Prospects for the use of fullerene C60 in medicine

The alchemy of "magic soot"

Dmitry Dzhagarov, "Biomolecule"In 1985, a molecule consisting of 60 carbon atoms, arranged like a football, was discovered – fullerene, named after engineer Richard Fuller, who became famous for designs of exactly this shape.

In addition to its surprisingly symmetrical shape, this molecule, which is the third (after diamond and graphite) allotropic form of carbon, turned out to be something like the philosopher's stone of alchemists [1].

Until recently, it has not ceased to amaze scientists with its extremely low toxicity [2, 3] (especially compared to something similar arranged nanotubes [4]) and other amazing properties [5]. The mechanisms of interaction of fullerenes with cells are not yet clear, but the result can truly be called magic [6].

Here is a far from complete list of those properties that interested doctors and biologists. Fullerene and its derivatives can be used:

• to protect the body from radiation and ultraviolet radiation [7, 8];
• to protect against viruses [9] and bacteria [10];
• to protect against allergies [11]. Thus, in vivo experiments, the introduction of fullerene derivatives inhibits anaphylaxis in mice, and no toxic effect is observed.;
• as a substance that stimulates immunity [12];
• as a powerful antioxidant [13], since it is an active acceptor of radicals. The antioxidant activity of fullerene is comparable to the action of antioxidants of the SkQ class ("Skulachev ions") and is 100-1000 times higher than the action of conventional antioxidants, such as vitamin E, butylhydroxytoluene, β-carotene;
• as drugs for the fight against cancer [14, 15];
• to inhibit angiogenesis [16];
• to protect the brain from alcohol [17, 18];
• to stimulate nerve growth;
• to stimulate skin regeneration processes. Thus, fullerene is an important component of cosmetic anti-aging products GRS and CEFINE;
• to stimulate hair growth [19];
• as a drug with an antiamyloid effect [20].

In addition, fullerene can be used for the delivery of various drugs into the cell [21] and non-viral delivery of genetic vectors into the cell nucleus [22, 23].

It would seem, where else to expand this list, but recently it has been replenished with another, perhaps the most amazing and incomprehensible, quality of fullerene C60. When studying the toxicity of fullerene C60 dissolved in olive oil, French researchers found that rats regularly receiving a solution of fullerene C60 live longer than those who were given just olive oil or a regular diet [24]. (A brief retelling can be read in the article "Olive oil with fullerenes – the elixir of youth?" – VM.)

Dissolution in oil dramatically increases the efficiency of fullerene C60, since its large aggregates (16 or more molecules) are not able to penetrate into cells [25].

At the same time, life expectancy did not increase by any 20-30%, as in experiments with the best of the "medicines for old age" (such as resveratrol or rapamycin), but at least twice [24]! Half of the animals treated with fullerene lived up to 60 months (the oldest rat lived up to 5.5 years). At the same time, in the control group (with a normal diet), the life expectancy of 50% of the animals was 30 months, and the oldest lived only up to 37 months. Animals that received olive oil without fullerene lived a little longer – 50% of them lived up to 40 months, and the oldest rat lived up to 58 months.

Survival diagram of rats treated with: a normal diet (blue line), in addition to a diet of olive oil (red) and olive oil with C60 fullerene dissolved in it (black line). Figure from [24].

The authors of the article attribute the life-giving effect of fullerene C60 to its antioxidant properties. However, it is possible that it may be related to the ability of fullerene C60 to interact with vitamin A [26]. It is known that retinoids (including vitamin A) play an important role in the expression of key genes of the immune system, and that local synthesis of retinoids, apparently, plays a key role in the regulation of embryogenesis and regeneration [27, 28].

Unfortunately, these experiments were performed on small groups of animals and therefore require careful verification. Given the fact that purified fullerene C60, produced in Russia, costs only about 1800 rubles per gram, it is not so difficult to repeat these experiments, clarify the dosages and duration of "treatment". Something else is more complicated. Will this "old age therapy" be as effective for humans? After all, people are not rats, and there are dozens of examples that a drug that works very effectively in experiments on mice turned out to be completely useless (if not harmful!) when the tests were transferred to the clinic. Well, time will tell. It would also be interesting to compare the life-prolonging activity of fullerene C60 with its numerous water-soluble analogues synthesized in Russia recently.

Written based on the materials of the original article [24].

LiteratureA.V. Yeletsky, B.M. Smirnov.

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Portal "Eternal youth" http://vechnayamolodost.ru25.05.2012