脂毛链菌素A和木霉肽A-D：来自海绵源菌株GXIMD 01001的五种新型短肽抗生素。

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

作者信息

Yang Weichan, Tang Zhenzhou, Luo Xiaowei, Gan Yuman, Bai Meng, Lin Houwen, Gao Chenghai, Chai Ling, Lin Xiao

机构信息

Guangxi Key Laboratory of Marine Drugs, Institute of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, China.

Research Center for Marine Drugs, Department of Pharmacy, Ren Ji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200127, China.

出版信息

Mar Drugs. 2025 Jun 24;23(7):264. doi: 10.3390/md23070264.

DOI:10.3390/md23070264

PMID:40710489

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12298237/

Abstract

Five previously undescribed peptaibiotics, including one 7-mer lipopeptaibol named lipotrichaibol A (), and four 11-mer peptaibiotics named trichoderpeptides A-D (-) were isolated from the rice culture medium of the sponge-derived fungus 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 exerted potent cytotoxicity against HT-29 and DLD-1 cells with IC values at 10.3 ± 1.9 and 12.31 ± 1.5 μM, respectively. In further in vitro bioassay, compound 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.

摘要

从海绵来源的真菌木霉属GXIMD 01001的水稻培养基中分离出5种先前未描述的缩氨酸抗生素，包括一种名为脂曲霉肽A（）的7聚体脂肽醇，以及4种名为木霉肽A-D（-）的11聚体缩氨酸抗生素。通过广泛的光谱数据分析和先进的马尔费方法明确确定了它们的结构和绝对构型。通过CCK8生物测定法评估所有分离出的化合物，以研究它们的抗增殖活性。只有化合物对HT-29和DLD-1细胞表现出强大的细胞毒性，IC值分别为10.3±1.9和12.31±1.5μM。在进一步的体外生物测定中，化合物在集落形成试验中表现出显著抑制作用，诱导细胞凋亡并使细胞周期阻滞在G0/G1期。其机制可能与Erk1/2信号通路的调节有关。