C60 fullerene as synergistic agent in tumor-inhibitory Doxorubicin treatment

Svitlana Prylutska 1, Iryna Grynyuk, Olga Matyshevska, Yuriy Prylutskyy, Maxim Evstigneev, Peter Scharff, Uwe Ritter

 Dox (total dose 2.5 mg/kg) combined with C60 fullerene (total dose 25 mg/kg) in tumor-bearing animals resulted in tumor growth inhibition, prolongation of life, metastasis inhibition, and increased number of apoptotic tumor cells and was more effective than the corresponding course of Dox treatment alone. C60 fullerene demonstrated a protective effect against superoxide dismutase and glutathione peroxidase inhibition induced by Dox-dependent oxidative insult in the liver and heart.


Medicinal applications of fullerenes

Rania Bakry, Rainer M Vallant, Muhammad Najam-ul-Haq, Matthias Rainer, Zoltan Szabo, Christian W Huck, and Günther K Bonn

Compounds with antiviral activity are generally of great medical interest and different modes of pharmaceutical actions have been described. Replication of the human immunodeficiency virus (HIV) can be suppressed by several antiviral compounds, which are effective in preventing or delaying the onset of acquired immunodeficiency syndrome (AIDS). Fullerenes (C60) and their derivatives have potential antiviral activity, which has strong implications on the treatment of HIV-infection. The antiviral activity of fullerene derivatives is based on several biological properties including their unique molecular architecture and antioxidant activity.

Fullerenes have unusual redox chemistry and may be reversibly reduced by up to six electrons. These, along with the low toxicity detected so far in fullerenes, are sufficient to stimulate researchers in chemistry and in biology to unite their efforts and systematically investigate the biological properties of these fascinating molecules. A wave of research and development activities all over the world has led to large number of application-oriented patents, spanning a very broad range spectrum of potential commercial applications, including: anticancer anticancer drug delivery systems using photodynamic therapy, HIV drugs, and cosmetics to slow down the aging of human skin.

Improve Cognitive Function

A carboxyfullerene SOD mimetic improves cognition and extends the lifespan of mice

Kevin L Quick 1, Sameh S Ali, Robert Arch, Chengjie Xiong, David Wozniak, Laura L Dugan

We administered a small-molecule synthetic enzyme superoxide dismutase (SOD) mimetic to wild-type (i.e. non-transgenic, non-senescence accelerated) mice starting at middle age. Chronic treatment not only reduced age-associated oxidative stress and mitochondrial radical production, but significantly extended lifespan. Treated mice also exhibited improved performance on the Morris water maze learning and memory task. This is to our knowledge the first demonstration that an administered antioxidant with mitochondrial activity and nervous system penetration not only increases lifespan, but rescues age-related cognitive impairment in mammals. SOD mimetics with such characteristics may provide unique complements to genetic strategies to study the contribution of oxidative processes to nervous system aging.

Improve Cognitive Function

Fullerene-based antioxidants and neurodegenerative disorders

L L. Dugan 1, E G. Lovett, K L. Quick, J Lotharius, T T. Lin, K L. O'Malley

Carboxyfullerenes demonstrated robust neuroprotection against excitotoxic, apoptotic and metabolic insults in cortical cell cultures. They were also capable of rescuing mesencephalic dopaminergic neurons from both MPP(+) and 6-hydroxydopamine-induced degeneration. Although there is limited in vivo data on these compounds to date, we have previously reported that systemic administration of the C(3) carboxyfullerene isomer delayed motor deterioration and death in a mouse model of familial amyotrophic lateral sclerosis (FALS). Ongoing studies in other animal models of CNS disease states suggest that these novel antioxidants are potential neuroprotective agents for other neurodegenerative disorders, including Parkinson’s disease.

Reduces Osteoarthritis

The applications of buckminsterfullerene C60 and derivatives in orthopaedic research

Qihai Liu 1, Quanjun Cui, Xudong Joshua Li, Li Jin

Buckminsterfullerene C60 and derivatives have been extensively explored in biomedical research due to their unique structure and unparalleled physicochemical properties. C60 is characterized as a “free radical sponge” with an anti-oxidant efficacy several hundred-fold higher than conventional anti-oxidants. Also, the C60 core has a strong electron-attracting ability and numerous functional compounds with widely different properties can be added to this fullerene cage. This review focused on the applications of C60 and derivatives in orthopaedic research, such as the treatment of cartilage degeneration, bone destruction, intervertebral disc degeneration (IVDD), vertebral bone marrow disorder, radiculopathy, etc., as well as their toxicity in vitro and in vivo.