title: Fluorine-18 radiolabeling of low-density lipoproteins: a potential approach for characterization and differentiation of metabolism of native and oxidized low-density lipoproteins in vivo.
abstract: Oxidative modification of low-density lipoprotein (LDL) is regarded as a crucial event in atherogenesis. Assessing the metabolic fate of oxidized LDL (oxLDL) in vivo with radiotracer techniques is hindered by the lack of suitable sensitive and specific radiolabeling methods. We evaluated an improved methodology based on the radiolabeling of native LDL (nLDL) and oxLDL with the positron emitter fluorine-18 ((18)F) by conjugation with N-succinimidyl-4-[(18)F]fluorobenzoate ([(18)F]SFB). We investigated whether radiolabeling of LDL induces adverse structural modifications. Results suggest that radiolabeling of both nLDL and oxLDL using [(18)F]SFB causes neither additional oxidative structural modifications of LDL lipids and proteins nor alteration of their biological activity and functionality, respectively. Thus, radiolabeling of LDL using [(18)F]SFB could prove to be a promising approach for studying the kinetics of oxLDL in vivo.
authors.affiliation: PET-Center, Institute of Bioinorganic and Radiopharmaceutical Chemistry, Research Center Rossendorf Dresden, D-01314 Dresden, Germany. j.pietzsch@fz-rossendorf.de
authors.forename: Jens
authors.initials: J
authors.lastname: Pietzsch
authors.forename: Ralf
authors.initials: R
authors.lastname: Bergmann
authors.forename: Katrin
authors.initials: K
authors.lastname: Rode
authors.forename: Christina
authors.initials: C
authors.lastname: Hultsch
authors.forename: Beate
authors.initials: B
authors.lastname: Pawelke
authors.forename: Frank
authors.initials: F
authors.lastname: Wuest
authors.forename: Joerg
authors.initials: J
authors.lastname: van den Hoff
mesh_terms: D001565:Benzoates / Q000493:pharmacokinetics*; D006528:Carcinoma, Hepatocellular / Q000000981:diagnostic imaging* / Q000378:metabolism*; D002460:Cell Line; D005240:Feasibility Studies; D006801:Humans; D008077:Lipoproteins, LDL / Q000493:pharmacokinetics*; D008113:Liver Neoplasms / Q000000981:diagnostic imaging / Q000378:metabolism; D008657:Metabolic Clearance Rate; D009000:Monocytes / Q000000981:diagnostic imaging* / Q000378:metabolism*; D049268:Positron-Emission Tomography / Q000379:methods; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D013388:Succinimides / Q000493:pharmacokinetics*
chemical_list: D001565:Benzoates; D008077:Lipoproteins, LDL; D019275:Radiopharmaceuticals; D013388:Succinimides; C075713:N-succinimidyl-4-fluorobenzoate