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Cancer Biother Radiopharm ; 26(5): 623-30, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21950558

RESUMO

The current study was aimed at synthesizing a glucuronide derivative of D-penicillamine (D-PA) to be used for imaging purposes. First of all, D-PA-glucuronide (D-PA-Glu) was synthesized by experimental treatments starting with uridine 5'-diphospho-glucuronosyltransferase enzyme rich microsome preparate. Then, the synthesized compound was labeled with technetium ((99m)Tc) by using a reduction method with stannous chloride. Quality controls were performed by using high-performance liquid chromatography and thin-layer radio chromatography (TLRC). Radiolabeling yield of (99m)Tc-D-PA-Glu was more than 98% according to TLRC results. In vitro evaluations of radiolabeled complexes were investigated on PC-3 human prostate cancer cells. (99m)Tc-D-PA-Glu exhibited more accumulation on PC-3 cells versus (99m)Tc-D-PA at 240 minutes. In order to determine its radiopharmaceutical potential, biodistribution studies were carried out in male Albino Wistar rats. The biodistribution results of (99m)Tc-D-PA-Glu, showed the highest uptake in prostate at 120 minutes postinjection with the main excretion route being through kidneys and bladder. (99m)Tc-D-PA-Glu and (99m)Tc-D-PA have exhibited different biodistribution results.


Assuntos
Glucuronídeos/síntese química , Compostos de Organotecnécio/síntese química , Penicilamina/análogos & derivados , Tecnécio/química , Animais , Linhagem Celular Tumoral , Cromatografia Líquida de Alta Pressão , Glucuronídeos/química , Glucuronídeos/farmacocinética , Humanos , Masculino , Espectrometria de Massas , Compostos de Organotecnécio/química , Compostos de Organotecnécio/farmacocinética , Penicilamina/síntese química , Penicilamina/química , Penicilamina/farmacocinética , Neoplasias da Próstata/metabolismo , Ratos , Ratos Wistar , Distribuição Tecidual
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