源自海绵的真菌中的四咪酸衍生物和多酚及其生物学评价。

Tetramic acid derivatives and polyphenols from sponge-derived fungus and their biological evaluation.

作者信息

Wang Jun-Feng, Qin Xiaochu, Xu Fu-Quan, Zhang Tianyu, Liao Shengrong, Lin Xiuping, Yang Bin, Liu Juan, Wang Lishu, Tu Zhengchao, Liu Yonghong

机构信息

a CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, RNAM Center for Marine Microbiology, Chinese Academy of Sciences , Guangzhou 510301 , P.R. China.

出版信息

Nat Prod Res. 2015;29(18):1761-5. doi: 10.1080/14786419.2014.999061. Epub 2015 Jan 9.

DOI:10.1080/14786419.2014.999061

PMID:25573692

Abstract

Fifteen compounds, including two tetramic acid derivatives, penicillenol A1 (1) and penicillenol A2 (2), six polyphenols containing both phenolic bisabolane sesquiterpenoid and diphenyl ether units, expansols A-F (3-8), together with six phenolic bisabolane sesquiterpenoids (9-14) and diorcinol (15), were isolated from the fermentation broth of the marine-derived fungus ZSDS1-F11 isolated from the sponge Phakellia fusca Thiele collected in the Yongxing island of Xisha. Their structures were elucidated mainly by using extensive NMR spectroscopic and mass spectrometric analyses. Compounds 3-5, 7 and 8 showed potent COX-1 inhibitory activity with IC50 values of 5.3, 16.2, 30.2, 41.0 and 56.8 μM, respectively. Meanwhile, compounds 3-8 showed potent COX-2 inhibitory activity with IC50 values of 3.1, 5.6, 3.0, 5.1, 3.2 and 3.7 μM, respectively. In addition, compound 1 exhibited antituberculosis activity with 96.1% inhibition at concentration of 10 μM.

摘要

从采自西沙永兴岛的海绵Phakellia fusca Thiele中分离得到的海洋来源真菌ZSDS1-F11的发酵液中，分离出了15种化合物，包括两种四嗪酸衍生物青霉烯醇A1（1）和青霉烯醇A2（2）、六种同时含有酚类没药烷倍半萜和二苯醚单元的多酚类化合物 expansols A-F（3-8），以及六种酚类没药烷倍半萜（9-14）和二氢间苯二酚（15）。它们的结构主要通过广泛的核磁共振光谱和质谱分析来阐明。化合物3-5、7和8表现出较强的COX-1抑制活性，IC50值分别为5.3、16.2、30.2、41.0和56.8 μM。同时，化合物3-8表现出较强的COX-2抑制活性，IC50值分别为3.1、5.6、3.0、5.1、3.2和3.7 μM。此外，化合物1在浓度为10 μM时表现出抗结核活性，抑制率为96.1%。