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KMID : 0620720040100060315
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Natural Product Sciences
2004 Volume.10 No. 6 p.315 ~ p.320
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Inhibitory Effect of Benzofuran Compound on Cyclooxygenase
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Min Kyung-Rak
Ahn Ki-Young
Chung Eun-Yong
Lee Yong-Rok
Kim Yeong-Shik
Kim Young-Soo
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Abstract
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Alpha-viniferin was previously isolated as a cyclooxygenase (COX)-2 inhibitor from Carex humilis (Cyperaceae) and is an oligomeric stilbene compound with benzofuran (BF) moieties in its chemical structure. In the present study, a chemically synthetic BF compound, named as 3,3-dimethyl-2,3,4,6,7,8,9,10,11,12,13,14,15,16,17,18-hexadecahydro-1H-benzo[b] cyclopentadeca[d]furan-1-one, was discovered to inhibit bacterial lipo polysaccharide (LPS)-induced prostaglandin E2(PGE2) production in macrophages RAW 264.7. The BF compound exhibited a selectively preferred inhibitory effect on COX-2 activity over COX-1 activity. Furthermore, BF compound inhibited LPS-induced COX-2 expression at transcription level. As a down-regulatory mechanism of COX-2 expression shown by BF compound, suppression of nuclear factor (NF)-κB activation has been demonstrated. BF compound inhibited LPS-induced NF-κB transcriptional activity and nuclear translocation of NF-κB p65, in parallel, but did not affect LPS-induced degradation of inhibitory κBα protein(IκBα). Taken together, anti-inflammatory effect of BF compound on PGE2 production was ascribed by its down-regulatory action on LPS-induced COX-2 synthesis in addition to inhibitory action on enzyme activity of COX-2.
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KEYWORD
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Benzofuran compound, Cyclooxygenase, Nuclear factor-κB, Macrophages
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