α-Cyperone, isolated from the rhizomes of Cyperus rotundus, inhibits LPS-induced COX-2 expression and PGE2 production through the negative regulation of NFκB signalling in RAW 264.7 cells.

ETHNOPHARMACOLOGICAL RELEVANCE

The rhizomes of Cyperus rotundus (Cyperaceae) have been used in Asian traditional medicine for the treatment of several inflammatory diseases. However, the anti-inflammatory effects of α-cyperone, a major active compound of Cyperus rotundus, are poorly understood.

MATERIALS AND METHODS

PGE2 and cytokines released from cells were measured using an EIA assay kit. The expression of iNOS, COX-2, TNF-α, and IL-6 was measured by real-time RT-PCR and/or Western blot analysis. A luciferase assay was performed to measure the effect of α-cyperone on NFκB activity.

RESULTS

The n-hexane fraction of the 80% EtOH extract from the rhizomes of Cyperus rotundus was found to inhibit both NO and PGE2 production in RAW 264.7 cells. α-Cyperone isolated from the n-hexane fraction significantly inhibited PGE2 production by suppressing the LPS-induced expression of inducible COX-2 at both the mRNA and the protein levels. In contrast, α-cyperone had little effect on NO production and iNOS expression. Additionally, α-cyperone downregulated the production and mRNA expression of the inflammatory cytokine IL-6. Moreover, treatment with α-cyperone suppressed the transcriptional activity of NFκB and the nuclear translocation of the p65 NFκB subunit in LPS-induced RAW 264.7 cells.

CONCLUSION

The anti-inflammatory activity of α-cyperone is associated with the down-regulation of COX-2 and IL-6 via the negative regulation of the NFκB pathway in LPS-stimulated RAW 264.7 cells.