Glionitrin A, an antibiotic-antitumor metabolite derived from competitive interaction between abandoned mine microbes

J Nat Prod. 2009 Feb 27;72(2):248-52. doi: 10.1021/np800606e.

Abstract

The nutrient conditions present in abandoned coal mine drainages create an extreme environment where defensive and offensive microbial interactions could be critical for survival and fitness. Coculture of a mine drainage-derived Sphingomonas bacterial strain, KMK-001, and a mine drainage-derived Aspergillus fumigatus fungal strain, KMC-901, resulted in isolation of a new diketopiperazine disulfide, glionitrin A (1). Compound 1 was not detected in monoculture broths of KMK-001 or KMC-901. The structure of 1, a (3S,10aS) diketopiperazine disulfide containing a nitro aromatic ring, was based on analysis of MS, NMR, and circular dichroism spectra and confirmed by X-ray crystal data. Glionitrin A displayed significant antibiotic activity against a series of microbes including methicillin-resistant Staphylococcus aureus. An in vitro MTT cytotoxicity assay revealed that 1 had potent submicromolar cytotoxic activity against four human cancer cell lines: HCT-116, A549, AGS, and DU145. The results provide further evidence that microbial coculture can produce novel biologically relevant molecules.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / isolation & purification*
  • Anti-Bacterial Agents / pharmacology*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / isolation & purification*
  • Antineoplastic Agents / pharmacology*
  • Aspergillus / chemistry
  • Aspergillus / metabolism*
  • Coal Mining
  • Crystallography, X-Ray
  • Diketopiperazines / chemistry
  • Diketopiperazines / isolation & purification*
  • Diketopiperazines / pharmacology
  • Drug Screening Assays, Antitumor
  • HCT116 Cells
  • Humans
  • Methicillin-Resistant Staphylococcus aureus / drug effects
  • Molecular Conformation
  • Molecular Structure
  • Sphingomonas / chemistry
  • Sphingomonas / metabolism*

Substances

  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Diketopiperazines
  • glionitrin A