Asperlones A and B, Dinaphthalenone Derivatives from a Mangrove Endophytic Fungus Aspergillus sp. 16-5C

Marine Drugs

Ze𠆞n Xiao¹  Shao𠆞 Lin¹  Chunbing Tan¹  Yongjun Lu²  Lei He²  Xishan Huang¹  Zhigang She¹ 

[1] School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China; E-Mails:;School of Life Sciences and Biomedical Center, Sun Yat-sen University, Guangzhou 510275, China; E-Mails:

关键词: marine fungi;    Aspergillus sp.;    asperlones;    azaphilones;    MptpB inhibitor;   

DOI  :  10.3390/md13010366

来源: mdpi

【 摘 要 】

Racemic dinaphthalenone derivatives, (±)-asperlone A (1) and (±)-asperlone B (2), and two new azaphilones, 6″-hydroxy-(R)-mitorubrinic acid (3) and purpurquinone D (4), along with four known compounds, (−)-mitorubrinic acid (5), (−)-mitorubrin (6), purpurquinone A (7) and orsellinic acid (8), were isolated from the cultures of Aspergillus sp. 16-5C. The structures were elucidated using comprehensive spectroscopic methods, including 1D and 2D NMR spectra and the structures of 1 further confirmed by single-crystal X-ray diffraction analysis, while the absolute configuration of 3 and 4 were determined by comparing their optical rotation and CD with those of the literature, respectively. Compounds 1, 2 and 6 exhibited potent inhibitory effects against Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) with IC₅₀ values of 4.24 ± 0.41, 4.32 ± 0.60 and 3.99 ± 0.34 μM, respectively.

【 授权许可】

CC BY   
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