A new pentanorlanostane, ganosineniol A (1), eight new lanostane triterpenoids, ganosinoside A (2), ganoderic acid Jc (3), ganoderic acid Jd (4), ganodermatetraol (5), ganolucidic acid.a (6), ganolucidate F (7), ganoderiol J (8), and methyl lucidenate Ha (9), and a new sesquiterpenoid, ganosinensine (10), together with eleven known triterpenoids (11-21), were isolated from the fruiting bodies of the fungus Ganoderma sinense. Chemical structures were determined based on spectroscopic evidence, including 1D, 2D NMR, and mass spectral data. Furthermore, all isolates were tested for cytotoxic activity and induction ability of hPXR-mediated CYP3A4 expression. Among them, ganoderic acid Jc (3) displayed selective inhibitory activity against HL-60 cells (IC50 = 8.30 mu M), and ganoderiol E (11) exhibited selective cytotoxic activity against MCF-7 cells (IC50 = 6.35 mu M). Meanwhile, compounds 5, 7, and ganolucidic acids B and C (19, 20) showed induction ability of hPXR-mediated CYP3A4 expression.