Anti-inflammatory constituents from the root of Litsea cubeba in LPS-induced RAW 264.7 macrophages
Context Litsea cubeba (Lour.) Pers. (Lauraceae) has long been used as a folk remedy in Traditional Chinese Medicine (TCM) for the treatment of rheumatic diseases. Previous studies from our laboratory indicated that L. cubeba extract showed anti-arthritic activity in rats. Objective To study L. cubeb...
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Published in | Pharmaceutical biology Vol. 54; no. 9; pp. 1741 - 1747 |
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Main Authors | , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
England
Taylor & Francis
01.09.2016
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Subjects | |
Online Access | Get full text |
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Summary: | Context Litsea cubeba (Lour.) Pers. (Lauraceae) has long been used as a folk remedy in Traditional Chinese Medicine (TCM) for the treatment of rheumatic diseases. Previous studies from our laboratory indicated that L. cubeba extract showed anti-arthritic activity in rats.
Objective To study L. cubeba chemically and biologically and to find the potential constituents responsible for its anti-arthritic effect.
Materials and methods The compounds were isolated from the root of L. cubeba by column chromatography which eluted with PE:EtOAc gradient system, and the structures were elucidated by detailed spectroscopic data analysis; the anti-inflammatory activity of the isolated compounds was evaluated by lipopolysaccharide (LPS)-induced RAW 264.7 cells and the TNF-α and NO level were measured by ELISA (commercial kit); The iNOS and COX-2 mRNA expression were measured by RT-PCR and the phosphorylation of IκBα, IKKβ, P38 and Akt were determined by western blots.
Results A novel 9-fluorenone, 1-ethoxy-3,7-dihydroxy-4,6-dimethoxy-9-fluorenone (1), together with 4 known compounds, namely pinoresinol (2), syringaresinol (3), 9,9′-O-di-(E)-feruloyl-meso-5,5′-dimethoxysecoisolariciresinol (4) and lyoniresinol (5) were isolated from the root of L. cubeba for the first time. The IC
50
for NO inhibition on compounds 1 and 4 were 56.1 ± 1.2 and 32.8 ± 2.3 μM, respectively. The IC
50
for TNF-α inhibition were 28.2 ± 0.9 and 15.0 ± 1.0 μM, respectively. Both 1 and 4 suppress mRNA expression of iNOS, COX-2 and protein phosphorylation of IκBα, IKKβ in LPS-induced RAW 264.7 cells.
Discussion and conclusion Compounds 1 and 4 isolated from L. cubeba exhibited potent anti-inflammatory activity through the NF-κB signal pathway. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 1388-0209 1744-5116 |
DOI: | 10.3109/13880209.2015.1126619 |