Developing polyphenolic acetates as radiation countermeasure agents: current status and future perspectives. Issue 4 (April 2020)

• Record Type: Journal Article
• Authors: Venkateswaran, Kavya; Shrivastava, Anju; Prasad, Ashok K.; Parmar, Virinder S.; Dwarakanath, Bilikere S.
• Is Part Of: Drug discovery today. Volume 25:Issue 4(2020)
• Page Start: 781
• Page End: 786
• Publication Date: 2020-04
• Subjects: Drugs -- Design -- Periodicals; Drugs -- Research -- Periodicals; 615.1
• DOI: 10.1016/j.drudis.2020.02.004
• Languages: English
• ISSNs: 1359-6446

Abstract

Highlights: Acute radiation syndrome (ARS); protein acetylation in cellular radiation response. Semi-synthetic polyphenolic acetates (PAs) and modification of radiation response. We provide an insight into PAs as potential radiation countermeasure agents. PAs as mitigators of ARS; considerations in designing countermeasure agents. PAs as adjuvant in radiotherapy of tumors for protection of normal cells. 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.