4.5 Article

Inhibition of Lipopolysaccharide-Induced iNOS and COX-2 Expression by Indole Alkaloid, 3-(Hydroxymethyl)-6,7-Dihydroindolo[2,3-a]Quinolizin-(12H)-one, via NF-κB Inactivation in RAW 264.7 Macrophages

Journal

PLANTA MEDICA
Volume 79, Issue 9, Pages 782-787

Publisher

GEORG THIEME VERLAG KG
DOI: 10.1055/s-0032-1328550

Keywords

Nauclea officinalis; Rubiaceae; indole alkaloid; anti-inflammatory effect

Funding

  1. National Natural Science Foundation of China [81102781]
  2. Taishan Scholar Project
  3. Undergraduate Scientific and Technological Innovation Project of Yantai University [121408]

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3-(Hydroxymethyl)-6,7-dihydroindolo[2,3-a]quinolizin-(12H)-one is a bioactive indole alkaloid isolated from Nauclea officinalis, a plant species which is used as a traditional Chinese medicine. We investigated the anti-inflammatory properties of 3-(hydroxymethyl)-6,7-dihydroindolo [2,3-a] quinolizin-(12H)-one in RAW 264.7 murine macrophages. The results indicated that it inhibited the overproduction of NO and the release of TNF-alpha. Furthermore, this compound inhibited the expression of iNOS and COX-2 proteins, the enzymatic activity of iNOS, and the translocation of NF-kappa B to the nucleus induced by LPS. Therefore, we suggested that the effect of 3-(hydroxymethyl)-6,7-dihydroindolo[2,3-a] quinolizin-(12H)-one-mediated inhibition of the expression of LPS-induced iNOS and COX-2 genes is due to the suppression of NF-kappa B activation in the transcriptional level.

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