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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
Biodistribution and pharmacokinetics of I-131 Labelled 4-Iodophenylacetic Acid
Current Radiopharmaceuticals, Volume 5, No. 4, Year 2012
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Description
Phenylacetate has been reported to have a potent anti-proliferative and anti-differentiating effect in haematological malignancies and in solid tumours at non-toxic concentrations. This study is a preliminary investigation of 131I-radiolabelled 4-iodophenylacetic acid as a potential radiopharmaceutical equivalent. Radiolabelling by isotope exchange gave a radiochemical yield of 53 ± 6 %, and a radiochemical purity of 97.8 ± 1.2 %, as qualified by HPLC. The labelled product was used in Sprague Dawley rats and athymic nude (balb/c) mice xenografted with WHCO1 cells (an oesophageal cancer cell line). Dynamic and static scans were carried out on rats with a SPECT camera to determine the biodistribution of 4-[131I]-iodophenylacetic acid. No target organ was found after 5 h with fast excretion from all organs via the kidney into the urine. Ex vivo studies (termination 5 h after injection) were performed in 12 xenograft mice carrying tumours of 5-8 mm on their right flank. Tumour uptake of 4 + 0.4 % ID/g was recorded with a tumour to background ratio of 2. As the blood pool still contains high levels of activity after 5 h in mice, increased tumour uptake may occur at later time points, which might warrant further investigation. © 2012 Bentham Science Publishers.
Authors & Co-Authors
Zeevaart, Jan Rijn
South Africa, Potchefstroom
North-west University
Szücs, Z.
Hungary, Debrecen
Atommagkutató Intézet
South Africa, Pretoria
Necsa
Pulker, Tamsyn
South Africa, Pretoria
University of Pretoria
Sello, Thato S.
South Africa, Pretoria
Necsa
Bracher, Jacqueline
South Africa, Cape Town
University of Cape Town
Sathekge, Mike Machaba
South Africa, Pretoria
Steve Biko Academic Hospital
Statistics
Citations: 6
Authors: 6
Affiliations: 6
Identifiers
Doi:
10.2174/1874471011205040356
e-ISSN:
18744729
Research Areas
Cancer
Environmental