comparative biodistribution profile of [131i]vip and [131i]vip10-28

Clicks: 253
ID: 256958
2005
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Abstract
Various tumor cells express significantly higher amounts of VIP receptors (VIPR) that provided the basis for the clinical use of radiolabeled VIP for the in vivo localization of tumors. This work studied the labeling of VIP and VIP10-28 with iodine-131 to compare the biological distribution of the labeled compounds in Nuce mice and the affinity for tumor cells. Both VIP and VIP10-28 peptides contain two tyrosine residues, in positions 10 and 22, that are theoretically equally susceptible to radioiodination employing oxidative electrophilic substitution using oxidizing agents like Chloramine T. Radiochemical purity of the reaction mixture was determined by electrophoresis and HPLC. The VIP peptide and the fragment were labeled with radioiodine with good radiochemical yield (above 96%). Suitable, but important differences can be observed in biological distribution studies. Comparatively, blood clearance was faster for labeled VIP and perhaps because of this, the uptake in tumor was lower, especially during the first hour. These differences observed in the biological distribution of the compounds can be related to the lipophilicity of the labeled compounds.
Várias células tumorais expressam significantemente uma alta quantidade de receptores VIP (VIPR) que determinam a base para o uso clínico de VIP radiomarcado para localização de tumores in vivo. Foi estudado neste trabalho a marcação do VIP e do fragmento VIP10-28 com iodo-131 comparando a distribuição biológica dos compostos marcados em camundongos Nude e sua afinidade pelas células tumorais. Ambos os peptídeos, VIP e VIP10-28. contém dois resíduos de tirosina nas posições 10 e 22, que teoricamente são igualmente susceptíveis pela substituição eletrofílica oxidativa do radioiodo utilizando Cloramina T como agente oxidante. A pureza radioquímica da mistura de reação foi determinada por eletroforese e cromatografia líquida de alta eficiência (CLAE). O VIP e fragmento foram marcados com radioiodo com bom rendimento radioquímico (superior a 96%). Importantes diferenças foram observadas nos estudos de distribuição biológica. Comparativamente, o clareamento sanguíneo foi mais rápido para VIP marcado e por esta razão, a captação no tumor foi inferior, especialmente na primeira hora. Estas diferenças observadas na distribuição biológica dos compostos podem estar relacionadas com a lipofilicidade dos compostos marcados.
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colturato2005braziliancomparative Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors ;Maria Tereza Colturato;Emiko Muramoto;Elaine Bortoleti de Araújo
Journal current drug delivery
Year 2005
DOI
10.1590/S1516-89132005000700012
URL
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1516-89132005000700012
Keywords
radiopharmaceuticals adenocarcinomasbiotechnology

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