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-alpha production. The 10 microM 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-alpha 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.