Lipotrichaibol A and Trichoderpeptides A–D: Five New Peptaibiotics from a Sponge-Derived Trichoderma sp. GXIMD 01001

Five previously undescribed peptaibiotics, including one 7-mer lipopeptaibol named lipotrichaibol A (<b>1</b>), and four 11-mer peptaibiotics named trichoderpeptides A-D (<b>2</b>-<b>5</b>) were isolated from the rice culture medium of the sponge-derived fungus <i>Trichoderma</i> sp. GXIMD 01001. Their structures and absolute configurations were unambiguously established by extensive spectroscopic data analysis and advanced Marfey's method. All isolated compounds were evaluated via CCK8 bioassays to investigate their antiproliferative activity. Only compound <b>1</b> exerted potent cytotoxicity against HT-29 and DLD-1 cells with IC₅₀ values at 10.3 ± 1.9 and 12.31 ± 1.5 μM, respectively. In further in vitro bioassay, compound <b>1</b> exhibited significant inhibition in colony formation assay, induced apoptosis and blocked the cell cycle in the G0/G1 phase. The mechanism may be related to the regulation of the Erk1/2 signaling pathway.