title: Study of the cytotoxic effects of the new synthetic Isothiocyanate CM9 and its fullerene derivative on human T-leukemia cells.
abstract: One important strategy to develop effective anticancer agents is based on natural products. Many active phytochemicals are in human clinical trials and have been used for a long time, alone and in association with conventional anticancer drugs, for the treatment of various types of cancers. A great number of in vitro, in vivo and clinical reports document the multi-target anticancer activities of isothiocyanates and of compounds characterized by a naphthalenetetracarboxylic diimide scaffold. In order to search for new anticancer agents with a better pharmaco-toxicological profile, we investigated hybrid compounds obtained by inserting isothiocyanate group(s) on a naphthalenetetracarboxylic diimide scaffold. Moreover, since water-soluble fullerene derivatives can cross cell membranes thus favoring the delivery of anticancer therapeutics, we explored the cytostatic and cytotoxic activity of hybrid compounds conjugated with fullerene. We studied their cytostatic and cytotoxic effects on a human T-lymphoblastoid cell line by using different flow cytometric assays. In order to better understand their pharmaco-toxicological potential, we also analyzed their genotoxicity. Our global results show that the synthesized compounds reduced significantly the viability of leukemia cells. However, the conjugation with a non-toxic vector did not increase their anticancer potential. This opens an interesting research pattern for certain fullerene properties.
authors: Interdepartmental Centre for Industrial Research in Advanced Mechanical Engineering Applications and Materials Technology, Alma Mater Studiorum-University of Bologna, Piazza Malatesta, 29/30, 47923 Rimini, Italy. elena.degianni2@unibo.it.
authors: Elena
authors: E
authors: De Gianni
authors: Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d'Augusto 237, 47921 Rimini, Italy. eleonora.turrini@unibo.it.
authors: Eleonora
authors: E
authors: Turrini
authors: Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d'Augusto 237, 47921 Rimini, Italy. andrea.milelli3@unibo.it.
authors: Andrea
authors: A
authors: Milelli
authors: Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d'Augusto 237, 47921 Rimini, Italy. francesca.maffei@unibo.it.
authors: Francesca
authors: F
authors: Maffei
authors: Department of Chemical and Pharmaceutical Sciences, University of Trieste, Piazzale Europa 1, 34127 Trieste, Italy. marco_carini@yahoo.it.
authors: Marco
authors: M
authors: Carini
authors: Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, via Belmeloro 6, 40126 Bologna, Italy. anna.minarini@unibo.it.
authors: Anna
authors: A
authors: Minarini
authors: Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d'Augusto 237, 47921 Rimini, Italy. vincenzo.tumiatti@unibo.it.
authors: Vincenzo
authors: V
authors: Tumiatti
authors: Department of Chemical and Pharmaceutical Sciences, University of Trieste, Piazzale Europa 1, 34127 Trieste, Italy. daros@units.it.
authors: Tatiana Da
authors: TD
authors: Ros
authors: Department of Chemical and Pharmaceutical Sciences, University of Trieste, Piazzale Europa 1, 34127 Trieste, Italy. prato@units.it.
authors: Maurizio
authors: M
authors: Prato
authors: Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d'Augusto 237, 47921 Rimini, Italy. carmela.fimognari@unibo.it.
authors: Carmela
authors: C
authors: Fimognari
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004249:DNA Damage; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000737:chemistry*; D055808:Drug Discovery; D005434:Flow Cytometry; D037741:Fullerenes / Q000737:chemistry*; D006801:Humans; D007094:Imides / Q000737:chemistry*; D017879:Isothiocyanates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D019169:Jurkat Cells; D015394:Molecular Structure; D009281:Naphthalenes / Q000737:chemistry*; D012995:Solubility
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D037741:Fullerenes; D007094:Imides; D017879:Isothiocyanates; D009281:Naphthalenes; C570715:naphthalenetetracarboxydiimide