Fullerenols are nanosized water-soluble polyhydroxylated derivatives of fullerenes, specific allotropic form of carbon, bioactive compounds and perspective pharmaceutical agents. We studied biological effects of a series of fullerenols. Antioxidant activity and toxicity of the fullerenols were compared using bioluminescence assays (cellular and enzymatic); a content of Reactive Oxygen Species in fullerenol solutions was determined using chemiluminescence luminol method. Two groups of fullerenols with different number of hydroxyl substituents were under investigation: (I) С60Оy(OH)x, С60,70Оy(OH)x, where х+у=24–28 and (II) С60,70Оy(OH)x, Fe0,5С60Оy(OH)x, where х+у=40–42. Toxicity of the fullerenols was evaluated using effective concentrations ЕС50. Fullerenol’ antioxidant activity was investigated in model solutions of organic toxicant of oxidative type, 1,4-benzoquinone. Detoxification coefficients were calculated to analyze and compare the antioxidant activity. Higher toxicity and lower antioxidant activity were demonstrated in the solutions of fullerenols with higher number of the oxygen substituents (х+у=40–42). The differences were concerned with fullerenol’ ability to disturb Reactive Oxygen Species balance in aqueous solutions. Toxic effect of the prospective endohedral metal-fullerenol with gadolinium atom involved, Gd@C82Oy(OH)x, where х+у=40–42, was evaluated and explained by a high number of oxygen groups