Chemical constituents from Phellinus igniarius and their anti-tumor activity in vitro

Eleven compounds were isolated and purified from Phellinus igniarius by column chromatography on silica gel, Sephedax LH-20, RP-8, MCI and preparative TLC. Their structures were identified as 3α-hydroxyfriedel-2-one (1), 3-hydroxyfriedel-3-en-2-one (2), ergosta-4, 6, 8 (14), 22-tetraen-3-one (3), ergosterol peroxide (4), uracil (5), uridine (6), 4-(3, 4-dihydroxyphenyl)-3-butene-2-one (7), protocatechualdehyde (8), inotilone (9), inoscavinA (10) and phellibaumin E (11), respectively, on the basis of NMR and MS data analysis. Among them, compounds 1, 2, 5, and 6 were firstly obtained from this genus. In vitro cytotoxic activity of compounds 1-11 was screened by Cell Titer-GLo Reagent, on 41 human tumor cell strains and 2 hamster normal cell strains via high-throughput screening. Compounds 2-4 exhibit significant cytotoxic activity against NOMO-1 and SKM-1 acute myeloid leukemia cell lines, and compounds 2 and 3 showed good selectivity to NOMO-1 with IC₅₀ values of 0.795 5, 1.828 μmol•L-1and SKM-1 with IC₅₀ values of higher than 10 μmol•L-1. Compound 7 showed remarkable antitumor activities against H526 Human lung cancer cell line, DU145 prostate cancer cell line and HEL erythroleukemia cell line with IC₅₀ values of 0.533 4, 1.885, 1.057 μmol•L⁻¹, respectively. Other compounds had no or weak antitumor effect. In addition, all compounds had no significant effect on hamster normal cell lines CHL and CHO with IC₅₀ values of higher than 10 μmol•L⁻¹, which showed that all compounds had no toxic effect on normal cells.