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KMID : 0617320020110010209
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Journal of Pharmacetical Sceiences Ewha Womans University
2002 Volume.11 No. 1 p.209 ~ p.216
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Suppressive Effect of Natural Sesquiterpenoids on Inducible Cyclooxygenase (COX-2) and Nitric Oxide Synthase (iNOS)Activity in Mouse Macrophage Cells
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Lee, Sang Kook
Hong, Chai-Hee/Huh, Sun-Kyung/Kim, Sun-Sook/Oh, O-Jin/Min, Hye-Young/Park, Kwang-Kyun
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Abstract
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Prostaglandins and nitric oxide produced by inducible cyclooygenase (COX-2)and nitric oxide synthase (iNOS), respectively, have been implicated asimportant mediators in the processes of inflammation and carcinogenesis.These potential COX-2 and iNOS inhibitors have been considered asantiinflammatory and cancer chemopreventive agents. In this study, weinvestigated the efect of natural sesquiterpenoids isolated from plants of theZingiberaceae family on the activities of COX-2 and iNOS in culturedlipopolysaccharide (LPS)-activated mouse. macrophage ce11 RAW 264.7 todiscover new lead compounds as COX-2 or iNOS inhibitors.Xanthorrhizol,a sesquiterpenoid, isolated from the rhizome of Curruma xanthrrbiza Roxb.(Zingiberaceae), exhibited a potent inhibition of COX-2 (IC_50= 0.2 μg/mL)and iNOS activity (IC_50 = 1.0 μg/mL) in the assay system of prostaglandin E2(PGE_2) accumulation and nitric oxide production, respectively. Western blotanalyses revealed that the inhibitory potential of xanthorrhizol on the COX-2activity coincided well with the suppression of COX-2 protein expression inLPS-induced macrophages. In addition, sesquiterpenoids β-turmerone andar-turmerone isolated from the rhisome of Curruma zedoaria Roscoe(Zingiberaceae) also showed a potent inhibitory activity of COX-2(β-turmerone, IC_50 = 1.6 μg/mL; ar-turmerone, IC_50 = 5.2 μg/mL) and iNOS(β-turmerone, IC_50 = 4.6 μg/mL; ar-turmerone, IC_50 = 3.2 μg/mL). Theseresults suggest that natural sesquiterpenoids from C. xanthorrbiza and C.zedoariamight be lead candidares for further developing COX-2 or iNOS inhibitorspossessing cancer chemopreventive or anti-inflammatory properties.
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