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Synthesis of an In vivo MRI-detectable Apoptosis Probe
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Synthesis of an In vivo MRI-detectable Apoptosis Probe

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(1) H-NMR relaxometric studies of interaction between apoptosis specific MRI paramagnetic contrast agents and

Aurore Van Koninckxloo1, Céline Henoumont1, Sophie Laurent1,2

  • 1Department of General, Organic and Biomedical Chemistry, NMR and Molecular Imaging Laboratory, University of Mons, 7000, Mons, Belgium.

Magnetic Resonance in Chemistry : MRC
|December 10, 2015
PubMed

Insights

This study investigated gadolinium-grafted peptides for MRI contrast agents, showing preferential binding to apoptotic cell models. This offers a faster method for evaluating potential MRI contrast agents targeting cancer cells.

Area of Science:

  • Biomedical Engineering
  • Radiology
  • Molecular Imaging

Background:

  • Phage display identified peptides E3 and R826 that target apoptotic cells.
  • Previous analysis used 1H-NMR to study peptide-cell interactions.
  • Developing efficient MRI contrast agents requires evaluating peptide-target binding.

Purpose of the Study:

  • To evaluate the proton relaxometric behavior of gadolinium-grafted peptides and their analogs.
  • To assess the efficiency of potential MRI contrast agents targeting apoptotic cells.
  • To provide a fast evaluation method avoiding the use of actual apoptotic cells.

Main Methods:

  • Proton relaxometric behavior investigation using nuclear magnetic relaxation dispersion (NMRD) profiles.
  • Utilized micelles mimicking healthy (phosphocholine) and apoptotic (phosphoserine) cells.
  • Determined association constants (Ka) for peptide-gadolinium complexes.

Main Results:

  • Conjugated peptides showed preferential interaction with apoptotic cell models (phosphoserine micelles) compared to healthy cell models (phosphocholine micelles).
  • Enhanced transverse proton relaxation rates were observed at 60 MHz.
  • Association constants confirmed stronger binding of selected conjugated peptides (Gd-PMN-E3 and Gd-DTPA-R826) than their scrambled analogs.

Conclusions:

  • Gadolinium-grafted peptides demonstrate selective interaction with apoptotic cell membrane models.
  • This approach provides a rapid method for assessing potential MRI contrast agents.
  • The findings support the development of targeted MRI contrast agents for apoptotic cell detection.
Keywords:
1H-NMRD profilesapoptosiscontrast agentinteractionmicellar modelrelaxometry

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