RESUMO
Oxomollugin (2) is a degradation product of mollugin (1) and a potent inhibitor of NO-production including nuclear factor kappa B signals. In our endeavor to develop a potent anti-inflammatory compound, we synthesized several aza-derivatives of oxomollugin (2) and evaluated their NO-production inhibitory activity. Azamollugin (3) showed a potent inhibitory activity, and its activity (IC50 0.34µM) was proved to be more potent than that of oxomollugin (2, IC50 1.3µM).
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Óxido Nítrico/antagonistas & inibidores , Quinolonas/farmacologia , Animais , Anti-Inflamatórios não Esteroides/síntese química , Benzopiranos/síntese química , Benzopiranos/farmacologia , Linhagem Celular , Lipopolissacarídeos/farmacologia , Camundongos , Quinolonas/síntese químicaRESUMO
Mollugin, a naphthoquinone derivative, was reported to possess various biological activities such as anti-inflammatory and anti-tumor activity. Mollugin isolated from Rubia tinctorum roots inhibited lipopolysaccharide-induced nitric oxide (NO) production in RAW264.7 macrophages. However, mollugin synthesized for further investigation of its anti-inflammatory mechanism showed weak activity in addition to unstable assay results. From the result of analysis on a degradation product of mollugin, oxomollugin was found to be the main active substance of mollugin degradation, showing a potent inhibitory activity on NO-production including nuclear factor kappa B signals.