3 years ago

Multivalent Siderophore–DOTAM Conjugates as Theranostics for Imaging and Treatment of Bacterial Infections

Multivalent Siderophore–DOTAM Conjugates as Theranostics for Imaging and Treatment of Bacterial Infections
Peter P. Müller, Verena Fetz, Kevin Ferreira, Hans Prochnow, Hai-Yu Hu, Bushra Rais, Mark Brönstrup
There is a strong need to better diagnose infections at deep body sites through noninvasive molecular imaging methods. Herein, we describe the synthesis and characterization of probes based on siderophore conjugates with catechol moieties and a central DOTAM scaffold. The probes can accommodate a metal ion as well as an antibiotic moiety and are therefore suited for theranostic purposes. The translocation of the conjugates across the outer and inner cell membranes of E. coli was confirmed by growth recovery experiments with enterobactin-deficient strains, by the antibacterial activity of ampicillin conjugates, and by confocal imaging using a fluorogen-activating protein–malachite green system adapted to E. coli. The suitability of the probes for in vivo imaging was demonstrated with a Cy5.5 conjugate in mice infected with P. aeruginosa. Trojan horses: A siderophore motif was coupled to functional imaging and/or antibiotic moieties via a DOTAM scaffold. The conjugates are internalized into Gram-positive as well as Gram-negative pathogenic bacteria and can be used for multiple theranostic applications, such as the in vivo imaging of infections.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/anie.201701358

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