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

作者：Xiao, Ze'en; Lin, Shao'e; Tan, Chunbing; Lu, Yongjun; He, Lei; Huang, Xishan^*; She, Zhigang

来源：Marine Drugs, 2015, 13(1): 366-378.

DOI：10.3390/md13010366

• marine fungi
• Aspergillus sp.
• asperlones
• azaphilones
• MptpB inhibitor

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 mu M, respectively.

• 出版日期2015-1
• 单位中山大学