开发多酚醋酸酯作为辐射防护剂：现状与未来展望。

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

作者信息

Venkateswaran Kavya, Shrivastava Anju, Prasad Ashok K, Parmar Virinder S, Dwarakanath Bilikere S

机构信息

Department of Zoology, University of Delhi, Delhi 110007, India.

Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110007, India.

出版信息

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

DOI:10.1016/j.drudis.2020.02.004

PMID:32062010

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.

摘要

全身暴露于电离辐射（TBI）会导致危及生命的急性放射综合征（ARS），ARS包括造血和胃肠道（GI）损伤，并导致剂量依赖性的发病率和死亡率。ARS的管理需要部署有效的医学对策剂（MCM），以预防和/或减轻致命的辐射损伤。多酚乙酸酯（PA）7,8-二乙酰氧基-4-甲基硫代香豆素（DAMTC）已被确定为一种潜在的抗ARS的MCM，因为它能减轻C57BL/6小鼠中TBI的致死效应。在此，我们描述了将PA用作抗ARS的MCM的当前证据，包括其作用机制方面，并为其作为减轻ARS的获批药物的进一步开发提供了前景。