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

TEKSÖZ S. , Ichedef C. A. , OZYUNCU S., Muftuler F. Z. B. , ÜNAK P. , Medine I. E. , ...Daha Fazla

CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS, cilt.26, ss.623-630, 2011 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 26 Konu: 5
  • Basım Tarihi: 2011
  • Doi Numarası: 10.1089/cbr.2010.0854
  • Sayfa Sayıları: ss.623-630


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.