Affinity ofnat/68ga-labelled curcumin and curcuminoid complexes for β-amyloid plaques: Towards the development of new metal-curcumin based radiotracers

Sara Rubagotti, Stefania Croci, Erika Ferrari, Michele Iori, Pier C. Capponi, Luca Lorenzini, Laura Calzà, Annibale Versari, Mattia Asti

Research output: Contribution to journalArticle

Abstract

Curcumin derivatives labelled with fluorine-18 or technetium-99m have recently shown their potential as diagnostic tools for Alzheimer’s disease. Nevertheless, no study by exploiting the labelling with gallium-68 has been performed so far, in spite of its suitable properties (positron emitter, generator produced radionuclide). Herein, an evaluation of the affinity for synthetic β-amyloid fibrils and for amyloid plaques of threenat/68Ga-labelled curcumin analogues, namely curcumin curcumin (CUR), bis-dehydroxy-curcumin (bDHC) and diacetyl-curcumin (DAC), was performed. Affinity and specificity were tested in vitro on amyloid synthetic fibrils by using gallium-68 labelled compounds. Post-mortem brain cryosections from Tg2576 mice were used for the ex vivo visualization of amyloid plaques. The affinity of 68Ga(CUR)2+,68Ga(DAC)2+, and68Ga(bDHC)2+ for synthetic β-amyloid fibrils was moderate and their uptake could be observed in vitro. On the other hand, amyloid plaques could not be visualized on brain sections of Tg2576 mice after injection, probably due to the low stability of the complexes in vivo and of a hampered passage through the blood-brain barrier. Like curcumin, allnat/68Ga-curcuminoid complexes maintain a high affinity for β-amyloid plaques. However, structural modifications are still needed to improve their applicability as radiotracers in vivo.

Original languageEnglish
Article number1480
JournalInternational Journal of Molecular Sciences
Volume17
Issue number9
DOIs
Publication statusPublished - Sep 6 2016

Keywords

  • Alzheimer disease
  • Curcumin
  • Curcuminoid complexes
  • Fluorescence
  • Gallium-68
  • β-amyloid

ASJC Scopus subject areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

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