Polyhydroxylated Fullerenes and Their Applications in Medicine

Recently, much attention has been paid to the bioactive properties of water-soluble fullerene derivatives since their discovery: polyhydroxylated fullerenes, with emphasis on their pro- and antioxidative properties and their potential applications have been widely studied in various fields of science. This causes particular interest in developing available and simple methods for the synthesis of water-soluble polyhydroxylated fullerene derivatives on an industrial scale as well as investigating the physicochemical and biological properties and principles of their application.

Due to their hydrophilic properties and the ability to scavenge free radicals, polyhydroxylated fullerenes may, in the future, provide a serious alternative to the currently used pharmacological methods in chemotherapy, treatment of neurodegenerative diseases, and radiobiology. Additionally, due to the hollow spherical shape, polyhydroxylated fullerenes may be used as drug carriers. Polyhydroxylated fullerenes show antimicrobial activity as well, it showed significant antimicrobial activity against Propionibacterium acnes, Staphylococcus epidermidis, Candida albicans, and Malassezia furfur, which suggests that polyhydroxylated fullerenes show antimicrobial activity via the inhibition of microbial cell growth.

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. Polyhydroxylated fullerenes may counteract the harmful effects of anthracyclines by scavenging free radicals and thereby improve the effects of chemotherapy.

The unique electronic properties of fullerenes are attributed to the large numbers of conjugated double π- bonds. Due to the low energy of its lowest unoccupied molecular orbital (LUMO), fullerenes react with various reactive oxygen species (ROS), such as free radicals.

Unique Properties of Polyhydroxylated Fullerenes:

Fullerenes with various numbers of hydroxyl groups have been reported previously. Fullerenes with fewer than 12 hydroxyl groups have poor water solubility. Increasing the number of hydroxyl groups of polyhydroxylated fullerenes can improve their water solubility. Polyhydroxylated fullerenescomprise with more than 40 hydroxyl groups on the fullerene cage and more than eight secondary bound water molecules. Polyhydroxylated fullerenes exhibits a high water solubility of up to 58.9 mg/mL under neutral pH conditions.

Polyhydroxylated fullerene applications:

Polyhydroxylated fullerene is used in rubber/film material modifiers.

Polyhydroxylated fullerene is used in cosmetics.

Polyhydroxylated fullerene is used in anti-HIV drugs.

Polyhydroxylated fullerene is used in anti-cancer drugs.

Polyhydroxylated fullerene is used in nuclear magnetic resonance imaging

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