Eleven diketopiperazine and fumiquinazoline alkaloids ( 1–11 ) together with a tetracyclic triterpenoid helvolic acid ( 12 ) were obtained from the cultures of a deep-sea derived fungus Aspergillus sp. SCSIO Ind09F01. The structures of these compounds ( 1 – 12 ) were determined mainly by the extensive NMR, ESIMS spectra data and by comparison with previously described compounds. Besides, anti-tuberculosis, cytotoxic, antibacterial, COX-2 inhibitory and antiviral activities of these compounds were evaluated. Gliotoxin ( 3 ), 12,13-dihydroxy-fumitremorgin C ( 11 ) and helvolic acid ( 12 ) exhibited very strong anti-tuberculosis activity towards Mycobacterium tuberculosis with the prominent MIC 50 values of