18-Residue Peptaibols Produced by the Sponge-Derived Trichoderma sp. GXIMD 01001

Seven new 18-residue peptaibols, trichorzins A-G (1-7), were isolated from the sponge-derived fungus Trichoderma sp. GXIMD 01001. Their structures and configurations were characterized by a comprehensive interpretation of the NMR spectroscopic data, MS/MS fragmentation, Marfey's method, and ECD analysis. The general sequences of trichorzins A-G are as follows: Ac-Aib¹-Ala/Ser²-Ala³-Aib/Iva⁴-Iva⁵-Gln⁶-Aib/Iva⁷-Val/allo-Ile⁸-Aib⁹-Gly¹⁰-Leu¹¹-Aib¹²-Pro¹³-Leu¹⁴-Aib¹⁵-Aib¹⁶-Gln¹⁷-Trpol/Pheol¹⁸. The obtained compounds were assessed for their potential antiproliferative and antimicrobial activities. All obtained compounds did not show potent antibacterial activity but exhibited significant cytotoxicity, with the lowest IC₅₀ values at 0.46-4.7 μM against four human carcinoma cell lines.