Porphyrin-containing Gadolinium Complex as a Tumor-targeting Magnetic Resonance Imaging (MRI) Contrast Agent

Curr Drug Deliv. 2018;15(7):972-978. doi: 10.2174/1567201815666180409111005.

Abstract

Objective: Gadolinium diethylenetriaminepentaacetic di[5-(4'-amidophenyl)-10,15,20- tris(4'-sulfonatophenyl) porphyrin trisodium salt] (Gd-DTPA-2APTSPP) was synthesized by the reaction of diethylenetriaminepentaacetic dianhydride with 5-(4'-aminophenyl)-10,15,20-tris(4'-sulfonatophenyl) porphyrin and subsequently chelation with gadolium chloride.

Methods: This gadolinium complex was characterized and its properties in vitro and in vivo were also evaluated. Compared with Gd-DTPA, Gd-DTPA-2APTSPP possessed high relaxivity r1, low cytotoxicity to HeLa cells and high enhanced signal intensities of the VX2 carcinoma in rabbits for a prolonged time.

Conclusion: Moreover, Gd-DTPA-2APTSPP can distinguish the VX2 carcinoma from the reactive hyperplasia incited by inflammation and normal tissues in rabbits. Therefore, Gd-DTPA-2APTSPP can be taken up selectively by tumors and show the potential as a tumor-targeting MRI contrast agent.

Keywords: Magnetic resonance imaging (MRI); VX2 carcinoma; contrast agent; gadolinium complex; porphyrin; tumortargeting..

MeSH terms

  • Animals
  • Cell Survival / drug effects
  • Contrast Media / administration & dosage*
  • Contrast Media / chemistry
  • Gadolinium / administration & dosage*
  • Gadolinium / chemistry
  • Gadolinium DTPA / administration & dosage*
  • Gadolinium DTPA / chemistry
  • HeLa Cells
  • Humans
  • Magnetic Resonance Imaging
  • Neoplasms / diagnostic imaging*
  • Porphyrins / administration & dosage*
  • Porphyrins / chemistry
  • Rabbits

Substances

  • Contrast Media
  • Porphyrins
  • Gadolinium
  • Gadolinium DTPA