ChemInform Abstract: Synthesis and Evaluation of Organosilicon Inhibitors of Active Purine Transport in Human Osteoblasts

Autor:	Gérard Déléris, Sol Ciro, Joëlle Amédée, Karine Estieu-Gionnet, Charles Baquey, Reine Bareille, Laurent Latxague, Cyril Rubio
Rok vydání:	2010
Předmět:	chemistry.chemical_classification chemistry.chemical_compound Biochemistry chemistry Hypoxanthine transport Nucleic acid General Medicine Bone regeneration Michaelis–Menten kinetics Hypoxanthine Alkyl Nucleobase Organosilicon
Zdroj:	ChemInform. 33
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200232218
Popis:	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.
Databáze:	OpenAIRE
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