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Inflammation targeted Gd(3+)-based MRI contrast agents imaging tumor and rheumatoid arthritis models

Arthur Ho-Hon Leung1, Jiefu Jin, Shuxia Wang

  • 1Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University , Hung Hom, Kowloon, Hong Kong, China.

Bioconjugate Chemistry
|May 27, 2014
PubMed

Insights

Researchers developed new MRI contrast agents (CAs) by linking anti-inflammatory drugs to gadolinium. These agents show promise for imaging inflammation and tumors, with one agent demonstrating superior retention and enhancement in arthritis models.

Area of Science:

  • Medical Imaging
  • Materials Science
  • Pharmacology

Background:

  • Inflammatory responses are critical in cancer and disease progression.
  • Targeted contrast agents can improve MRI sensitivity for inflammation.
  • Nonsteroidal anti-inflammatory drugs (NSAIDs) can be utilized in targeted imaging.

Purpose of the Study:

  • To synthesize and evaluate novel gadolinium-based MRI contrast agents conjugated to mefenamic acid (MA).
  • To assess the relaxivity, albumin binding, cytotoxicity, and cellular uptake of the new agents.
  • To investigate the in vivo performance of these agents for molecular imaging of inflammation and tumors.

Main Methods:

  • Synthesis of three Gd(3+) DO3A-amide MRI contrast agents (GdL1, GdL2, GdL3) conjugated to mefenamic acid via different linkers.
  • Measurement of relaxivities at 400 MHz, 25 °C.
  • Serum albumin binding studies using tryptophan emission-quenching.
  • Cytotoxicity assays on HeLa cells and cellular uptake studies in U87 cells.
  • In vivo MRI studies in U87 tumor and adjuvant-induced arthritis (AIA) models.

Main Results:

  • GdL1, GdL2, and GdL3 exhibited relaxivities of 4.74, 4.77, and 4.95 mM(-1) s(-1), respectively.
  • GdL1 showed preferential binding to human serum albumin (HSA) and bovine serum albumin (BSA).
  • Agents displayed low cytotoxicity and high cellular uptake in U87 cells.
  • In vivo MRI demonstrated enhanced T1-weighted contrast in tumor and arthritis models, with GdL3 showing the highest enhancement in the arthritis joint.
  • GdL1-3 showed superior retention and intensity enhancements compared to GdDOTA in various organs and target sites.

Conclusions:

  • The developed Gd(3+)-MA conjugates are effective MRI contrast agents for inflammation and tumor imaging.
  • GdL3 exhibits promising characteristics, including high relaxivity and retention, making it a potential candidate for targeted MRI of inflammation.
  • These agents offer improved performance over conventional agents like GdDOTA for specific disease imaging applications.

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