Review

Bioapplication and activity of fullerenol C₆₀(OH)₂₄

Injac Rade¹*, Radic Natasa¹, Govedarica Biljana², Djordjevic Aleksandar³ and Strukelj Borut¹

¹Faculty of Pharmacy, Institute of Pharmaceutical Biology, University of Ljubljana, Askerceva 7, 1000 Ljubljana, Slovenia.

²Faculty of Pharmacy, Institute of Pharmaceutical Technology, University of Ljubljana, Askerceva 7, 1000 Ljubljana, Slovenia.

³Faculty of Science, Department of Chemistry, University of Novi Sad, Trg Dositeja Obradovica 10, 21000 Novi Sad, Serbia.

*Corresponding author. E-mail: injacrade@gmail.com. Tel: +386 41 964462.         Fax: + 386 1 425803.

Abbreviations: Dox, Doxorubicin; FRL, fullerenol; CK, creatine kinase; ALT, alanine aminotransferase; AST, aspartate aminotransferase; LDH, lactate dehydrogenase; α-HBDH, α-hydroxybutyrate dehydrogenase; MDA, malondialdehyde; GSH, glutathione; GSSG, oxidized glutathione; GSH-Px, glutathione peroxidase; GR, glutathione reductase; CAT, catalase; SOD, superoxide dismutase; ROS, reactive oxygen species; TAS, total antioxidant status.

Accepted 8 December, 2008

Here we summarize current investigations about a relatively new group of compounds mainly composed of carbon atoms - fullerenes and their derivatives. One of the fundamental characteristics of fullerene is its ability to quench various free radicals, behaving as a ‘‘free radical sponge’’. Moreover, the dual nature of fullerenes to act as either quenchers or generators of cell - damaging ROS could be exploited for development of cytoprotective agents on one side or cytotoxic anticancer/antimicrobial agents on the other. In addition, several derivatives have shown immunomodulating, neuroprotective and radioprotective effect. Fullerenes are hydrophobic molecules best dissolved in organic solvents, so potential biomedical applications are restricted by their extremely poor solubility in polar solvents. One of the strategies for improving poor solubility is derivatization. Fullerenol C₆₀(OH)₂₄ is a water-soluble derivative of C₆₀ with improved chemical properties and potential bioapplicability as a free radical scavenger in biological systems, in oxidative stress induced by xenobiotics or radioactive irradiations. However, solubility of C₆₀(OH)₂₄ in water (44 mg/l) is not satisfactory and presents a major drawback in its application as an organo-protector. Improvement of physicochemical characteristics of C₆₀(OH)₂₄ and chronic investigations on different animal models as well as in human trials are recommended for establishing its antioxidant effect.

Key words: Carbon atoms, cytoprotective, derivatization, antioxidant effect.