Bioactivity-guided isolation of cytotoxic sesquiterpenes of Rolandra fruticosa

Bioassay-guided fractionation of a methanol extract of Rolandra fruticosa led to the isolation of seven germacrane-type derived sesquiterpenes, including two previously unknown compounds, 13-methoxyisorolandrolide (1), and 2α,13-diacetoxy-4α-hydroxy-8α-isobutyloyloxybourbonen-12,6α-olide (2). All isolates were evaluated for their cytotoxicity using the HT-29 cell line. Compounds 3, 5, 6 were also tested in an enzyme-based ELISA NF-κB (p65) inhibition assay. 13-Acetoxyrolandrolide (3) was investigated in an in vivo hollow fiber assay.