来自深海真菌曲霉属菌株SCSIO Ind09F01的抗结核化合物。

Antituberculosis compounds from a deep-sea-derived fungus Aspergillus sp. SCSIO Ind09F01.

作者信息

Luo Xiaowei, Zhou Xuefeng, Lin Xiuping, Qin Xiaochu, Zhang Tianyu, Wang Junfeng, Tu Zhengchao, Yang Bin, Liao Shengrong, Tian Yongqi, Pang Xiaoyan, Kaliyaperumal Kumaravel, Li Jian Lin, Tao Huaming, Liu Yonghong

机构信息

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

b University of Chinese Academy of Sciences , Beijing , P.R. China.

出版信息

Nat Prod Res. 2017 Aug;31(16):1958-1962. doi: 10.1080/14786419.2016.1266353. Epub 2017 Jan 9.

DOI:10.1080/14786419.2016.1266353

PMID:28068839

Abstract

Eleven diketopiperazine and fumiquinazoline alkaloids (1-11) together with a tetracyclic triterpenoid helvolic acid (12) were obtained from the cultures of a deep-sea derived fungus Aspergillus sp. SCSIO Ind09F01. The structures of these compounds (1-12) were determined mainly by the extensive NMR, ESIMS spectra data and by comparison with previously described compounds. Besides, anti-tuberculosis, cytotoxic, antibacterial, COX-2 inhibitory and antiviral activities of these compounds were evaluated. Gliotoxin (3), 12,13-dihydroxy-fumitremorgin C (11) and helvolic acid (12) exhibited very strong anti-tuberculosis activity towards Mycobacterium tuberculosis with the prominent MIC values of <0.03, 2.41 and 0.894 μM, respectively, which was here reported for the first time. Meanwhile gliotoxin also displayed significant selective cytotoxicities against K562, A549 and Huh-7 cell lines with the IC values of 0.191, 0.015 and 95.4 μM, respectively.

摘要

从一株深海来源的曲霉属真菌Aspergillus sp. SCSIO Ind09F01的培养物中获得了11种二酮哌嗪和烟曲喹唑啉生物碱（1-11）以及一种四环三萜类化合物赫沃酸（12）。这些化合物（1-12）的结构主要通过广泛的核磁共振、电喷雾离子化质谱光谱数据以及与先前描述的化合物进行比较来确定。此外，还评估了这些化合物的抗结核、细胞毒性、抗菌、环氧合酶-2抑制和抗病毒活性。Gliotoxin（3）、12,13-二羟基-烟曲霉震颤素C（11）和赫沃酸（12）对结核分枝杆菌表现出非常强的抗结核活性，其显著的最低抑菌浓度值分别为<0.03、2.41和0.894 μM，这是首次在此报道。同时，Gliotoxin对K562、A549和Huh-7细胞系也表现出显著的选择性细胞毒性，其半数抑制浓度值分别为0.191、0.015和95.4 μM。