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Developing polyphenolic acetates as radiation countermeasure agents: current status and future perspectives.
Drug Discovery Today ( IF 7.4 ) Pub Date : 2020-02-13 , DOI: 10.1016/j.drudis.2020.02.004
Kavya Venkateswaran 1 , Anju Shrivastava 1 , Ashok K Prasad 2 , Virinder S Parmar 3 , Bilikere S Dwarakanath 4
Affiliation  

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.

中文翻译:

发展多酚乙酸盐作为辐射对策剂:现状和未来展望。

全身暴露于电离辐射(TBI)会导致威胁生命的急性辐射综合症(ARS),其中包括造血和胃肠道(GI)损伤,并导致剂量依赖性的发病率和死亡率。ARS的管理层保证部署有效的医疗对策代理(MCM),以防止和/或减轻致命的放射伤害。多酚乙酸酯(PA)7,8-二乙酰氧基-4-甲基硫代香豆素(DAMTC)由于其减轻了T57在C57BL / 6小鼠中的致死作用,已被确定为对抗ARS的潜在MCM。本文中,我们描述了将PAs用作抗ARS的MCM的当前证据,包括机制方面的信息,并为将其用作缓解ARS的批准药物提供了进一步的发展前景。
更新日期:2020-02-13
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