X-ray, structural assignment and molecular docking study of dihydrogeodin from Aspergillus Terreus TM8

Nat Prod Res. 2019 Jan;33(1):117-121. doi: 10.1080/14786419.2018.1431642. Epub 2018 Feb 1.

Abstract

A re-cultivation of the thermophilic fungus Aspergillus terreus TM8, and working up of its extract afforded the dichloro-benzophenone derivative, dihydrogeodin (1) in addition to the butyrolactones I (2), V (3) and VI (4). A literature surveying revealed one recent structural assignment trial for dihydrogeodin (1), however, with some inaccuracies. We report herein a full assignment of dihydrogeodin (1) using extensive study of 1D, 2D NMR and ESI HR mass data. For the first time as well, we report the planar structure of 1 using X-ray crystallography. Docking and molecular dynamic simulation of dihydrogeodin (1) on the isomerase cyclophilin A has revealed its significant potential activity as an antiviral and immunosuppressive agent.

Keywords: TM8; Crystal structure; dihydrogeodin; molecular docking; thermophilic fungi.

MeSH terms

  • 4-Butyrolactone / analogs & derivatives
  • 4-Butyrolactone / chemistry
  • 4-Butyrolactone / isolation & purification
  • Antiviral Agents / chemistry
  • Antiviral Agents / isolation & purification*
  • Antiviral Agents / pharmacology
  • Aspergillus / chemistry*
  • Benzofurans / chemistry*
  • Benzofurans / isolation & purification
  • Benzofurans / metabolism
  • Benzophenones / chemistry
  • Crystallography, X-Ray
  • Cyclophilin A / metabolism
  • Immunosuppressive Agents / chemistry
  • Immunosuppressive Agents / isolation & purification*
  • Immunosuppressive Agents / pharmacology
  • Molecular Docking Simulation
  • Molecular Dynamics Simulation
  • Molecular Structure

Substances

  • Antiviral Agents
  • Benzofurans
  • Benzophenones
  • Immunosuppressive Agents
  • geodin
  • benzophenone
  • butyrolactone I
  • Cyclophilin A
  • 4-Butyrolactone