Synthesis and anti-inflammation evaluation of new C₆₀ fulleropyrrolidines bearing biologically active xanthine

We designed and prepared the new C₆₀ fullerene hybrids bearing a xanthine moiety as potential double-action anti-inflammatory agents, capable of simultaneous inhibition of LPS-induced NO and TNF-α production. The 10 μM of fulleropyrrolidine-xanthine dyad 2a and b were effective in suppressing LPS-induced NO production by 55.1 ± 2.1% and 58.6 ± 2.6%, respectively, but only 2b was also effectively in suppressing LPS-induced TNF-α production by 34.0 ± 2.7%. We believed that the agents synthesized herein would hold promise for future development of a new generation of potent anti-inflammatory agents.