An Esterase-Sensitive Prodrug Approach for Controllable Delivery of Persulfide Species

Angew Chem Int Ed Engl. 2017 Sep 18;56(39):11749-11753. doi: 10.1002/anie.201704117. Epub 2017 Aug 16.

Abstract

A strategy to deliver a well-defined persulfide species in a biological medium is described. Under near physiological conditions, the persulfide prodrug can be activated by an esterase to generate a "hydroxymethyl persulfide" intermediate, which rapidly collapses to form a defined persulfide. Such persulfide prodrugs can be used either as chemical tools to study persulfide chemistry and biology or for future development as H2 S-based therapeutic reagents. Using the persulfide prodrugs developed in this study, the reactivity between S-methyl methanethiosulfonate (MMTS) with persulfide was unambiguously demonstrated. Furthermore, a representative prodrug exhibited potent cardioprotective effects in a murine model of myocardial ischemia-reperfusion (MI/R) injury with a bell shape therapeutic profile.

Keywords: bell shape therapeutic profile; hydrogen sulfide; persulfide; prodrugs.

Publication types

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

MeSH terms

  • Activation, Metabolic
  • Animals
  • Cardiotonic Agents / administration & dosage
  • Cardiotonic Agents / chemistry
  • Cell Line
  • Dose-Response Relationship, Drug
  • Drug Development
  • Esterases / metabolism*
  • Methyl Methanesulfonate / analogs & derivatives
  • Methyl Methanesulfonate / chemistry
  • Mice
  • Myocardial Reperfusion Injury / prevention & control
  • Prodrugs / administration & dosage
  • Prodrugs / pharmacokinetics*
  • Sulfides / administration & dosage*
  • Sulfides / chemistry

Substances

  • Cardiotonic Agents
  • Prodrugs
  • Sulfides
  • persulfides
  • methyl methanethiosulfonate
  • Methyl Methanesulfonate
  • Esterases