Developing polyphenolic acetates as radiation countermeasure agents: current status and future perspectives

Drug Discov Today. 2020 Apr;25(4):781-786. doi: 10.1016/j.drudis.2020.02.004. Epub 2020 Feb 13.

Abstract

Total-body exposure to ionizing radiation (TBI) results in life-threatening acute radiation syndrome (ARS), which encompasses hematopoietic and gastrointestinal (GI) injuries and results in dose-dependent morbidity and mortality. Management of ARS warrants the deployment of effective medical countermeasure agents (MCM) that protect against and/or mitigate lethal radiation injury. The polyphenolic acetate (PA) 7,8-diacetoxy-4-methylthiocoumarin (DAMTC) has been identified as a potential MCM against ARS by virtue of it mitigating the lethal effects of TBI in C57BL/6 mice. Herein, we describe current evidence, including mechanistic aspects, for the use of PAs as MCMs against ARS and provide perspectives for their further development as approved drugs for the mitigation of ARS.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Acute Radiation Syndrome / prevention & control*
  • Animals
  • Coumarins / pharmacology*
  • Disease Models, Animal
  • Drug Development
  • Humans
  • Mice
  • Mice, Inbred C57BL
  • Polyphenols / pharmacology
  • Radiation Injuries, Experimental / prevention & control
  • Radiation-Protective Agents / pharmacology*

Substances

  • 7,8-diacetoxy-4-methylthiocoumarin
  • Coumarins
  • Polyphenols
  • Radiation-Protective Agents