4.7 Article

Bioactive Azaphilone Derivatives from the Fungus Talaromyces aculeatus

Journal

JOURNAL OF NATURAL PRODUCTS
Volume 80, Issue 8, Pages 2199-2203

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.7b00032

Keywords

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Funding

  1. National Natural Science Foundation of China [41606174]
  2. Natural Science Foundation of Hebei Province of China [B2017201059]
  3. Scientific Research Foundation of Hebei Educational Committee [ZD2017004]
  4. Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University), Ministry of Education of China [CMEMR2017-B07]
  5. High Performance Computer Center of Hebei University

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Six new azaphilone derivatives, talaraculones A-F (1-6), together with five known analogues (7-11), were obtained from the saline soil-derived fungus Talaromyces aculeatus. The absolute configurations of 1 and 6 were assigned by quantum chemical calculations of the electronic circular dichroism (ECD) spectra. Compounds 1 and 5 represent the first reported azaphilone derivatives with a C4 aliphatic side chain and a methylal group at C-3, respectively. Talaraculones A and B (1 and 2) exhibited stronger inhibitory activity against alpha-glucosidase than the positive control acarbose (IC50 = 101.5 mu M), with IC50 values of 78.6 and 22.9 mu M respectively.

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