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Planta Med 2015; 81 - PT20
DOI: 10.1055/s-0035-1556398
DOI: 10.1055/s-0035-1556398
Novel 22-mer peptaibols isolated from Tolypocladium sp. with potent antitumor activities
Genome mining of a Tolypocladium sp. isolate led to the purification and identification of gichigamin A (1), the first 22-mer and longest peptaibol from a natural source. The β-alanine rich sequence of 1 results in the assembly of an unprecedented 310-like helical structure, which was revealed by single-crystal X-ray diffraction analysis. The unique structural character of 1 was determined to be essential for its unexpected high penetrability through cell membranes. As a result, gichigamin A (1) exhibited potent in vitro cytotoxicity by direct disruption of mitochondrial function and the capability to inhibit MIA PaCa-2 xenograft tumor growth in nude mice.