99m Tc-D-Penicillamine-Glucuronide: Synthesis, Radiolabeling, In Vitro and In Vivo Evaluation
Makaleler > Tam Makale · 2011
Yazarlar: Serap TEKSÖZ, Çiğdem İÇHEDEF, Seniha OZYUNCU, Fazilet Zümrüt BİBER MÜFTÜLER, Perihan ÜNAK, Emin İlker MEDİNE, Turkan Ertay, Mine Sencan Eren
Cancer Biotherapy and Radiopharmaceuticals, SCI Expanded İndekslerine Giren Dergi, Uluslararası, Wos, 2011, cilt 26, ss 623-630
Özet
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.