Study of the Cytotoxic Effects of the New Synthetic Isothiocyanate CM9 and Its Fullerene Derivative on Human T-Leukemia Cells
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...
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| Format: | Article |
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MDPI AG
2015-02-01
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| Series: | Toxins |
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| Online Access: | http://www.mdpi.com/2072-6651/7/2/535 |
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| author | Elena De Gianni Eleonora Turrini Andrea Milelli Francesca Maffei Marco Carini Anna Minarini Vincenzo Tumiatti Tatiana Da Ros Maurizio Prato Carmela Fimognari |
| author_facet | Elena De Gianni Eleonora Turrini Andrea Milelli Francesca Maffei Marco Carini Anna Minarini Vincenzo Tumiatti Tatiana Da Ros Maurizio Prato Carmela Fimognari |
| author_sort | Elena De Gianni |
| collection | DOAJ |
| description | 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. |
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| issn | 2072-6651 |
| language | English |
| last_indexed | 2024-04-11T22:26:23Z |
| publishDate | 2015-02-01 |
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| series | Toxins |
| spelling | doaj.art-356724fcb6e2411c9bd6c060b00f272b2022-12-22T03:59:38ZengMDPI AGToxins2072-66512015-02-017253555210.3390/toxins7020535toxins7020535Study of the Cytotoxic Effects of the New Synthetic Isothiocyanate CM9 and Its Fullerene Derivative on Human T-Leukemia CellsElena De Gianni0Eleonora Turrini1Andrea Milelli2Francesca Maffei3Marco Carini4Anna Minarini5Vincenzo Tumiatti6Tatiana Da Ros7Maurizio Prato8Carmela Fimognari9Interdepartmental Centre for Industrial Research in Advanced Mechanical Engineering Applications and Materials Technology, Alma Mater Studiorum-University of Bologna, Piazza Malatesta, 29/30, 47923 Rimini, ItalyDepartment for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d'Augusto 237, 47921 Rimini, ItalyDepartment for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d'Augusto 237, 47921 Rimini, ItalyDepartment for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d'Augusto 237, 47921 Rimini, ItalyDepartment of Chemical and Pharmaceutical Sciences, University of Trieste, Piazzale Europa 1, 34127 Trieste, ItalyDepartment of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, via Belmeloro 6, 40126 Bologna, ItalyDepartment for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d'Augusto 237, 47921 Rimini, ItalyDepartment of Chemical and Pharmaceutical Sciences, University of Trieste, Piazzale Europa 1, 34127 Trieste, ItalyDepartment of Chemical and Pharmaceutical Sciences, University of Trieste, Piazzale Europa 1, 34127 Trieste, ItalyDepartment for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d'Augusto 237, 47921 Rimini, ItalyOne 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.http://www.mdpi.com/2072-6651/7/2/535fullereneisothiocyanatenaphthalene diimidecancerapoptosiscell proliferationp53doxorubicingenotoxicity |
| spellingShingle | Elena De Gianni Eleonora Turrini Andrea Milelli Francesca Maffei Marco Carini Anna Minarini Vincenzo Tumiatti Tatiana Da Ros Maurizio Prato Carmela Fimognari Study of the Cytotoxic Effects of the New Synthetic Isothiocyanate CM9 and Its Fullerene Derivative on Human T-Leukemia Cells Toxins fullerene isothiocyanate naphthalene diimide cancer apoptosis cell proliferation p53 doxorubicin genotoxicity |
| title | Study of the Cytotoxic Effects of the New Synthetic Isothiocyanate CM9 and Its Fullerene Derivative on Human T-Leukemia Cells |
| title_full | Study of the Cytotoxic Effects of the New Synthetic Isothiocyanate CM9 and Its Fullerene Derivative on Human T-Leukemia Cells |
| title_fullStr | Study of the Cytotoxic Effects of the New Synthetic Isothiocyanate CM9 and Its Fullerene Derivative on Human T-Leukemia Cells |
| title_full_unstemmed | Study of the Cytotoxic Effects of the New Synthetic Isothiocyanate CM9 and Its Fullerene Derivative on Human T-Leukemia Cells |
| title_short | Study of the Cytotoxic Effects of the New Synthetic Isothiocyanate CM9 and Its Fullerene Derivative on Human T-Leukemia Cells |
| title_sort | study of the cytotoxic effects of the new synthetic isothiocyanate cm9 and its fullerene derivative on human t leukemia cells |
| topic | fullerene isothiocyanate naphthalene diimide cancer apoptosis cell proliferation p53 doxorubicin genotoxicity |
| url | http://www.mdpi.com/2072-6651/7/2/535 |
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