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

作者：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

来源：Natural Product Research, 2017, 31(16): 1958-1962.

DOI：10.1080/14786419.2016.1266353

• Deep sea fungi
• Aspergillus sp
• anti-tuberculosis
• alkaloids

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 MIC50 values of <0.03, 2.41 and 0.894M, 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 IC50 values of 0.191, 0.015 and 95.4M, respectively. @@@ [GRAPHICS] @@@ .

• 出版日期2017
• 单位南方医科大学; 呼吸疾病国家重点实验室; 中国科学院大学; 中国科学院广州生物医药与健康研究院; 南通大学