Inhibitory Effects of Fullerene C₆₀derivatives on Endothelium-Derived Relaxation in Rabbit Thoracic Aorta

Inhibitory effects of newly synthesized fullerene C60 derivatives 1 (C60-bis(N,N-dimethylpyrrolidinium iodide)), 2 (C60-proline-N-acetic acid) and 3 (C60-ethylenediamine-N, N′-diacetic acid) on acetylcholine-induced relaxation in endothelium-intact rabbit thoracic aorta precontracted by phenylephrine (10−6 M) were studied. Fullerene C60 derivative 1 (3 × 10−6 M), 2 (10−5 M) and 3 (10−5 M) reduced the maximum amplitude of the acetylcholine-induced relaxation without significantly changing the pD2 values obtained from the concentration - response curves. In the presence of fullerene C60 derivative 1 (10−5 M) the acetylcholine-induced relaxation was eliminated and an acetylcholine-induced contraction was observed. These results suggest that fullerene C60 derivative 1 strongly inhibits endothelium (nitric oxide)-dependent acetylcholine-induced relaxation in thoracic aorta of rabbit.