The secondary metabolites of the endophytic fungus Aspergillus terreus TZS-201607 isolated from Pseudostellaria heterophyllawere fully studied.A total of 16 compounds were isolated from the EtOAc extracts of the PDB culture broth by means of chromatographic techniques,including silica gel,Sephadex LH-20 gel,reversed-phase and semi-preparative HPLC column chromatography.Their structures were identified as sterigmatocystin (1),5-methoxysterigmatocystin (2),variecoxanthone A（3）,chryxanthone A（4）,6,8-di-O-methylaverufin（5）,6,8-di-O-methylnidurufin（6）,6,8,1′-tri-O-methyl averantin（7）,(22E,24R)-ergosta-7,9(11),22-trien-3β-ol（8）,(22E,24R)-ergosta-4,6,8(14),22-trtraen-3-one（9）,(22E,24R)-3β,5α-dihydroxy-ergosta-7,22-dien-6-one（10）,(22E,24R)-3β,5α,9α-trihydroxy-ergosta-7,22-diene-6-one（11）,(22E,24R)-3α-ureido-ergosta-4,6,8(14),22-tetraene（12）,(22E,24R)-ergosta-7,22-dien-3β,5α,6β-triol（13）,(22E,24R)-5α,8α-epidioxyergosta-6,22-dien-3β-ol（14）,demethylincisterol A₃（15）and (17R)-17-methylincisterol（16）,by spectroscopic analysis and by comparison with previously reported literatures.Compounds 1-7,12,and 14-16 were isolated from the fungus A. terreus for the first time.The cytotoxicity of compounds 1-16 against A549,BT-549,HeLa,HepG2,MCF-7,and THP-1 cell lines was evaluated.Compounds 6,7,and 14 showed strong inhibitory activity against A549,BT-549,HeLa,and THP-1 cell lines,respectively (IC₅₀<10 μM).