title: Inhibitors of the LPS-induced NF-kappaB activation from Artemisia sylvatica.
abstract: Three guaianolide sesquiterpene lactones, 3alpha,4alpha-epoxyrupicolins C-E, together with six known sesquiterpenes, artemisolide, 3-methoxytanapartholide, deacetyllaurenobiolide, moxartenolide as well as arteminolides B and D were isolated by bioassay-guided fractionation from the methanol extract of the aerial parts of Artemisia sylvatica using the NF-kappaB mediated reporter gene assay. All isolated compounds displayed inhibitory activity on the LPS-induced NF-kappaB activation, NO production, and TNF-alpha production with IC50 values of 0.49-7.17, 1.46-6.16, and 3.19-27.76 microM, respectively, in RAW264.7 cells. It was also established that arteminolide B suppressed the expression of NF-kappaB target genes such as iNOS and COX-2. This is the first report of NF-kappaB inhibitory activities of these compounds and supports the pharmacological use of Artemisia sylvatica, which has been employed as an herbal medicine for the treatment of inflammation.
authors.affiliation: Anticancer Research Laboratory, Korea Research Institute of Bioscience and Biotechnology, Yuseong, Daejeon 305-600, Korea.
authors.forename: Hui Zi
authors.initials: HZ
authors.lastname: Jin
authors.forename: Jeong Hyung
authors.initials: JH
authors.lastname: Lee
authors.forename: Dongho
authors.initials: D
authors.lastname: Lee
authors.forename: Young Soo
authors.initials: YS
authors.lastname: Hong
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Kim
authors.forename: Jung Joon
authors.initials: JJ
authors.lastname: Lee
mesh_terms: D000818:Animals; D019306:Artemisia / Q000737:chemistry*; D015153:Blotting, Western; D002460:Cell Line; D051546:Cyclooxygenase 2; D007527:Isoenzymes / Q000096:biosynthesis; D007783:Lactones / Q000302:isolation & purification / Q000494:pharmacology*; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009569:Nitric Oxide / Q000096:biosynthesis; D019001:Nitric Oxide Synthase / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II; D035261:Plant Components, Aerial / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry; D011451:Prostaglandin-Endoperoxide Synthases / Q000096:biosynthesis; D012717:Sesquiterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D014409:Tumor Necrosis Factor-alpha / Q000096:biosynthesis
chemical_list: D007527:Isoenzymes; D007783:Lactones; D008070:Lipopolysaccharides; D016328:NF-kappa B; D010936:Plant Extracts; D012717:Sesquiterpenes; D014409:Tumor Necrosis Factor-alpha; D009569:Nitric Oxide; D019001:Nitric Oxide Synthase; D052247:Nitric Oxide Synthase Type II; C496317:Nos2 protein, mouse; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases