Investigation of a potential scintigraphic tracer for imaging apoptosis: radioiodinated annexin V-Kunitz protease inhibitor fusion protein

J Biomed Biotechnol. 2011:2011:675701. doi: 10.1155/2011/675701. Epub 2011 Apr 27.

Abstract

Radiolabeled annexin V (ANV) has been widely used for imaging cell apoptosis. Recently, a novel ANV-Kunitz-type protease inhibitor fusion protein, ANV-6L15, was found to be a promising probe for improved apoptosis detection based on its higher affinity to phosphatidylserine (PS) compared to native ANV. The present paper investigates the feasibility of apoptosis detection using radioiodinated ANV-6L15. Native ANV and ANV-6L15 were labeled with iodine-123 and iodine-125 using Iodogen method. The binding between the radioiodinated proteins and erythrocyte ghosts or chemical-induced apoptotic cells was examined. ANV-6L15 can be radioiodinated with high yield (40%-60%) and excellent radiochemical purity (>95%). (123)I-ANV-6L15 exhibited a higher binding ratio to erythrocyte ghosts and apoptotic cells compared to (123)I-ANV. The biodistribution of (123)I-ANV-6L15 in mice was also characterized. (123)I-ANV-6L15 was rapidly cleared from the blood. High uptake in the liver and the kidneys may limit the evaluation of apoptosis in abdominal regions. Our data suggest that radiolabeled ANV-6L15 may be a better scintigraphic tracer than native ANV for apoptosis detection.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Annexin A5 / chemistry*
  • Annexin A5 / pharmacokinetics
  • Apoptosis / physiology*
  • Aprotinin / chemistry*
  • Aprotinin / pharmacokinetics
  • Erythrocyte Membrane / metabolism
  • Flow Cytometry
  • Humans
  • Hydrogen-Ion Concentration
  • Iodine Radioisotopes / chemistry*
  • Isotope Labeling / methods
  • Jurkat Cells
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Molecular Imaging / methods*
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / pharmacokinetics
  • Recombinant Fusion Proteins / chemistry*
  • Recombinant Fusion Proteins / pharmacokinetics
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon / methods*
  • Whole Body Imaging

Substances

  • Annexin A5
  • Iodine Radioisotopes
  • Radiopharmaceuticals
  • Recombinant Fusion Proteins
  • Aprotinin