title: Synthesis and biological evaluation of receptor-based tumor imaging agent: (99m)Tc-folate-glucaric acid.
abstract: The aim of the present study was to prepare (99m)Tc-folate-glucaric acid and investigate the radiopharmaceutical potential for tumors imaging that over express folate receptor. Folate-glucaric acid was synthesized and the synthesized folate conjugate was confirmed with (1)H NMR and LC-MS/MS methods. Folate-glucaric acid was labeled with (99m)Tc, and its radiolabelling efficiency was found as 96 ± 2.0%. Biodistribution study of (99m)Tc-folate-glucaric acid was carried out in vivo using two groups of female Albino Wistar rats: folate receptor (FR) saturated and unsaturated. Biodistribution study showed that (99m)Tc-folate-glucaric acid indicated high uptake in folate receptor rich tissues such as breast, ovary and uterus. Therefore, (99m)Tc-folate-glucaric acid shows good radiolabeling and biodistribution in FR organs, the radiolabeled conjugate is a reason potentially useful radiopharmaceutical for detection of FR-positive tumors.
authors.affiliation: Department of Nuclear Applications, Ege University, Bornova 35100 Izmir, Turkey.
authors.forename: Mehmet
authors.initials: M
authors.lastname: Onursal
authors.forename: Fatma Yurt
authors.initials: FY
authors.lastname: Lambrecht
authors.forename: Aykut
authors.initials: A
authors.lastname: Ozgur
mesh_terms: D000818:Animals; D004355:Drug Stability; D005260:Female; D058973:Folate Receptors, GPI-Anchored / Q000378:metabolism*; D005492:Folic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D007553:Isotope Labeling / Q000379:methods; D009369:Neoplasms / Q000175:diagnosis* / Q000000981:diagnostic imaging*; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D014018:Tissue Distribution
chemical_list: D058973:Folate Receptors, GPI-Anchored; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C568842:technetium 99m folate-glucaric acid; D005492:Folic Acid