Study of the Cytotoxic Effects of the New Synthetic Isothiocyanate CM9 and Its Fullerene Derivative on Human T-Leukemia Cells

Toxins

Elena De Gianni⁴  Eleonora Turrini¹  Andrea Milelli¹  Francesca Maffei¹  Marco Carini³  Anna Minarini²  Vincenzo Tumiatti¹  Tatiana Da Ros³  Maurizio Prato³  Carmela Fimognari¹ 

[1] Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d’Augusto 237, 47921 Rimini, Italy; E-Mails:;Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, via Belmeloro 6, 40126 Bologna, Italy; E-Mail:;Department of Chemical and Pharmaceutical Sciences, University of Trieste, Piazzale Europa 1, 34127 Trieste, Italy; E-Mails:;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; E-Mail:

关键词: fullerene;    isothiocyanate;    naphthalene diimide;    cancer;    apoptosis;    cell proliferation;    p53;    doxorubicin;    genotoxicity;   

DOI  :  10.3390/toxins7020535

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.