Fullerenols as a New Therapeutic Approach in Nanomedicine

Abstract

Recently, much attention has been paid to the bioactive properties of water-soluble fullerene derivatives: fullerenols, with emphasis on their pro- and antioxidative properties. Due to their hydrophilic properties and the ability to scavenge free radicals, fullerenols may, in the future, provide a serious alternative to the currently used pharmacological methods in chemotherapy, treatment of neurodegenerative diseases, and radiobiology. Some of the most widely used drugs in chemotherapy are anthracycline antibiotics. Anthracycline therapy, in spite of its effective antitumor activity, induces systemic oxidative stress, which interferes with the effectiveness of the treatment and results in serious side effects. Fullerenols may counteract the harmful effects of anthracyclines by scavenging free radicals and thereby improve the effects of chemotherapy. Additionally, due to the hollow spherical shape, fullerenols may be used as drug carriers. Moreover, because of the existence of the currently ineffective ways for neurodegenerative diseases treatment, alternative compounds, which could prevent the negative effects of oxidative stress in the brain, are still sought. In the search of alternative methods of treatment and diagnosis, today's science is increasingly reaching for tools in the field of nanomedicine, for example, fullerenes and their water-soluble derivatives, which is addressed in the present paper.

Bioluminescent Enzymatic Assay as a Tool for Studying Antioxidant Activity and Toxicity of Bioactive Compounds

“…Being bioactive compounds, fullerenols can produce either toxic or activating effect (3)(4)(5)(6). The biological activity of a series of fullerenols C 60 (OH) [12][13][14] , C 60 (OH) [18][19][20][21][22][23][24] , C 60 (OH) [30][31][32][33][34][35][36][37][38] was studied by Eropkin and coworkers (3).…”

“…The biological activity of a series of fullerenols C 60 (OH) [12][13][14] , C 60 (OH) [18][19][20][21][22][23][24] , C 60 (OH) [30][31][32][33][34][35][36][37][38] was studied by Eropkin and coworkers (3). Fullerenols C 60 (OH) [18][19][20][21][22][23][24] have revealed maximal biological activity (4,7,8). Fullerenols demonstrated antioxidant activity, neutralizing reactive oxygen and nitrogen species (5,8,9), correcting neurological diseases (4,5,9,10), as well as functioning as radioprotectors (9) or antitumor agents (6).…”

“…Fullerenols C 60 (OH) [18][19][20][21][22][23][24] have revealed maximal biological activity (4,7,8). Fullerenols demonstrated antioxidant activity, neutralizing reactive oxygen and nitrogen species (5,8,9), correcting neurological diseases (4,5,9,10), as well as functioning as radioprotectors (9) or antitumor agents (6).…”

Suppression of synaptic plasticity by fullerenol in rat hippocampus in vitro

“…9,10 Hence, several studies reported that fullerenol and other fullerene derivatives may be used as drug carriers, 11,12 neuroprotective agents, 13,14 bioimaging contrast agents, [15][16][17][18][19] and anticancer drugs. [20][21][22] Despite convincing evidence of the potential value of fullerenol in biomedicine, [23][24][25][26][27][28] the data pertaining to its side effects are inadequate. Hippocampal synapse represents/is a model system to study the mechanisms of learning and memory in the brain.…”

Carbon Nanomaterials Alter Global Gene Expression Profiles

“…Because hydroxyl groups are polar, polyhydroxylation overcomes the problem of the poor dispersion of fullerenes in polar solvents such as water, greatly increasing their biological activity as well as providing several novel and interesting properties. 18 20 Fullerenols have been shown to enhance cellular defenses against oxidation through bonding with reactive oxygen species as well as through modulating expression of oxidative stress-induced enzymes. 21 In addition, through molecular modeling and in vitro experimentation, fullerenols have been shown to bind to plasma membrane-bound proteins as well as to bind directly to the phosphate backbone of double-stranded DNA, providing the potential for fullerenols to be used in important biological applications.…”