<p>Eleven diketopiperazine and fumiquinazoline alkaloids (<b>1–11</b>) together with a tetracyclic triterpenoid helvolic acid (<b>12</b>) were obtained from the cultures of a deep-sea derived fungus <i>Aspergillus</i> sp. SCSIO Ind09F01. The structures of these compounds (<b>1</b>–<b>12</b>) 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 (<b>3</b>), 12,13-dihydroxy-fumitremorgin C (<b>11</b>) and helvolic acid (<b>12</b>) exhibited very strong anti-tuberculosis activity towards <i>Mycobacterium tuberculosis</i> with the prominent MIC<sub>50</sub> values of <0.03, 2.41 and 0.894 μM, respectively, which was here reported for the first time. Meanwhile gliotoxin also displayed significant selective cytotoxicities against K562, A549 and Huh-7 cell lines with the IC<sub>50</sub> values of 0.191, 0.015 and 95.4 μM, respectively.</p
