Gephyronic acid, a novel inhibitor of eukaryotic protein synthesis from Archangium gephyra (myxobacteria). Production, isolation, physico-chemical and biological properties, and mechanism of action

J Antibiot (Tokyo). 1995 Jan;48(1):21-5. doi: 10.7164/antibiotics.48.21.

Abstract

A new antibiotic compound, gephyronic acid was isolated from the culture broth of the myxobacterium, Archangium gephyra strain Ar 3895. Up to 3 mg/liter was produced during the logarithmic and stationary growth phase. The compound is an aliphatic acid, which tends to form a hemiacetal. Both forms inhibited growth of yeasts and molds (MIC 1-25 micrograms/ml) and had a cytostatic effect on mammalian cell cultures (IC50 10-60 ng/ml). Gephyronic acid is a specific inhibitor of eukaryotic protein synthesis showing an IC50 of 1-2 x 10(-7) mol/liter in an in vitro translation assay.

MeSH terms

  • Animals
  • Antifungal Agents / biosynthesis
  • Antifungal Agents / chemistry*
  • Antifungal Agents / pharmacology*
  • Cell Division / drug effects
  • Chemical Phenomena
  • Chemistry, Physical
  • Fatty Acids, Monounsaturated / chemistry
  • Fatty Acids, Monounsaturated / metabolism
  • Fatty Acids, Monounsaturated / pharmacology
  • Fibroblasts / drug effects
  • Fibroblasts / metabolism
  • Humans
  • Leukemia, Experimental / drug therapy
  • Leukemia, Experimental / metabolism
  • Mice
  • Myxococcales / chemistry*
  • Myxococcales / metabolism*
  • Protein Biosynthesis* / drug effects
  • Proteins / drug effects*
  • Rabbits
  • Tumor Cells, Cultured
  • Yeasts / drug effects
  • Yeasts / metabolism

Substances

  • Antifungal Agents
  • Fatty Acids, Monounsaturated
  • Proteins
  • gephyronic acid