BACKGROUND: Antrodia cinnamomea is known for its antihepatoma activity, yet the identity of its active compound was unclear. In this study, a 5-ton fermenter was used to prepare sufficient mycelium of A. cinnamomea for active compound isolation and identification. RESULTS: Using antiproliferative activity toward HepG2 cells as guidance in the isolation process, 4-acetylantroquinonol B was purified and identified to be the major bioactive compound of A. cinnamomea cultivated by submerged fermentation. The median effective doses (EC(50)) of 4-acetylantroquinonol B for HepG2 cells were 0.10 +/- 0.00 and 0.08 +/- 0.00 microg mL(-1) for 72 and 96 h treatments, respectively. The selective indices of 4-acetylantroquinonol B were 100 and 125 for 72 and 96 h treatments, respectively, indicating that this compound had high selective activity for hepatoma cells. CONCLUSION: 4-Acetylantroquinonol B is the major antihepatoma constituent of Antrodia cinnamomea mycelium produced by submerged fermentation. Copyright (c) 2010 Society of Chemical Industry.
BACKGROUND:Antrodia cinnamomea is known for its antihepatoma activity, yet the identity of its active compound was unclear. In this study, a 5-ton fermenter was used to prepare sufficient mycelium of A. cinnamomea for active compound isolation and identification. RESULTS: Using antiproliferative activity toward HepG2 cells as guidance in the isolation process, 4-acetylantroquinonol B was purified and identified to be the major bioactive compound of A. cinnamomea cultivated by submerged fermentation. The median effective doses (EC(50)) of 4-acetylantroquinonol B for HepG2 cells were 0.10 +/- 0.00 and 0.08 +/- 0.00 microg mL(-1) for 72 and 96 h treatments, respectively. The selective indices of 4-acetylantroquinonol B were 100 and 125 for 72 and 96 h treatments, respectively, indicating that this compound had high selective activity for hepatoma cells. CONCLUSION:4-Acetylantroquinonol B is the major antihepatoma constituent of Antrodia cinnamomea mycelium produced by submerged fermentation. Copyright (c) 2010 Society of Chemical Industry.