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- Title
Inhibitory Activity of Natural cis -Khellactone on Soluble Epoxide Hydrolase and Proinflammatory Cytokine Production in Lipopolysaccharides-Stimulated RAW264.7 Cells.
- Authors
Kim, Jang Hoon; Park, Ji Hyeon; Koo, Sung Cheol; Huh, Yun-Chan; Hur, Mok; Park, Woo Tae; Moon, Youn-Ho; Kim, Tae Il; Cho, Byoung Ok
- Abstract
The pursuit of anti-inflammatory agents has led to intensive research on the inhibition of soluble epoxide hydrolase (sEH) and cytokine production using medicinal plants. In this study, we evaluated the efficacy of cis-khellactone, a compound isolated for the first time from the roots of Peucedanum japonicum. The compound was found to be a competitive inhibitor of sEH, exhibiting an IC50 value of 3.1 ± 2.5 µM and ki value of 3.5 µM. Molecular docking and dynamics simulations illustrated the binding pose of (−)cis-khellactone within the active site of sEH. The results suggest that binding of the inhibitor to the enzyme is largely dependent on the Trp336–Gln384 loop within the active site. Further, cis-khellactone was found to inhibit pro-inflammatory cytokines, including NO, iNOS, IL-1β, and IL-4. These findings affirm that cis-khellactone could serve as a natural therapeutic candidate for the treatment of inflammation.
- Subjects
EPOXIDE hydrolase; MOLECULAR dynamics; CYTOKINES; ANTI-inflammatory agents; ENZYME inhibitors
- Publication
Plants (2223-7747), 2023, Vol 12, Issue 20, p3656
- ISSN
2223-7747
- Publication type
Article
- DOI
10.3390/plants12203656