title: Effects of Two Fullerene Derivatives on Monocytes and Macrophages.
abstract: Two fullerene derivatives (fullerenes 1 and 2), bearing a hydrophilic chain on the pyrrolidinic nitrogen, were developed with the aim to deliver anticancer agents to solid tumors. These two compounds showed a significantly different behaviour on human neoplastic cell lines in vitro in respect to healthy leukocytes. In particular, the pyrrolidinium ring on the fullerene carbon cage brings to a more active compound. In the present work, we describe the effects of these fullerenes on primary cultures of human monocytes and macrophages, two kinds of immune cells representing the first line of defence in the immune response to foreign materials. These compounds are not recognized by circulating monocytes while they get into macrophages. The evaluation of the pronecrotic or proapoptotic effects, analysed by means of analysis of the purinergic receptor P2X7 activation and of ROS scavenging activity, has allowed us to show that fullerene 2, but not its analogue fullerene 1, displays toxicity, even though at concentrations higher than those shown to be active on neoplastic cells.
authors.affiliation: Department of Life Sciences, University of Trieste, Via L. Giorgieri 5, 34127 Trieste, Italy.
authors.forename: Sabrina
authors.initials: S
authors.lastname: Pacor
authors.affiliation: Department of Life Sciences, University of Trieste, Via L. Giorgieri 5, 34127 Trieste, Italy.
authors.forename: Alberto
authors.initials: A
authors.lastname: Grillo
authors.affiliation: Department of Chemical and Pharmaceutical Sciences, University of Trieste, Via L. Giorgieri 5, 34127 Trieste, Italy.
authors.forename: Luka
authors.initials: L
authors.lastname: Đorđević
authors.affiliation: Department of Life Sciences, University of Trieste, Via L. Giorgieri 5, 34127 Trieste, Italy.
authors.forename: Sonia
authors.initials: S
authors.lastname: Zorzet
authors.affiliation: Department of Life Sciences, University of Trieste, Via L. Giorgieri 5, 34127 Trieste, Italy.
authors.forename: Marianna
authors.identifier: 0000-0003-1355-3782
authors.initials: M
authors.lastname: Lucafò
authors.affiliation: Department of Chemical and Pharmaceutical Sciences, University of Trieste, Via L. Giorgieri 5, 34127 Trieste, Italy.
authors.forename: Tatiana
authors.initials: T
authors.lastname: Da Ros
authors.affiliation: Department of Chemical and Pharmaceutical Sciences, University of Trieste, Via L. Giorgieri 5, 34127 Trieste, Italy.
authors.forename: Maurizio
authors.initials: M
authors.lastname: Prato
authors.affiliation: Department of Life Sciences, University of Trieste, Via L. Giorgieri 5, 34127 Trieste, Italy ; Callerio Foundation, Institutes of Biological Research, Via A. Fleming 22-31, 34127 Trieste, Italy.
authors.forename: Gianni
authors.identifier: 0000-0002-5138-6041
authors.initials: G
authors.lastname: Sava
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D037741:Fullerenes / Q000008:administration & dosage* / Q000737:chemistry; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008264:Macrophages / Q000187:drug effects*; D009000:Monocytes / Q000187:drug effects; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D009584:Nitrogen / Q000737:chemistry; D058486:Receptors, Purinergic P2X7 / Q000096:biosynthesis / Q000235:genetics
chemical_list: D000970:Antineoplastic Agents; D037741:Fullerenes; D058486:Receptors, Purinergic P2X7; D009584:Nitrogen