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Artemisolide fromArtemisia asiatica: Nuclear Factor-κB (NF-κB) inhibitor suppressing prostaglandin E2 and nitric oxide production in macrophages

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Aerial parts ofArtemisia asiatica (Compositae) have been traditionally used as an oriental medicine for the treatment of inflammatory and ulcerogenic diseases. In the present study, artemisolide was isolated as a nuclear factor (NF)-κB inhibitor fromA. asiatica by activity-guided fractionation. Artemisolide inhibited NF-κB transcriptional activity in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 with an IC50 value of 5.8 μM. The compound was also effective in blocking NF-κB transcriptional activities elicited by the expression vector encoding the NF-κB p65 or p50 subunits bypassing the inhibitory kB degradation signaling NF-κB activation. The macrophages markedly increased their PGE2 and NO production upon exposure to LPS alone. Artemisolide inhibited LPS-induced PGE2 and NO production with IC50 values of 8.7 μM and 6.4 μM, respectively, but also suppressed LPS-induced synthesis of cyclooxygenase (COX)-2 or inducible NO synthase (iNOS). Taken together, artemisolide is a NF-κB inhibitor that attenuates LPS-induced production of PGE2 or NOvia down-regulation of COX-2 or iNOS expression in macrophages RAW 264.7. Therefore, artemisolide could represent and provide the anti-inflammatory principle associated with the traditional medicine,A. asiatica.

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Correspondence to Youngsoo Kim.

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Reddy, A.M., Lee, J., Seo, J.H. et al. Artemisolide fromArtemisia asiatica: Nuclear Factor-κB (NF-κB) inhibitor suppressing prostaglandin E2 and nitric oxide production in macrophages. Arch Pharm Res 29, 591–597 (2006). https://doi.org/10.1007/BF02969271

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Key words

  • Artemisolide
  • Artemisia asiatica
  • Nuclear factor-κB
  • Prostaglandin E2
  • Nitric oxide
  • Macrophages