Eight sesquiterpene lactones were isolated from the roots of Inula helenium and fl owers of I. japonica. Among them, isoalantolactone (3) and santamarine (6) exhibited signifi cant growth inhibitory activities against gynecologic cancer cell lines, while others weakly inhibited the growth of the cell lines (IC 50 100 μM). In addition, 3 signifi cantly inhibited the tumour growth of S180 tumour-bearing mice. Compounds 3 and 6 were not toxic to human embryonic lung fi broblast cells in vitro. These results demonstrated that the antitumour activities are closely related to the structures of the compounds, that is, an α-exomethylene-γ-lactone ring is necessary for these activities.
Achillinin A (2β,3β-epoxy-1α,4β,10α-trihydroxyguai-11(13)-en-12,6α-olide, 1), a new guaianolide isolated from the flower of Achillea millefolium, exhibited potential antiproliferative activity to A549, RERF-LC-kj and QG-90 cells with 50% inhibitory concentration (IC(50)) values of 5.8, 10 and 0.31 µM, respectively.
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