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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
, 1
, 2, 1
, 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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