Discovery of clostrubin, an exceptional polyphenolic polyketide antibiotic from a strictly anaerobic bacterium

Angew Chem Int Ed Engl. 2014 Jul 21;53(30):7856-9. doi: 10.1002/anie.201402632. Epub 2014 May 14.

Abstract

Genome mining of the strictly anaerobic bacterium Clostridium beijerinckii, an industrial producer of solvents, revealed the presence of several cryptic gene clusters for secondary metabolite biosynthesis. To unearth its metabolic potential, a C. beijerinckii strain was cultured under various conditions, which led to the discovery of a deep purple pigment. This novel metabolite, named clostrubin (1), was isolated and its structure was fully elucidated. The pentacyclic polyphenol features a benzo[a]tetraphene ring topology that is unprecedented for natural products. Stable-isotope labeling experiments showed that 1 is an aromatic polyketide that folds in a noncanonical manner to form the unusual perifused ring system. In addition to being the first reported polyketide from an anaerobic bacterium, 1 is a potent antibiotic with pronounced activity against various pathogenic bacteria, such as MRSA, VRE, and mycobacteria, with minimum inhibitory concentrations (MIC) of 0.12-0.97 μM.

Keywords: Clostridium beijerinckii; anaerobes; antibiotics; polyketides; polyphenols.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / biosynthesis
  • Anti-Bacterial Agents / isolation & purification*
  • Anti-Bacterial Agents / pharmacology
  • Chromatography, High Pressure Liquid
  • Clostridium beijerinckii / chemistry*
  • Clostridium beijerinckii / metabolism
  • Drug Discovery
  • Microbial Sensitivity Tests
  • Phenols / isolation & purification*
  • Phenols / pharmacology
  • Polycyclic Aromatic Hydrocarbons / isolation & purification*
  • Polycyclic Aromatic Hydrocarbons / pharmacology
  • Polyketides / isolation & purification*
  • Polyketides / pharmacology

Substances

  • Anti-Bacterial Agents
  • Phenols
  • Polycyclic Aromatic Hydrocarbons
  • Polyketides
  • clostrubin