Synthesis, radiolabeling, biodistribution and fluorescent imaging of histidine-coupled hematoporphyrin

Nucl Med Biol. 2012 May;39(4):579-85. doi: 10.1016/j.nucmedbio.2011.10.010. Epub 2012 Jan 5.

Abstract

Introduction: Hematoporphyrin (Hp) and hematoporphyrin derivatives (HpDs) have been widely used as photosensitizers in photodynamic therapy (PDT). Radiolabeling of HpDs is helpful for preclinical and clinical studies of PDT.

Methods: The histidine-coupled hematoporphyrin (His-Hp) was synthesized and radiolabeled with [(99m)Tc(CO)(3)(H(2)O)(3)](+). Biodistribution of the radioligand and fluorescent imaging of His-Hp in mice bearing S180 tumor were investigated.

Results: [(99m)Tc(CO)(3)](+)-labeled His-Hp was electrically neutral, hydrophilic and stable. The biodistribution of the radioligand in S180 tumor-bearing mice was similar with that of nonlabeled HpD in the literature. The uptake of His-Hp in tumors and livers was confirmed by fluorescent imaging.

Conclusions: The complex [(99m)Tc(CO)(3)](+)-His-Hp might be suitable for in vivo dose evaluation of HpD in PDT.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Chemistry Techniques, Synthetic*
  • Hematoporphyrins / chemical synthesis*
  • Hematoporphyrins / chemistry
  • Hematoporphyrins / pharmacokinetics*
  • Hematoporphyrins / therapeutic use
  • Histidine / chemistry*
  • Isotope Labeling
  • Male
  • Mice
  • Molecular Imaging / methods*
  • Organotechnetium Compounds / chemistry
  • Photochemotherapy
  • Photosensitizing Agents / chemical synthesis*
  • Photosensitizing Agents / chemistry
  • Photosensitizing Agents / pharmacokinetics*
  • Photosensitizing Agents / therapeutic use
  • Spectrometry, Fluorescence

Substances

  • Hematoporphyrins
  • Organotechnetium Compounds
  • Photosensitizing Agents
  • Histidine