title: 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.
abstract: 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-α. Furthermore, this compound inhibited the expression of iNOS and COX-2 proteins, the enzymatic activity of iNOS, and the translocation of NF-κB 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-κB activation in the transcriptional level.
authors.affiliation: School of Pharmacy, Yantai University, Yantai, PR China. zhaofeng74@yahoo.com.cn
authors.forename: Feng
authors.initials: F
authors.lastname: Zhao
authors.forename: Lei
authors.initials: L
authors.lastname: Chen
authors.forename: Menglin
authors.initials: M
authors.lastname: Zhang
authors.forename: Chenchen
authors.initials: C
authors.lastname: Bi
authors.forename: Lichun
authors.initials: L
authors.lastname: Li
authors.forename: Qingzhen
authors.initials: Q
authors.lastname: Zhang
authors.forename: Cuicui
authors.initials: C
authors.lastname: Shi
authors.forename: Miao
authors.initials: M
authors.lastname: Li
authors.forename: Songsong
authors.initials: S
authors.lastname: Zhou
authors.forename: Linghua
authors.initials: L
authors.lastname: Kong
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D002467:Cell Nucleus / Q000187:drug effects / Q000378:metabolism; D002478:Cells, Cultured; D051546:Cyclooxygenase 2 / Q000378:metabolism; D052246:Cyclooxygenase 2 Inhibitors / Q000494:pharmacology*; D026121:Indole Alkaloids / Q000737:chemistry* / Q000494:pharmacology; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D008070:Lipopolysaccharides / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects* / Q000378:metabolism; D051379:Mice; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009569:Nitric Oxide / Q000378:metabolism; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D021381:Protein Transport / Q000187:drug effects; D011807:Quinolizines / Q000737:chemistry / Q000494:pharmacology*; D019666:Rubiaceae / Q000737:chemistry; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: C585783:3-(hydroxymethyl)-6,7-dihydroindolo(2,3-a)quinolizin-(12H)-one; D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D026121:Indole Alkaloids; D007211:Indoles; D008070:Lipopolysaccharides; D016328:NF-kappa B; D011807:Quinolizines; D014409:Tumor Necrosis Factor-alpha; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II; C496317:Nos2 protein, mouse; C077623:Ptgs2 protein, mouse; D051546:Cyclooxygenase 2