Preparation, in vitro and in vivo evaluation of (99m)Tc-Annexin B1: a novel radioligand for apoptosis imaging

To develop a radiopharmaceutical for apoptosis imaging, Annexin B1, a new Ca2+-dependent phosphatidylserine (PS)-binding protein, was directly radiolabeled with (99m)Tc. This procedure yields up to 96% of radiochemical purity and higher radiolabeling efficiency. The preparation has been found to be...

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Bibliographic Details
Published in:Biochemical and biophysical research communications 2005-10, Vol.335 (4), p.1102-1106
Main Authors: Luo, Quan-Yong, Zhang, Zhi-Yong, Wang, Fang, Lu, Han-Kui, Guo, Yu-Zhi, Zhu, Rui-Sen
Format: Article
Language:English
Subjects:
60 APPLIED LIFE SCIENCES
Animals
Annexins - chemistry
Annexins - pharmacokinetics
ANTIBODIES
APOPTOSIS
Apoptosis - physiology
BLOOD
Blood Platelets - diagnostic imaging
Blood Platelets - physiology
CALCIUM IONS
Cells, Cultured
Drug Stability
EFFICIENCY
EVALUATION
Humans
IN VITRO
IN VIVO
Isotope Labeling - methods
KIDNEYS
LABELLING
LIVER
MICE
Mice, Inbred BALB C
Organ Specificity
Organotechnetium Compounds - chemistry
Organotechnetium Compounds - pharmacokinetics
PROTEINS
Radionuclide Imaging
RADIOPHARMACEUTICALS
Radiopharmaceuticals - chemistry
Radiopharmaceuticals - pharmacokinetics
Reproducibility of Results
TECHNETIUM 99
Tissue Distribution
TRACER TECHNIQUES
UPTAKE
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Summary:To develop a radiopharmaceutical for apoptosis imaging, Annexin B1, a new Ca2+-dependent phosphatidylserine (PS)-binding protein, was directly radiolabeled with (99m)Tc. This procedure yields up to 96% of radiochemical purity and higher radiolabeling efficiency. The preparation has been found to be sufficiently stable in vitro. Binding assay with human activated platelets indicated that (99m)Tc-Annexin B1 retained its PS binding activity. Biodistribution in mice revealed that (99m)Tc-Annexin B1 rapidly cleared from the blood and predominantly accumulated in the kidney. The increase in hepatic uptake in anti-Fas antibody treated mice correlated to histologic evidence of fulminant hepatic apoptosis. These data suggest that (99m)Tc-Annexin B1 can be used as a novel radiotracer to detect apoptosis in vivo.
ISSN:0006-291X
1090-2104
DOI:10.1016/j.bbrc.2005.07.188