Synthesis and Biological Activity of Fullerenols with Various Contents of Hydroxyl Groups

Polyhydroxyfullerenes, fullerenols with various contents of hydroxy groups, C60(OH) 12 –1 4 ,C 60(OH) 18 –2 4, and C60(OH) 30 –3 8, were synthesized. The first group was insoluble in water and exhibited no biological activity when introduced into cell cultures as suspensions. The other two versions of fullerenols possessed a broad spectrum of antiviral activity in vitro against actual strains of human influenza virus A(H1N1) and A(H3N2), avian influenza A(H5N1), human herpes simplex virus, adenovirus, and respiratory-syncytial virus. The water-soluble versions of fullerenol were non-toxic in vitro toward human and animal cells of various tissue origins. Besides the antiviral activity, the fullerenols demonstrated a protective effect against UVA-induced phototoxicity. The fullerenol version C60(OH) 18 –2 4had the maximum biological activity for all studied parameters. The soluble biologically active versions of fullerenol could find application in pharmacology because they could serve as a basis for new effective and non-toxic antiviral and cytoprotective drugs.