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从红树林内生真菌ML-P8-2中分离出两种具有强效抗菌和细胞毒性活性的短肽菌素。

Isolation of two peptaibols with potent antimicrobial and cytotoxic activities from the mangrove endophytic fungus ML-P8-2.

作者信息

Yin Yihao, Zhu Ge, Wu Jianying, She Zhigang, Yuan Jie, Wang Bo

机构信息

School of Chemistry, Sun Yat-sen University, Guangzhou, China.

Department of Biochemistry, Zhongshan School of Medicine, Sun Yat-sen University, Guangzhou, China.

出版信息

Nat Prod Res. 2025 Jun;39(12):3376-3381. doi: 10.1080/14786419.2024.2334880. Epub 2024 Mar 27.

Abstract

Trichorzin PA is a family of 18-residue peptaibols with linear and flexible peptide chains. The three-dimensional structures and biological activities of trichorzin PA peptaibols are largely uncharacterised. In this work, two previously identified peptaibols, trichorzin PA VI () and II (), were isolated from ML-P8-2. While for the first time, we report here the X-ray crystallographic structure of , antimicrobial activities against a panel of common pathogenic bacteria and fungi, and cytotoxicities of and . In bioassays, and exhibited strong antimicrobial activities against the seven tested microbes, with MIC values in the range of 0.19-6.25 μM. Additionally, and displayed potent cytotoxicities against five human cancer cell lines, with IC values in the range of 0.01 ± 0.02-2.75 ± 0.17 μM. The bioassay results were generally better than those reported for other 18-residue peptaibols, including other trichorzin PA members.

摘要

Trichorzin PA是一类由18个残基组成的肽抗生素,其肽链呈线性且具有柔性。Trichorzin PA肽抗生素的三维结构和生物活性在很大程度上尚未得到表征。在这项工作中,从ML-P8-2中分离出了两种先前鉴定的肽抗生素,即Trichorzin PA VI()和II()。我们首次在此报告了的X射线晶体学结构、对一组常见病原菌和真菌的抗菌活性以及和的细胞毒性。在生物测定中,和对七种测试微生物表现出较强的抗菌活性,MIC值在0.19 - 6.25μM范围内。此外,和对五种人类癌细胞系显示出较强的细胞毒性,IC值在0.01±0.02 - 2.75±0.17μM范围内。生物测定结果总体上优于其他18个残基的肽抗生素所报道的结果,包括其他Trichorzin PA成员。

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