Preclinical assessment of a 68Ga-DOTA-functionalized depsipeptide as a radiodiagnostic infection imaging agent

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Authors

Ebenhan, Thomas
Mokaleng, Botshelo B.
Venter, Jacobus Daniel
Kruger, Hendrik Gert
Zeevaart, Jan Rijn
Sathekge, Mike Machaba

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MDPI Publishing

Abstract

The study assessed a radiolabeled depsipeptide conjugate (68Ga-DOTA-TBIA101) for its potential as an imaging agent targeting infection or infection-associated inflammation. 68Ga-labeled DOTA-TBIA101 imaging was performed in (NZR1) healthy rabbits; (NZR2) rabbits bearing muscular sterile inflammation and Staphylococcus aureus (SA) infection; and (NZR3) rabbits infected with Mycobacterium tuberculosis (MTB) combined with a subcutaneous scruff infection of SA in the same animal. All animals were imaged using a PET/CT scanner at 5 and 60 min post injection. Images showed elevated accumulation of 68Ga-DOTA-TBIA101 in the sterile muscular inflammation site (T/NT ratio = 2.6 0.37 (5 min) and 2.8 2.3 (60 min)) and muscles infected with MTB (T/NT ratio = 2.6 0.35 (5 min) and 2.8 0.16 (60 min)). The findings suggest that 68Ga-DOTA-TBIA101-PET/CT may detect MTB-associated inflammation, although more foundational studies need to be performed to rationalize the diagnostic value of this technique.

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Keywords

DOTA-TBIA101, Depsipeptides, Infection, Inflammation, 68Ga/68Ge generator, PET/CT imaging, Tuberculosis (TB)

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Citation

Ebenhan, T., Mokaleng, B.B., Venter, J.D., Kruger, H.G., Zeevaart, J.R. & Sathekge, M. 2017, 'Preclinical assessment of a 68Ga-DOTA-functionalized depsipeptide as a radiodiagnostic infection imaging agent', Molecules, vol. 22, no. 9, art. no. 1403, pp. 1-14.