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Oxygenated lanosterol derivatives, which were isolated from Ganoderma lucidum (Polyporaceae) or their derivatives obtained by chemical conversion, were tested for their effect on cholesterol biosynthesis from 24,25-dihydrolanosterol by rat hepatic subscellular 10,000 x g supernatant fraction. The sterol (VI, 40 μM) with 7-oxo and 15α-hydroxy groups potently inhibited the synthesis of cholesterol from [24,25-^3H]-24,25-dihydrolanosterol (18 μM).