Anti-inflammatory constituents from the root of Litsea cubeba in LPS-induced RAW 264.7 macrophages

Autor: Lian-Na Sun, Hua Nian, Hai-Liang Xin, Hong-Tao Song, Zhen-Qiao Wei, Bing Lin, Ting Han, Lu-Ping Qin, Yi-Ping Jiang
Rok vydání: 2016
Předmět:
Lipopolysaccharides
Syringaresinol
Litsea
medicine.drug_class
Anti-Inflammatory Agents
Nitric Oxide Synthase Type II
Pharmaceutical Science
Context (language use)
Plant Roots
p38 Mitogen-Activated Protein Kinases
01 natural sciences
Anti-inflammatory
Mice
chemistry.chemical_compound
Drug Discovery
medicine
Animals
Phosphorylation
RAW 264.7 Cells
Inflammation
Pharmacology
Plants
Medicinal
Molecular Structure
Traditional medicine
biology
010405 organic chemistry
business.industry
Macrophages
NF-kappa B
Litsea cubeba
General Medicine
biology.organism_classification
0104 chemical sciences
010404 medicinal & biomolecular chemistry
IκBα
Complementary and alternative medicine
chemistry
Pinoresinol
Cyclooxygenase 2
Cytokines
Molecular Medicine
Inflammation Mediators
business
Proto-Oncogene Proteins c-akt
Phytotherapy
Signal Transduction
Zdroj: Pharmaceutical Biology. 54:1741-1747
ISSN: 1744-5116
1388-0209
Popis: 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 IC50 for NO inhibition on compounds 1 and 4 were 56.1 ± 1.2 and 32.8 ± 2.3 μM, respectively. The IC50 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.
Databáze: OpenAIRE
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