It is shown that fullerene C 60 /water-soluble complex with PVP molecular mass of 10,000 injected in the dorsal hippocampus completely prevents the development of amnesia caused by cycloheximide, the inhibitor of protein synthesis. With the increased PVP molecular mass up to 25,000 the complex does not produce protective effect disturbance of learning.
The present report describes development of hexamethonium complexes based on fullerene C60. Hexamethonium has a limited penetration into CNS and therefore can antagonize central effects of nicotine only when given at high doses. In the present studies conducted in laboratory rodents, intraperitoneal administration of hexamethonium-fullerene complexes blocked effects of nicotine (convulsions and locomotor stimulation). When compared to equimolar doses of hexamethonium, complexes of hexamethonium with derivatives of fullerene C60 were 40 times more potent indicating an enhanced ability to interact with central nicotine receptors. Thus, fullerene C60 derivatives should be explored further as potential carrier systems for polar drug delivery into CNS.
The mechanisms of biological action of various fullerene preparations -water-soluble C 60 /polyvinylpyrrolidone (C 60 /PVP) complex and solid-state pristine fullerene C 60 (fullerene on the surfaces [FoS]), in cell-free system and in different cell cultures were studied. In the cell-free system the C 60 /PVP complex showed the pro-oxidant activity. On the other hand, FoS in the darkness proved to be antioxidant (AO) and was nontoxic for different cell lines. But under visiblelight illumination cell viability dropped in time-and light-dose-dependent way. Moreover, photodynamic damage of cells of tumor origin was greater than normal. The effect of illumination was reversed by some antioxidants. Therefore, redox properties in cell-free system and biological activity of pristine fullerene in vitro, in particular, photoxicity, depend on its aggregation state.
It is shown for the first time that the mammalian enzymes can cause the degradation of the C60 fullerene molecules. This biodegradation is caused by the action of а hypochlorite generated neutrophil enzyme myeloperoxidase of fullerene molecule and leads to the loss of the topology of the fullerene core.
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