dc.contributor.author |
Mokaleng, Botshelo B.
|
|
dc.contributor.author |
Ebenhan, Thomas
|
|
dc.contributor.author |
Ramesh, Suhas
|
|
dc.contributor.author |
Govender, Thavendran
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|
dc.contributor.author |
Kruger, Hendrik G.
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|
dc.contributor.author |
Parboosing, Raveen
|
|
dc.contributor.author |
Hazari, Puja P.
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|
dc.contributor.author |
Mishra, Anil K.
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|
dc.contributor.author |
Marjanovic-Painter, Biljana
|
|
dc.contributor.author |
Zeevaart, Jan Rijn
|
|
dc.contributor.author |
Sathekge, Mike Machaba
|
|
dc.date.accessioned |
2015-12-11T05:33:48Z |
|
dc.date.available |
2015-12-11T05:33:48Z |
|
dc.date.issued |
2015 |
|
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_ZA |
dc.description.librarian |
hb2015 |
en_ZA |
dc.description.sponsorship |
Department of Nuclear Medicine at the University of Pretoria. Department of Science and
Technology. |
en_ZA |
dc.description.uri |
http://www.hindawi.com/journals/bmri/ |
en_ZA |
dc.identifier.citation |
Mokaleng, BB, Ebenhan, T, Ramesh, S, Govender, T, Kruger, HG, Parboosing, R, Hazari, PP, Mishra, AK, Marjanovic-Painter, B, Zeevaart, JR & Sathekge, MM 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, vol. 2015, art. #284354, pp. 1-12. |
en_ZA |
dc.identifier.issn |
2314-6133 (print) |
|
dc.identifier.issn |
2314-6141 (online) |
|
dc.identifier.other |
10.1155/2015/284354 |
|
dc.identifier.uri |
http://hdl.handle.net/2263/51139 |
|
dc.language.iso |
en |
en_ZA |
dc.publisher |
Hindawi Publishing |
en_ZA |
dc.rights |
© 2015 Botshelo B. Mokaleng et al. This is an open access article distributed under the Creative Commons Attribution License. |
en_ZA |
dc.subject |
Radiopharmaceuticals |
en_ZA |
dc.subject |
Infectious diseases |
en_ZA |
dc.subject |
Sterile inflammation |
en_ZA |
dc.subject |
Depsidomycin-derived compounds |
en_ZA |
dc.subject |
Radiolabeling |
en_ZA |
dc.title |
Synthesis, 68Ga-radiolabeling, and preliminary in vivo assessment of a depsipeptide-derived compound as a potential PET/CT infection imaging agent |
en_ZA |
dc.type |
Article |
en_ZA |