dc.contributor.author | Mokaleng, Botshelo B. | |
dc.contributor.author | Zeevaart, Jan R. | |
dc.contributor.author | Ebenhan, Thomas | |
dc.contributor.author | Ramesh, Suhas | |
dc.contributor.author | Govender, Thavendran | |
dc.date.accessioned | 2016-08-22T08:30:54Z | |
dc.date.available | 2016-08-22T08:30:54Z | |
dc.date.issued | 2015 | |
dc.identifier.citation | Mokaleng, B.B. et al. 2015. Synthesis, 68Ga-radiolabeling, and preliminary in vivo assessment of a depsipeptide-derived compound as a potential PET/CT infection imaging agent. BioMed research international, 2015: Article no 284354. [https://doi.org/10.1155/2015/284354] | |
dc.identifier.issn | 2314-6133 | |
dc.identifier.issn | 2314-6141 (Online) | |
dc.identifier.uri | http://hdl.handle.net/10394/18350 | |
dc.identifier.uri | http://www.hindawi.com/journals/bmri/2015/284354/ | |
dc.identifier.uri | https://doi.org/10.1155/2015/284354 | |
dc.description.abstract | Noninvasive imaging is a powerful tool for early diagnosis and monitoring of various disease processes, such as infections. An
alarming shortage of infection-selective radiopharmaceuticals exists for overcoming the diagnostic limitations with unspecific
tracers such as 67/68Ga-citrate or 18F-FDG. We report here TBIA101, an antimicrobial peptide derivative that was conjugated to
DOTA and radiolabeled with 68Ga for a subsequent in vitro assessment and in vivo infection imaging using Escherichia coli-bearing
mice by targeting bacterial lipopolysaccharides with PET/CT. Following DOTA-conjugation, the compound was verified for its
cytotoxic and bacterial binding behaviour and compound stability, followed by 68Gallium-radiolabeling. 𝜇PET/CT using 68Ga-
DOTA-TBIA101 was employed to detect muscular E. coli-infection in BALB/c mice, as warranted by the in vitro results. 68Ga-
DOTA-TBIA101-PET detected E. coli-infected muscle tissue (SUV = 1.3–2.4) > noninfected thighs (𝑃 = 0.322) > forearm muscles
(𝑃 = 0.092) > background (𝑃 = 0.021) in the same animal. Normalization of the infected thigh muscle to reference tissue showed
a ratio of 3.0 ± 0.8 and a ratio of 2.3 ± 0.6 compared to the identical healthy tissue. The majority of the activity was cleared by
renal excretion.The latter findings warrant further preclinical imaging studies of greater depth, as the DOTA-conjugation did not
compromise the TBIA101’s capacity as targeting vector | en_US |
dc.description.sponsorship | Department of Nuclear
Medicine at the University of Pretoria; Catalysis & Peptide Research Unit and the Department of
Virology at the University of KwaZulu-Natal; Department of Science and
Technology (DST) | en_US |
dc.language.iso | en | en_US |
dc.publisher | Hindawi | en_US |
dc.title | Synthesis, 68Ga-radiolabeling, and preliminary in vivo assessment of a depsipeptide-derived compound as a potential PET/CT infection imaging agent | en_US |
dc.type | Article | en_US |
dc.contributor.researchID | 16951484 - Zeevaart, Jan Rijn | |