1. Academic Validation
  2. Lipotrichaibol A and Trichoderpeptides A-D: Five New Peptaibiotics from a Sponge-Derived Trichoderma sp. GXIMD 01001

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

  • Mar Drugs. 2025 Jun 24;23(7):264. doi: 10.3390/md23070264.
Weichan Yang 1 Zhenzhou Tang 1 Xiaowei Luo 1 Yuman Gan 1 Meng Bai 1 Houwen Lin 2 Chenghai Gao 1 Ling Chai 3 Xiao Lin 1
Affiliations

Affiliations

  • 1 Guangxi Key Laboratory of Marine Drugs, Institute of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, China.
  • 2 Research Center for Marine Drugs, Department of Pharmacy, Ren Ji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200127, China.
  • 3 Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards, Guangxi Institute of Chinese Medicine and Pharmaceutical Science, Nanning 530022, China.
Abstract

Five previously undescribed peptaibiotics, including one 7-mer lipopeptaibol named lipotrichaibol A (1), and four 11-mer peptaibiotics named trichoderpeptides A-D (2-5) were isolated from the rice culture medium of the sponge-derived fungus Trichoderma 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 1 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 1 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.

Keywords

Trichoderma sp.; cytotoxic activity; peptaibiotics; sponge-associated fungi.

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