Suppression of cyclooxygenase-2 gene transcription by humulon of beer hop extract studied with reference to glucocorticoid.

Abstract	In murine osteoblastic MC3T3-E1 cells which produced prostaglandin E2 as a bone resorption factor, the cyclooxygenase-2 induction by tumor necrosis factor alpha (TNFalpha) was suppressed by dexamethasone with an IC(50) of 1 nM. Humulon isolated from hop extract for beer brewing was reported previously as an inhibitor of bone resorption [Tobe, H. et al. (1997) Biosci. Biotech. Biochem. 61, 158-159]. We showed that the compound suppressed the TNFalpha-dependent cyclooxygenase-2 induction with an IC(50) of as low as about 30 nM as demonstrated experimentally by catalytic activity assay, Northern blot analysis and promoter analysis. Reporter gene experiments suggested that humulon blocked the cyclooxygenase-2 expression mediated by NFkappaB and NF-IL6, but the intracellular glucocorticoid receptor was not involved. The catalytic activity of cyclooxygenase-2 was inhibited by humulon with an IC(50) of as high as 1.6 microM. These results showed that humulon suppressed cyclooxygenase-2 induction at the step of transcription.
Authors	K Yamamoto, J Wang, S Yamamoto, H Tobe
Journal	FEBS letters (FEBS Lett) Vol. 465 Issue 2-3 Pg. 103-6 (Jan 14 2000) ISSN: 0014-5793 [Print] England
PMID	10631313 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	CCAAT-Enhancer-Binding Proteins Cyclohexenes DNA Primers DNA-Binding Proteins Isoenzymes NF-kappa B Nuclear Proteins RNA, Messenger Terpenes Dexamethasone Cyclooxygenase 2 Prostaglandin-Endoperoxide Synthases Thymidine Kinase Dinoprostone humulon
Topics	3T3 Cells Animals Base Sequence Beer (analysis) Bone Resorption CCAAT-Enhancer-Binding Proteins Catalysis Cyclohexenes Cyclooxygenase 2 DNA Primers DNA-Binding Proteins (genetics) Dexamethasone (pharmacology) Dinoprostone (biosynthesis) Isoenzymes (genetics, metabolism) Mice NF-kappa B (genetics) Nuclear Proteins (genetics) Prostaglandin-Endoperoxide Synthases (genetics, metabolism) RNA, Messenger (genetics, metabolism) Terpenes (isolation & purification, pharmacology) Thymidine Kinase (genetics) Transcription, Genetic (drug effects)

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