One new alkaloid, named 16 alpha-hydroxy-5 N-acetylardeemin (1), along with seven known metabolites (2-8) was isolated from the fermentation broth of an endophytic fungus, Aspergillus terreus. The structures of these metabolites were assigned on the basis of detailed spectroscopic analysis and by comparing spectroscopic data with those in the literature. Compound 1 displayed an inhibitory effect against acetylcholinesterase. Compounds 1-8 also showed moderate or weak cytotoxic activity against KB and HSC-T6 cell lines.