Inhibitors of the LPS-induced NF-κB activation from Artemisia sylvatica

Three guaianolide type sesquiterpene lactones, 3α,4α- epoxyrupicolins C-E (1-3), together with six known sesquiterpenes (4-9) were isolated and identified from the methanol extract of the aerial parts of Artemisia sylvatica, and their biological activities were reported. Three guaianolide sesquiterpene lactones, 3α,4α-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-κB mediated reporter gene assay. All isolated compounds displayed inhibitory activity on the LPS-induced NF-κB activation, NO production, and TNF-α production with IC ₅₀ values of 0.49-7.17, 1.46-6.16, and 3.19-27.76 μM, respectively, in RAW264.7 cells. It was also established that arteminolide B suppressed the expression of NF-κB target genes such as iNOS and COX-2. This is the first report of NF-κB 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.