title: Preliminary evaluation of two radioiodinated maleimide derivatives targeting peripheral and membrane sulfhydryl groups for in vitro cell labeling.
abstract: A factor impeding the advancement of cell mediated therapy is the inability to track these cells in vivo by noninvasive techniques. It has been shown that cells express high levels of sulfhydryl groups. We sought to explore these groups to covalently label cells with radiolabeled maleimide derivatives. Two maleimide derivatives; N-[2-(2,5-dioxoazolinyl)ethyl](5-iodo(3-pyridyl))carboxamide and N-[2-(2,5-dioxoazolinyl)ethyl](3-iodophenyl)carboxamide ([(125)I]-4 and [(125)I]-8) were synthesized and radioiodinated. These compounds were evaluated for in vitro binding to neutrophils, endothelial and mesenchymal stem cells, and biodistribution of the radiolabeled stem cells in nude mice. These radiotracers were obtained in moderate to high radiochemical yields. Binding to cells were moderate (20-60%/10(6) cells) and the label was retained, although washout (an average of 18-55%) was observed depending on the cell type and the tracer used. The labeled cells initially localized in well perfused organs and at a later time showed a general distribution as expected. The novel tracers labeled several cell types and shown that the stability of the label and viability of the cells were maintained in vitro and in vivo for a reasonable period and warrant further in vivo investigation.
authors.affiliation: Cyclotron and Radiopharmaceuticals Department, P.O. Box 3354, Riyadh 11211, Saudi Arabia. amarjk48@hotmail.com
authors.forename: John K
authors.initials: JK
authors.lastname: Amartey
authors.forename: Ranjit S
authors.initials: RS
authors.lastname: Parhar
authors.forename: Yufei
authors.initials: Y
authors.lastname: Shi
authors.forename: Futwan
authors.initials: F
authors.lastname: Al-Mohanna
mesh_terms: D000818:Animals; D001681:Biological Assay; D002460:Cell Line; D002470:Cell Survival; D006801:Humans; D007457:Iodine Radioisotopes / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008301:Maleimides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013058:Mass Spectrometry; D051379:Mice; D008819:Mice, Nude; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013438:Sulfhydryl Compounds / Q000378:metabolism*; D014018:Tissue Distribution
chemical_list: D007457:Iodine Radioisotopes; D008301:Maleimides; D019275:Radiopharmaceuticals; D013438:Sulfhydryl Compounds