Lugdunomycin, an Angucycline-Derived Molecule with Unprecedented Chemical Architecture

Angew Chem Int Ed Engl. 2019 Feb 25;58(9):2809-2814. doi: 10.1002/anie.201814581. Epub 2019 Jan 29.

Abstract

The angucyclines form the largest family of polycyclic aromatic polyketides, and have been studied extensively. Herein, we report the discovery of lugdunomycin, an angucycline-derived polyketide, produced by Streptomyces species QL37. Lugdunomycin has unique structural characteristics, including a heptacyclic ring system, a spiroatom, two all-carbon stereocenters, and a benzaza-[4,3,3]propellane motif. Considering the structural novelty, we propose that lugdunomycin represents a novel subclass of aromatic polyketides. Metabolomics, combined with MS-based molecular networking analysis of Streptomyces sp. QL37, elucidated 24 other rearranged and non-rearranged angucyclines, 11 of which were previously undescribed. A biosynthetic route for the lugdunomycin and limamycins is also proposed. This work demonstrates that revisiting well-known compound families and their producer strains still is a promising approach for drug discovery.

Keywords: Baeyer-Villiger oxidation; angucycline; molecular networking; natural product; polyketide.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / metabolism
  • Anti-Bacterial Agents / pharmacology*
  • Bacillus subtilis / drug effects*
  • Escherichia coli / drug effects*
  • Metabolomics
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Molecular Conformation
  • Polyketides / chemistry
  • Polyketides / metabolism
  • Polyketides / pharmacology*
  • Streptomyces / chemistry

Substances

  • Anti-Bacterial Agents
  • Polyketides