Herpotrichones A and B, Two Intermolecular [4 + 2] Adducts with Anti-Neuroinflammatory Activity from a Herpotrichia Species

Org Lett. 2020 Jan 17;22(2):405-409. doi: 10.1021/acs.orglett.9b04099. Epub 2019 Dec 24.

Abstract

Herpotrichones A and B (1 and 2), two intermolecular [4 + 2] adducts with an unprecedented pentacyclic 6/6/6/6/3 skeleton, were isolated from Herpotrichia sp. SF09, an isopod-associated fungus, along with a new shunt product protrichone (3). Their structures were elucidated by the analysis of spectroscopic data, residual dipolar coupling (RDC)-based computer-assisted 3D structure elucidation (CASE-3D), and single-crystal X-ray diffraction in combination with electronic circular dichroism (ECD) calculations. Compounds 1 and 2 were assessed to be potent anti-neuroinflammatory agents in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) values of 0.41 and 0.11 μM, respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Ascomycota / chemistry*
  • Cell Line
  • Density Functional Theory
  • Heterocyclic Compounds, 4 or More Rings / chemical synthesis
  • Heterocyclic Compounds, 4 or More Rings / chemistry
  • Heterocyclic Compounds, 4 or More Rings / pharmacology*
  • Lipopolysaccharides / antagonists & inhibitors
  • Lipopolysaccharides / pharmacology
  • Mice
  • Microglia / drug effects*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Heterocyclic Compounds, 4 or More Rings
  • Lipopolysaccharides