4.7 Article

Thioester-Containing Benzoate Derivatives with α-Glucosidase Inhibitory Activity from the Deep-Sea-Derived Fungus Talaromyces indigoticus FS688

Journal

MARINE DRUGS
Volume 20, Issue 1, Pages -

Publisher

MDPI
DOI: 10.3390/md20010033

Keywords

thioester-containing benzoate; deep-sea-derived fungus; alpha-glucosidase inhibitory activity; docking study

Funding

  1. National Natural Science Foundation of China [41906106, 31272087, 41876052]
  2. GDAS' Project of Science and Technology Development [2019GDASYL-0103007]
  3. Guangdong Provincial Special Fund for Marine Economic Development Project [GDNRC [2020]042]
  4. Guangdong MEDP fund [GDOE [2019]A35]
  5. NSFC Shiptime Sharing Project [41849906, 41949906]

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Eurothiocins C-H (1-6) and Eurothiocin A were isolated from a deep-sea-derived fungus, with compound 1 showing significant inhibitory activity against alpha-glucosidase. Compound 4 and 5 exhibited moderate effects.
Eurothiocins C-H (1-6), six unusual thioester-containing benzoate derivatives, were isolated from the deep-sea-derived fungus Talaromyces indigoticus FS688 together with a known analogue eurothiocin A (7). Their structures were elucidated through spectroscopic analysis and the absolute configurations were determined by X-ray diffraction and ECD calculations. In addition, compound 1 exhibited significant inhibitory activity against alpha-glucosidase with an IC50 value of 5.4 mu M, while compounds 4 and 5 showed moderate effects with IC50 values of 33.6 and 72.1 mu M, respectively. A preliminary structure-activity relationship is discussed and a docking analysis was performed.

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