title: (9R)-9-Hydroxystearate-Functionalized Hydroxyapatite as Antiproliferative and Cytotoxic Agent toward Osteosarcoma Cells.
abstract: The possibility to functionalize calcium phosphates with bioactive agents is a promising strategy to design innovative biomaterials for bone repair able to couple the bioactive properties of the inorganic compounds with the therapeutic effect of the functionalizing agent. The R enantiomer of the 9-hydroxystearic acid, (9R)-9-HSA, produced from Dimorphotheca sinuata L. seeds, has proven to act as a natural negative regulator of tumor cell proliferation. On this basis, hydroxyapatite was synthesized with increasing contents of (9R)-9-hydroxystearate, up to ∼8.6 wt %. The incorporation of HSA in the composite nanocrystals induces a reduction of the crystal mean dimensions and of the length of the coherently scattering crystalline domains, which suggest a preferential adsorption onto the hydroxyapatite crystal faces parallel to the c-axis direction. The composite nanocrystals were designed so that their cytostatic and cytotoxic effects toward osteosarcoma cells were modulated by hydroxystearate content. In fact, results of in vitro tests show that the presence of HSA in the composite nanocrystals provokes a significant decrease in SaOS2 osteosarcoma cells proliferation and viability as well as an increase in lactate dehydrogenase, tumor necrosis factor α, and caspase 3 levels, with a cytotoxic effect increasing with HSA content in the nanocrystals.
authors.affiliation: Department of Chemistry "G. Ciamician", University of Bologna , via Selmi 2, 40126 Bologna, Italy.
authors.forename: Elisa
authors.initials: E
authors.lastname: Boanini
authors.affiliation: Laboratory of Preclinical and Surgical Studies, Research Institute Codivilla Putti - Rizzoli Orthopaedic Institute , via di Barbiano, 40136 Bologna, Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Torricelli
authors.affiliation: Department of Industrial Chemistry "Toso Montanari", University of Bologna , Viale del Risorgimento 4, 40136 Bologna, Italy.
authors.forename: Carla
authors.initials: C
authors.lastname: Boga
authors.affiliation: Department of Industrial Chemistry "Toso Montanari", University of Bologna , Viale del Risorgimento 4, 40136 Bologna, Italy.
authors.forename: Gabriele
authors.initials: G
authors.lastname: Micheletti
authors.affiliation: Department of Industrial Chemistry "Toso Montanari", University of Bologna , Viale del Risorgimento 4, 40136 Bologna, Italy.
authors.forename: Maria Cristina
authors.initials: MC
authors.lastname: Cassani
authors.affiliation: Laboratory of Preclinical and Surgical Studies, Research Institute Codivilla Putti - Rizzoli Orthopaedic Institute , via di Barbiano, 40136 Bologna, Italy.
authors.forename: Milena
authors.initials: M
authors.lastname: Fini
authors.affiliation: Department of Chemistry "G. Ciamician", University of Bologna , via Selmi 2, 40126 Bologna, Italy.
authors.forename: Adriana
authors.initials: A
authors.lastname: Bigi
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D001672:Biocompatible Materials / Q000737:chemistry; D002454:Cell Differentiation / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D017886:Durapatite / Q000737:chemistry*; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry; D013229:Stearic Acids / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D001672:Biocompatible Materials; D013229:Stearic Acids; C070375:9-hydroxystearic acid; D017886:Durapatite