The marine environment has recently been described as a source of novel chemical diversity for drug discovery, as many bioactive substances are isolated from marine organisms, including phytoplankton, algae, sponges, tunicates and mollusks. Our group has reported the isolation of azaspiracid-2 from marine sponges. Microorganisms from marine habitats, especially fungi, also constitute a promising untapped resource for discovering novel bioactive substances such as diketopiperazine alkaloids, trichodermatides and carbonarones. We also have reported new sesquiterpenes—JBIR-27 and JBIR-28—from a tunicate-derived fungus Penicillium sp. SS080624SCf1, a new aspochracin derivative—JBIR-15—from a marine sponge-derived fungus Aspergillus sclerotiorum Huber Sp080903f04, and new glycosyl benzenediols—JBIR-37 and JBIR-38—from a marine sponge-derived fungus, Acremonium sp. SpF080624G1f01. Further investigation resulted in the discovery of two new terpeptin analogs, designated as JBIR-81 (1) and JBIR-82 (2), together with terpeptin (3), from the culture of a marine-derived Aspergillus sp. SpD081030G1f1 (Figure 1a). This paper describes the fermentation, isolation, structure elucidation, and in brief, the biological activity of 1 and 2.