Scientists from Skoltech and the Institute of Problems of Chemical Physics of the Russian Academy of Sciences have created water-soluble fullerene compounds that have valuable biological properties, thanks to which they can be used to develop effective antiviral drugs, including to suppress the human immunodeficiency virus (HIV). The results of the study are published in the journal Chemical Communications.
Fullerenes are molecular compounds composed of three-coordinated carbon atoms, which are convex closed polyhedra. Depending on the number of atoms in a molecule, fullerenes are shaped like a soccer ball (C60) or a rugby ball (C70). Fullerene-based compounds have pronounced antiviral, antibacterial, antitumor, and antioxidant activity; therefore, scientists have long considered them as a promising basis for creating new medicines. Unfortunately, fullerenes are absolutely insoluble in water, which prevents their use in medicine.
Russian scientists led by Professor Pavel Troshin from the Skoltech Center for Energy Technologies, together with Belgian colleagues from the Catholic University of Leuven, have proposed an effective one-step method for obtaining stable water-soluble chlorofullerenes C60Cl6 and C70Cl8, fullerene derivatives with high activity against the human immunodeficiency virus (HIV), comparable to the characteristics of commercial drugs.
The methods that existed before for the preparation of water-soluble fullerene compounds gave a very low yield - usually up to 10 percent - and included several complex technological stages, which was unacceptable for industrial synthesis and made it extremely difficult to create drugs based on them.
The method developed by scientists makes it possible to obtain water-soluble compounds with a yield close to 100 percent without lengthy and laborious chromatographic purification, which opens up new opportunities for the synthesis of fullerene derivatives on any scale required by the pharmaceutical industry.
"Despite the fact that more than 20 years have passed since the discovery of the high antiviral activity of fullerene derivatives, these unique compounds remained inaccessible for clinical trials, since their preparation turned out to be very laborious. We hope that the simple and one-step method proposed by us for the synthesis of water-soluble fullerene compounds will solve this problem and bring us one step closer to the creation of effective antiviral drugs based on them,” the words of the first author of the article, postgraduate student Olga Kraeva, are quoted in a Skoltech press release.
The results obtained within the framework of the study open up new possibilities for the targeted design of water-soluble fullerene derivatives with a given set of properties, which in the future will make it possible to bring a new generation of drugs based on these compounds to the market.