由海绵来源的菌株GXIMD 01001产生的18个残基的肽菌素

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

作者信息

Lin Xiao, Tang Zhenzhou, Gan Yuman, Li Zhengyuan, Luo Xiaowei, Gao Chenghai, Zhao Longyan, Chai Ling, Liu Yonghong

机构信息

Institute of Marine Drugs, Guangxi Key Laboratory of Marine Drugs, Guangxi University of Chinese Medicine, Nanning 530200, People's Republic of China.

Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards, Guangxi Institute of Chinese Medicine and Pharmaceutical Science, Nanning 530022, People's Republic of China.

出版信息

J Nat Prod. 2023 Apr 28;86(4):994-1002. doi: 10.1021/acs.jnatprod.3c00014. Epub 2023 Mar 22.

DOI:10.1021/acs.jnatprod.3c00014

PMID:36947873

Abstract

Seven new 18-residue peptaibols, trichorzins A-G (-), were isolated from the sponge-derived fungus 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-Aib-Ala/Ser-Ala-Aib/Iva-Iva-Gln-Aib/Iva-Val/-Ile-Aib-Gly-Leu-Aib-Pro-Leu-Aib-Aib-Gln-Trpol/Pheol. 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 IC values at 0.46-4.7 μM against four human carcinoma cell lines.

摘要

从海绵来源的真菌sp. GXIMD 01001中分离出七种新的18个残基的肽菌素，即曲古抑菌素A-G（-）。通过对核磁共振光谱数据、串联质谱碎片分析、马尔菲方法和电子圆二色光谱分析的综合解读，确定了它们的结构和构型。曲古抑菌素A-G的一般序列如下：Ac-Aib-Ala/Ser-Ala-Aib/Iva-Iva-Gln-Aib/Iva-Val/-Ile-Aib-Gly-Leu-Aib-Pro-Leu-Aib-Aib-Gln-Trpol/Pheol。对所得到的化合物进行了潜在的抗增殖和抗菌活性评估。所有得到的化合物均未表现出强效抗菌活性，但均表现出显著的细胞毒性，对四种人类癌细胞系的最低半数抑制浓度值在0.46-4.7 μM之间。