Two microoganisms were selected (Penicillium sp. DT-F27 and Penicillium sp. DT-F29) from 38 sediment-derived fungi from Dongtou, Zhejiang by screening antitumor activity. The fungi were cultured in PDB medium with shaking or stationary condition.26 compounds were identified from ethyl acetate extract of the broth and were subjected to a preliminary evaluation of antitumor activity.Compounds were purified through silica gel, reversed phase preparative HPLC and recrystallization etc. The structures were determined by extensive spectroscopic methods.10 compounds were separated from static fermentation broth of Penicillium sp. DT-F29, including 4 new compounds 7,7-dimethoxybrefeldin C (2), 6a-hydroxybrefeldin C (3),4-epi-15-epi-brefeldin A (4),4-eip-8a-hydroxy-15-epi-brefeldin C (5) and 6 known compounds, in which brefeldin A (6) (ICso< 0.2 μmol/L) and 7-ep/-brefeldin A (7) (IC505.2μmol/L) showed significant anti-tumor bioactivity against H1975 cell line.16 compounds were identified from the broth of Penicillium sp. DT-F27 cultured in shaker, including 14 peptide compounds, a sterol and a naphthalene derivative (trans-(3RS,4RS)-3,4-dihydro-3,4,8-trihydroxy-naphthalen-1(2H)-one), wherein ergosterol (11) and 3-0-methylviridicatin (13) exhibitted a medium antitumor activity against PC3 cell line with the value of 45.6% and 34.8% at 1μmol/L, respectively. |