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Eugenol suppresses cyclooxygenase-2 expression in lipopolysaccharide-stimulated mouse macrophage RAW264.7 cells
Sun Suk Kim1, O-Jin Oh, Hye-Young Min
1College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-ku, Seoul 120-750, South Korea.
Abstract:
Inducible cyclooxygenase (COX-2) has been implicated in the processes of inflammation and carcinogenesis. Thus, the potential COX-2 inhibitors have been considered as anti-inflammatory or cancer chemopreventive agents. In this study, the methanolic extract of the cortex of Eugenia caryophyllata Thunberg (Myrtaceae) was found to potently inhibit the prostaglandin E(2) production in lipopolysaccharide (LPS)-activated mouse macrophage RAW264.7 cells (98.3% inhibition at the test concentration of 10 microg/ml). Further, hexane-soluble layer was the most active partition compared to ethyl acetate, n-butanol, and water-soluble parts. By bioassay-guided fractionation of hexane-soluble partition, eugenol was isolated and exhibited a significant inhibition of PGE(2) production (IC(50) = 0.37 microM). In addition, eugenol suppressed the cyclooxygenase-2 (COX-2) gene expression in LPS-stimulated mouse macrophage cells. On the line of COX-2 playing an important role in colon carcinogenesis further study was designed to investigate the effect of eugenol on the growth and COX-2 expression in HT-29 human colon cancer cells. Eugenol inhibited the proliferation of HT-29 cells and the mRNA expression of COX-2, but not COX-1. This result suggests that eugenol might be a plausible lead candidate for further developing the COX-2 inhibitor as an anti-inflammatory or cancer chemopreventive agent.
Insights
Eugenol from Eugenia caryophyllata potently inhibits prostaglandin E(2) production and cyclooxygenase-2 (COX-2) gene expression. This natural compound shows promise as an anti-inflammatory and cancer chemopreventive agent.
Area of Science:
- Pharmacology
- Natural Products Chemistry
- Cancer Biology
Background:
- Inducible cyclooxygenase-2 (COX-2) is linked to inflammation and cancer development.
- COX-2 inhibitors are explored as potential anti-inflammatory and cancer chemopreventive agents.
Purpose of the Study:
- To investigate the anti-inflammatory and anti-cancer properties of Eugenia caryophyllata extract and its active compound, eugenol.
- To evaluate the effect of eugenol on prostaglandin E(2) production, COX-2 gene expression, and colon cancer cell proliferation.
Main Methods:
- Methanolic extract of Eugenia caryophyllata cortex was tested for inhibition of prostaglandin E(2) (PGE(2)) in LPS-activated mouse macrophage RAW264.7 cells.
- Bioassay-guided fractionation of the active hexane-soluble partition led to the isolation of eugenol.
- Eugenol's effects on PGE(2) production, COX-2 gene expression in macrophages, and proliferation and COX-2 mRNA expression in HT-29 human colon cancer cells were assessed.
Main Results:
- The Eugenia caryophyllata extract strongly inhibited PGE(2) production (98.3% at 10 microg/ml).
- Eugenol significantly inhibited PGE(2) production (IC(50) = 0.37 microM) and suppressed COX-2 gene expression in LPS-stimulated macrophages.
- Eugenol inhibited HT-29 colon cancer cell proliferation and reduced COX-2 mRNA expression without affecting COX-1.
Conclusions:
- Eugenol, isolated from Eugenia caryophyllata, exhibits potent inhibition of PGE(2) production and COX-2 expression.
- Eugenol demonstrates anti-proliferative effects on human colon cancer cells, suggesting a role in cancer chemoprevention.
- Eugenol is a promising candidate for developing novel COX-2 inhibitors for anti-inflammatory and anti-cancer applications.