99mTc-Cys-Annexin A5 as a Apoptosis Imaging Agent

1
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1
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2, 1
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2, 1,*  and 2,3,*
1 Key Laboratory of Nuclear Medicine, Ministry of Health & Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China 2 Jiangsu Target Pharma Laboratories Inc., Changzhou High-Tech Research Institute of Nanjing University, Changzhou 213164, China 3 The State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, China
* Authors to whom correspondence should be addressed.
Received: 15 May 2013 / Revised: 24 May 2013 / Accepted: 5 June 2013 / Published: 10 June 2013
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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 cys-annexin A5; 99mTc-labelled; biodistribution; apoptosis imaging
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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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.

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