Litcius/Paper detail

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

Mingqiong Li, Saini Li, Jinhua Hu, Xiaoxia Gao, Yanlin Wang, Zhaoming Liu, Weimin Zhang

2021Marine Drugs29 citationsDOIOpen Access PDF

Abstract

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 α-glucosidase with an IC50 value of 5.4 μM, while compounds 4 and 5 showed moderate effects with IC50 values of 33.6 and 72.1 μM, respectively. A preliminary structure–activity relationship is discussed and a docking analysis was performed.

Topics & Concepts

ThioesterIC50FungusChemistryStereochemistryEnzymeBiochemistryIn vitroBiologyBotanySulfur-Based Synthesis TechniquesMicrobial Natural Products and BiosynthesisCarbohydrate Chemistry and Synthesis