Synthesis, 68Ga-radiolabeling, and preliminary in vivo assessment of a depsipeptide-derived compound as a potential PET/CT infection imaging agent
dc.contributor.author | Mokaleng, Botshelo B. | |
dc.contributor.author | Ebenhan, Thomas | |
dc.contributor.author | Ramesh, Suhas | |
dc.contributor.author | Govender, Thavendran | |
dc.contributor.author | Kruger, Hendrik G. | |
dc.contributor.author | Parboosing, Raveen | |
dc.contributor.author | Hazari, Puja P. | |
dc.contributor.author | Mishra, Anil K. | |
dc.contributor.author | Marjanovic-Painter, Biljana | |
dc.contributor.author | Zeevaart, Jan Rijn | |
dc.contributor.author | Sathekge, Mike Machaba | |
dc.contributor.email | mike.sathekge@up.ac.za | en_ZA |
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 |