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Molecules 2017, 22(9), 1403; doi:10.3390/molecules22091403

Preclinical Assessment of a 68Ga-DOTA-Functionalized Depsipeptide as a Radiodiagnostic Infection Imaging Agent

1
University of Pretoria & Steve Biko Academic Hospital, Crn Malherbe and Steve Biko Rd, Pretoria 0001, South Africa
2
South African Medical Research Council, 1 Southpansberg Road, Pretoria 0001, South Africa
3
School of Health Sciences, Catalysis and Peptide Research Unit, University of KwaZulu Natal, E-block 6th Floor, Westville Campus, University Rd, Westville, Durban 3630, South Africa
4
Department of Science and Technology, Preclinical Drug Development Platform, North West University, 11 Hoffman St, Potchefstroom 2520, South Africa
*
Author to whom correspondence should be addressed.
Received: 30 May 2017 / Accepted: 18 August 2017 / Published: 24 August 2017
(This article belongs to the Special Issue Peptide-Based Drugs and Drug Delivery Systems)
View Full-Text   |   Download PDF [1926 KB, uploaded 24 August 2017]   |  

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. View Full-Text
Keywords: DOTA-TBIA101; depsipeptides; infection; inflammation; tuberculosis; 68Ga/68Ge generator; PET/CT imaging DOTA-TBIA101; depsipeptides; infection; inflammation; tuberculosis; 68Ga/68Ge generator; PET/CT imaging
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Ebenhan, T.; Mokaleng, B.B.; Venter, J.D.; Kruger, H.G.; Zeevaart, J.R.; Sathekge, M. Preclinical Assessment of a 68Ga-DOTA-Functionalized Depsipeptide as a Radiodiagnostic Infection Imaging Agent. Molecules 2017, 22, 1403.

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