title: Sesquiterpene lactones from Inula falconeri, a plant endemic to the Himalayas, as potential anti-inflammatory agents.
abstract: A phytochemical investigation of Inula falconeri, a plant endemic to the Himalayas, afforded 10 new sesquiterpenoids and 26 known sesquiterpene lactones, including those bearing guaiane, pseudoguaiane, xanthane, eudesmane, germacrane, rare secocaryophyllane, chromolaevane, and carabrane frameworks. The structures were elucidated via spectroscopic analysis and compared with data from literature. All the isolates were assessed for their inhibitory effects against LPS-induced nitric oxide production in RAW264.7 macrophages. Compounds 4, 11, 24, and 31 showed stronger inhibitory activities than the positive control with IC(50) values of 0.13, 0.07, 0.11, and 0.11 μM, respectively. These studies also led to a better understanding of the structure-activity relationships for the sesquiterpene lactone family of compounds.
authors.affiliation: School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China.
authors.forename: Xiangrong
authors.initials: X
authors.lastname: Cheng
authors.forename: Qi
authors.initials: Q
authors.lastname: Zeng
authors.forename: Jie
authors.initials: J
authors.lastname: Ren
authors.forename: Jiangjiang
authors.initials: J
authors.lastname: Qin
authors.forename: Shoude
authors.initials: S
authors.lastname: Zhang
authors.forename: Yunheng
authors.initials: Y
authors.lastname: Shen
authors.forename: Jiaxian
authors.initials: J
authors.lastname: Zhu
authors.forename: Fei
authors.initials: F
authors.lastname: Zhang
authors.forename: Ruijie
authors.initials: R
authors.lastname: Chang
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhu
authors.forename: Weidong
authors.initials: W
authors.lastname: Zhang
authors.forename: Huizi
authors.initials: H
authors.lastname: Jin
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D002460:Cell Line; D038143:Inula / Q000737:chemistry* / Q000254:growth & development; D007783:Lactones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D009569:Nitric Oxide / Q000096:biosynthesis; D012717:Sesquiterpenes / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000893:Anti-Inflammatory Agents; D007783:Lactones; D012717:Sesquiterpenes; D009569:Nitric Oxide