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Anti-inflammatory Effects of Canthin-6-one Alkaloids from Ailanthus altissima
- Source :
- Planta Medica. 84:527-535
- Publication Year :
- 2017
- Publisher :
- Georg Thieme Verlag KG, 2017.
-
Abstract
- Canthin-6-one (CO) alkaloids possess various biological activities, including antibacterial, antitumor, antifungal, and antiviral activities. However, their anti-inflammatory effects and underlying molecular mechanisms are poorly characterized. This study aimed to investigate the anti-inflammatory effects of CO and its derivative 5-(1-hydroxyethyl)-canthin-6-one (5-HCO), isolated from the stem barks of Ailanthus altissima in lipopolysaccharide (LPS)-stimulated macrophages. CO (1 and 5 µM) and 5-HCO (7.5 and 15 µM) significantly inhibited the LPS-induced expression of inducible nitric oxide synthase. In addition, CO (1 and 5 µM) and 5-HCO (15 µM) markedly suppressed the production of prostaglandin E2 (PGE2) and expression of cyclooxygenase-2, a key enzyme in PGE2 synthesis, in LPS-stimulated macrophages. Moreover, CO treatment significantly reduced monocyte chemotactic protein-1 (MCP-1) and tumor necrosis factor-α (TNF-α) expression, whereas 5-HCO inhibited MCP-1, but not TNF-α expression. Both CO and 5-HCO inhibited the phosphorylation of inhibitor kappa B and transcriptional activation of nuclear factor kappa B (NF-κB) in LPS-stimulated macrophages. In addition, CO, but not 5-HCO, markedly reduced Akt phosphorylation. Taken together, these data suggest that CO, but not 5-HCO with a hydroxyethyl moiety on the D ring, has potent anti-inflammatory activity in LPS-stimulated macrophages through the downregulation of both the NF-κB and the Akt pathway.
- Subjects :
- 0301 basic medicine
Lipopolysaccharide
Anti-Inflammatory Agents
Pharmaceutical Science
Inflammation
Indole Alkaloids
Analytical Chemistry
03 medical and health sciences
chemistry.chemical_compound
Alkaloids
Drug Discovery
medicine
Prostaglandin E2
PI3K/AKT/mTOR pathway
Ailanthus
Pharmacology
biology
Macrophages
Monocyte
Organic Chemistry
NF-kappa B
Molecular biology
Nitric oxide synthase
030104 developmental biology
medicine.anatomical_structure
Complementary and alternative medicine
chemistry
Biochemistry
biology.protein
Molecular Medicine
Phosphorylation
Tumor necrosis factor alpha
medicine.symptom
Carbolines
medicine.drug
Subjects
Details
- ISSN :
- 14390221 and 00320943
- Volume :
- 84
- Database :
- OpenAIRE
- Journal :
- Planta Medica
- Accession number :
- edsair.doi.dedup.....7121cc0ad9e494b170d410c672974cf2