title: 99mTc-d-penicillamine-glucuronide: synthesis, radiolabeling, in vitro and in vivo evaluation.
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 ((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.
authors.affiliation: Ege University Institute of Nuclear Sciences, Ankara Street, Bornova, Izmir, Turkey. serap.teksoz@ege.edu.tr
authors.forename: Serap
authors.initials: S
authors.lastname: Teksöz
authors.forename: Ciğdem Acar
authors.initials: CA
authors.lastname: Içhedef
authors.forename: Seniha
authors.initials: S
authors.lastname: Ozyüncü
authors.forename: Fazilet Zümrüt Biber
authors.initials: FZ
authors.lastname: Müftüler
authors.forename: Perihan
authors.initials: P
authors.lastname: Unak
authors.forename: Ilker Emin
authors.initials: IE
authors.lastname: Medine
authors.forename: Türkan
authors.initials: T
authors.lastname: Ertay
authors.forename: Mine Şencan
authors.initials: MŞ
authors.lastname: Eren
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D020719:Glucuronides / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D008297:Male; D013058:Mass Spectrometry; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D010396:Penicillamine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D011471:Prostatic Neoplasms / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D013667:Technetium / Q000737:chemistry*; D014018:Tissue Distribution
chemical_list: D020719:Glucuronides; D015609:Organotechnetium Compounds; D013667:Technetium; D010396:Penicillamine