title: Synthesis and evaluation of organosilicon inhibitors of active purine transport in human osteoblasts.
abstract: In the search for new compounds that might, once incorporated into biomaterials, stimulate the natural processes of bone regeneration, a new series of silicon-containing alkyl nucleobase analogues has been synthesized. An active hypoxanthine transport process in human osteoblasts was demonstrated, with an apparent Michaelis constant of 2.3 microM and a maximum possible rate of 0.47 pmol s(-1) x 10(6) cell. The synthesized analogues were tested for toxicity in human osteoblasts. Nontoxic analogues were tested in competition transport studies with [(14)C]hypoxanthine. Two of them were found to inhibit the active transport of hypoxanthine in human osteoblasts, with IC(50) values of 6.5 and 11.6 microM.
authors.affiliation: INSERM U 443, Université Victor Segalen-Bordeaux 2, 146 rue Léo Saignat, 33076 Bordeaux Cedex, France.
authors.forename: Sol
authors.initials: S
authors.lastname: Ciro
authors.forename: Cyril
authors.initials: C
authors.lastname: Rubio
authors.forename: Karine
authors.initials: K
authors.lastname: Estieu-Gionnet
authors.forename: Laurent
authors.initials: L
authors.lastname: Latxague
authors.forename: Gérard
authors.initials: G
authors.lastname: Déléris
authors.forename: Reine
authors.initials: R
authors.lastname: Bareille
authors.forename: Joëlle
authors.initials: J
authors.lastname: Amédée
authors.forename: Charles
authors.initials: C
authors.lastname: Baquey
mesh_terms: D000328:Adult; D000368:Aged; D001672:Biocompatible Materials / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry*; D001693:Biological Transport, Active / Q000187:drug effects; D002478:Cells, Cultured; D006801:Humans; D008875:Middle Aged; D017646:Organosilicon Compounds / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry*; D010006:Osteoblasts / Q000187:drug effects / Q000378:metabolism*; D011687:Purines / Q000378:metabolism*
chemical_list: D001672:Biocompatible Materials; D017646:Organosilicon Compounds; D011687:Purines