Edible mushroom is a profilic source of bioactive metabolites for the development of drugs and nutraceuticals. In this work, four new monoterpenoids (1-4) and one new sesquiterpenoid (6) were isolated from the mycelia of edible mushroom Pleurotus cornucopiae fermented on rice. Their structures were established by nuclear magnetic resonance, mass spectrometry, and circular dichroism (CD) data analysis. Compound 1 possesses an unusual spiro[benzofuran-3,2'-oxiran] skeleton. The absolute configuration of the 6,7-diol moieties in compounds 1, 2, and 6 was assigned using the in situ dimolybdenum CD method. Compounds 1-5, 7, and 8 showed moderate inhibitory activity against nitric oxide production in lipopolysaccaride-activated macrophages, with IC50 values in the range of 60-90 μM. Compounds 6 and 7 also exhibited slight cytotoxicity against HeLa and HepG2 cells.
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