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Abstract
Chemical modification of fullerenes to hydrosoluble cluster molecules made fullerenes interesting for biological investigation. Among them, polycarbonated and polyhydroxylated fullerene C60 derivatives showed the most interesting biological activities. In this paper, we present the most important recent results of in vitro and in vivo biological studies with fullerenol C60(OH)24. Fullerenol C60(OH)24 was strong antioxidant: it reacted with superoxide anion radical, hydroxy radical and nitrous oxide radical in chemical and biological systems. Fullerenol C60(OH)24 did not inhibit human breast cancer cell growth at concentrations from 0.8 to 3.45 ?M, but strongly modulated cytotoxic effects of doxorubicin and cis-platinum after 24 and 48 hours of treatment. Radioprotective effects of fullerenol C60(OH)24 were shown in different in vitro and in vivo models. Fullerenol C60(OH)24 (100 mg/kg) protected rat heart from doxorubicin toxicity. Biodistribution studies of fulelrenol were also investigated. Accumulating data from the literature and from our studies suggest that fullerenol, as a nanoparticle might be a new promising pharmaceutical in the near future.
Highlights
Antiproliferative and cytotoxic effects of various water-soluble fullerenol C60(OH)n have been observed in different experimental models [23,24,25,26]
Protective effect of fullerenol was found to be more pronounced against doxorubicin and cisplatin, antitumor drugs whose general toxicity is related to free radical formation
Protective effect of fullerenol in the model of doxorubicininduced cytotoxicity on human breast cancer cell lines could be explained by fullerenol localization close to the mitochondria [35], its free radical scavenger activity, and by the ability to act as an artificial electron acceptor leading to inhibition of monooxygenase activity [34]
Summary
Chemical modification of fullerenes to hydrosoluble cluster molecules made fullerenes interesting for biological investigation. UDC: 577.11:678.048:615.076 Among them, polycarbonated and polyhydroxylated fullerene C60 derivatives showed the most interesting biological activities. C60(OH) was strong antioxidant: it reacted with superoxide anion radical, hydroxy radical and nitrous oxide radical in chemical and biological systems. Radioprotective effects of Kamenica, Serbia fullerenol C60(OH) were shown in different in vitro and in vivo models. Accumulating data from the literature and from our $OHNVDQGDUéRUāHYLþ)DFXOW\RI studies suggest that fullerenol, as a nanoparticle might be a new promising pharmaceutical in the near future. University of Novi Sad, Trg 'RVLWHMD2EUDGRYLþD1RYL Key words: Fulleren; Antioxidants; Doxorubicin; Drug Toxicity; Protective Agents; Radiation-Protective Agents
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