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Sesquiterpene Lactones with COX‐2 Inhibition Activity from Artemisia lavandulaefolia
Authors:Jie‐Li Lü  Zhou Li  Li‐Min Guo  Lai‐Bin Zhang
Affiliation:School of Pharmacy, Xinxiang Medical University, Xinxiang, P. R. China
Abstract:Two new sesquiterpene lactones, artelavanolides A ( 1 ) and B ( 2 ), and four known sesquiterpene lactones ( 3 – 6 ) were isolated from the leaves of Artemisia lavandulaefolia. Their structures were elucidated based on the analysis of spectroscopic data (1D, 2D‐NMR and HR‐ESI‐MS). The absolute configuration of 1 was determined by the analysis of single‐crystal X‐ray diffraction data. Artelavanolide A ( 1 ) is a rare sesquiterpene lactone possessing an unusual skeleton with the linkage of Me(14)–C(1) that is probably formed through a rearrangement of the guaiane‐type sesquiterpenoids. Artelavanolide B ( 2 ) is a new highly unsaturated guaianolide. Compounds 1 – 6 were tested for activities on the inhibition of COX‐2 enzyme in vitro. All of compounds exhibited inhibitory activity against COX‐2 with IC50 values ranging from 43.29 to 287.07 μm compared with the positive control, celecoxib (IC50 = 18.10 μm ). Among them, 3 showed the best COX‐2 inhibitory activity with an IC50 value of 43.29 μm .
Keywords:   Artemisia lavandulaefolia     Compositae  sesquiterpene lactones  COX‐2 inhibitory activity  absolute configuration
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