Abstract

A phytochemical investigation of the ethanol extracts of Taiwanese Vernonia cinerea L. resulted in the isolation of ten hirsutinolide-type sesquiterpenoids, including seven new ones, named vercinolides A˜G (1˜7). All structures were elucidated by a combination of detailed spectroscopic analyses (NMR and MS) and comparison with reported data. Furthermore, in in vitro anti-inflammatory assays, compounds 4, 5, and 8˜10 exhibited strong inhibitory activities of NO production by LPS-induced RAW264.7 macrophages, IC50 values of 1.16, 0.91, 0.75, 0.55, and 0.28 µM, without affecting cellular viability at 40 µM. Structure-activity relationship studies implied that the functional groups at C-1, C-8, and C-13 may enhance inhibition of NO production, especially the ether group at C-8.

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