Reducing Holomycin Thiosulfonate to its Disulfide with Thiols

Chem Res Toxicol. 2019 Mar 18;32(3):400-404. doi: 10.1021/acs.chemrestox.8b00243. Epub 2018 Dec 24.

Abstract

The dithiolopyrrolone (DTP) natural products contain a unique ene-disulfide that is essential for their antimicrobial and anticancer activities. The ene-disulfide in some DTPs is oxidized to a cyclic thiosulfonate, but it is unknown how the DTP thiosulfonates react with biomolecules. We studied the reactivity of the thiosulfonate derivative of the DTP holomycin, oxo-holomycin, and discovered a unique redox reaction: Oxo-holomycin is reduced to its parent disulfide, while oxidizing small molecule and protein thiols to disulfides. Our work reveals that the DTP core is a privileged scaffold that undergoes unusual redox chemistry. The redox chemistry of the DTP natural products may contribute to their mechanism of action.

Publication types

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

MeSH terms

  • Disulfides / chemistry*
  • Lactams / chemistry*
  • Molecular Structure
  • Oxidation-Reduction
  • Pyrrolidinones / chemistry*
  • Sulfhydryl Compounds / chemistry*
  • Sulfonic Acids / chemistry*

Substances

  • Disulfides
  • Lactams
  • Pyrrolidinones
  • Sulfhydryl Compounds
  • Sulfonic Acids
  • holomycin