Abstract
N,N-Didesmethylgrossularine-1 (DDMG-1), a compound with a rare α-carboline structure, was isolated from an Indonesian ascidian Polycarpa aurata as responsible for the observed inhibitory activity against TNF-α production in lipopolysaccharide-stimulated murine macrophage-like RAW264.7 cells. DDMG-1 inhibited the mRNA level of mTNF-α, IκB-α degradation, and binding of NF-κB to the target DNA site in LPS-stimulated RAW 264.7 cells. Moreover, DDMG-1 had an inhibitory effect on the production of IL-8, which is produced in CD14+-THP-1 cells stimulated by LPS. DDMG-1 is thus a promising drug candidate lead compound for the treatment of chronic inflammatory diseases, such as rheumatoid arthritis.
Original language | English |
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Pages (from-to) | 589-599 |
Number of pages | 11 |
Journal | Marine Drugs |
Volume | 7 |
Issue number | 4 |
DOIs | |
Publication status | Published - 2009 Dec |
Externally published | Yes |
Keywords
- LPS
- N,N-didesmethylgrossularine-1
- NF-κB
- Natural product
- Raw 264.7 cells
- TNF-α
ASJC Scopus subject areas
- Drug Discovery