Bioactive Metabolites from Mangrove Endophytic Fungus Aspergillus sp. 16-5B

Marine Drugs

Yayue Liu¹  Senhua Chen¹  Zhaoming Liu¹  Yongjun Lu²  Guoping Xia¹  Hongju Liu¹  Lei He²  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, 135 Xin gang West Road, Guangzhou 510275, China; E-Mails:

关键词: marine fungi;    Aspergillus sp.;    α-glucosidase inhibitor;    theoretical calculations;    ECD;    optical rotation;   

DOI  :  10.3390/md13053091

来源: mdpi

【 摘 要 】

Chemical investigation of the endophytic fungus Aspergillus sp. 16-5B cultured on Czapek’s medium led to the isolation of four new metabolites, aspergifuranone (1), isocoumarin derivatives (±) 2 and (±) 3, and (R)-3-demethylpurpurester A (4), together with the known purpurester B (5) and pestaphthalides A (6). Their structures were determined by analysis of 1D and 2D NMR spectroscopic data. The absolute configuration of Compound 1 was determined by comparison of the experimental and calculated electronic circular dichroism (ECD) spectra, and that of Compound 4 was revealed by comparing its optical rotation data and CD with those of the literature. The structure of Compound 6 was further confirmed by single-crystal X-ray diffraction experiment using CuKα radiation. All isolated compounds were evaluated for their α-glucosidase inhibitory activities, and Compound 1 showed significant inhibitory activity with IC₅₀ value of 9.05 ± 0.60 μM. Kinetic analysis showed that Compound 1 was a noncompetitive inhibitor of α-glucosidase. Compounds 2 and 6 exhibited moderate inhibitory activities.

【 授权许可】

CC BY   
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