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.
Huang
Sheng-Tung
ST
Graduate Institute of Biotechnology, National Taipei University of Technology, Taipei, Taiwan. ws75624@ntut.edu.tw
Liao
Jian-Sheng
JS
Fang
Hsu-Wei
HW
Lin
Chun-Mao
CM
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D037741:Fullerenes / Q000737:chemistry / Q000494:pharmacology*; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects / Q000276:immunology; D051379:Mice; D009569:Nitric Oxide / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D014970:Xanthines / Q000138:chemical synthesis* / Q000494:pharmacology*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D037741:Fullerenes; D008070:Lipopolysaccharides; D011759:Pyrrolidines; D014409:Tumor Necrosis Factor-alpha; D014970:Xanthines; D009569:Nitric Oxide; C069837:fullerene C60