Tc-99m-D-Penicillamine-Glucuronide: Synthesis, Radiolabeling, In Vitro and In Vivo Evaluation

TEKSÖZ S., İÇHEDEF Ç., Ozyuncu S., BİBER MÜFTÜLER F. Z., ÜNAK P., MEDİNE E. İ., ...More

CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS, vol.26, no.5, pp.623-630, 2011 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 26 Issue: 5
  • Publication Date: 2011
  • Doi Number: 10.1089/cbr.2010.0854
  • Journal Name: CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.623-630
  • Keywords: glucuronidation, PC-3 cell line, penicillamine, radiolabeling, scintigraphy, Tc-99m, BETA-GLUCURONIDASE
  • Dokuz Eylül University Affiliated: Yes

Abstract

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 (Tc-99m) 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 Tc-99m-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. Tc-99m-D-PA-Glu exhibited more accumulation on PC-3 cells versus Tc-99m-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 Tc-99m-D-PA-Glu, showed the highest uptake in prostate at 120 minutes postinjection with the main excretion route being through kidneys and bladder. Tc-99m-D-PA-Glu and Tc-99m-D-PA have exhibited different biodistribution results.