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Issue 33, 2011
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3,4,3-LI(1,2-HOPO): In vitro formation of highly stable lanthanide complexes translates into efficacious in vivoeuropium decorporation

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Abstract

The spermine-based hydroxypyridonate octadentate chelator 3,4,3-LI(1,2-HOPO) was investigated for its ability to act as an antenna that sensitizes the emission of SmIII, EuIII, and TbIII in the Visible range (Φtot = 0.2–7%) and the emission of PrIII, NdIII, SmIII, and YbIII in the Near Infra-Red range, with decay times varying from 1.78 μs to 805 μs at room temperature. The particular luminescence spectroscopic properties of these lanthanide complexes formed with 3,4,3-LI(1,2-HOPO) were used to characterize their respective solution thermodynamic stabilities as well as those of the corresponding LaIII, GdIII, DyIII, HoIII, ErIII, TmIII, and LuIII complexes. The remarkably high affinity of 3,4,3-LI(1,2-HOPO) for lanthanide metal ions and the resulting high complex stabilities (pM values ranging from 17.2 for LaIII to 23.1 for YbIII) constitute a necessary but not sufficient criterion to consider this octadentate ligand an optimal candidate for in vivo metal decorporation. The in vivo lanthanide complex stability and decorporation capacity of the ligand were assessed, using the radioactive isotope 152Eu as a tracer in a rodent model, which provided a direct comparison with the in vitro thermodynamic results and demonstrated the great potential of 3,4,3-LI(1,2-HOPO) as a therapeutic metal chelating agent.

Graphical abstract: 3,4,3-LI(1,2-HOPO): In vitro formation of highly stable lanthanide complexes translates into efficacious in vivoeuropium decorporation

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Supplementary files

Article information


Submitted
04 May 2011
Accepted
06 Jun 2011
First published
15 Jul 2011

Dalton Trans., 2011,40, 8340-8346
Article type
Paper

3,4,3-LI(1,2-HOPO): In vitro formation of highly stable lanthanide complexes translates into efficacious in vivoeuropium decorporation

M. Sturzbecher-Hoehne, C. Ng Pak Leung, A. D'Aléo, B. Kullgren, A. Prigent, D. K. Shuh, K. N. Raymond and R. J. Abergel, Dalton Trans., 2011, 40, 8340
DOI: 10.1039/C1DT10840A

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