应用化学 ›› 2021, Vol. 38 ›› Issue (4): 407-413.DOI: 10.19894/j.issn.1000-0518.200357

• 研究论文 • 上一篇    下一篇

咪唑类氮氧自由基的合成及其对细胞辐射损伤的防护效应

杨青青, 王时雨, 薛姗姗, 何炜*   

  1. 中国人民解放军空军军医大学药学系,化学制药学教研室,西安 710000
  • 发布日期:2021-06-01
  • 通讯作者: *E-mail:weihechem@fmmu.edu.cn
  • 基金资助:
    国家自然科学基金(No.21272272)和陕西省重点研发计划(No.2019ZDLSF03-03)资助

Protecting Effects of Titronyl Nitroxide Radicals on Radiation Damage of Cells

YANG Qing-Qing, WANG Shi-Yu, XUE Shan-Shan, HE Wei*   

  1. Department of Chemistry, School of Pharmacy, the Fourth Military Medical University, Xi'an 710032, China
  • Online:2021-06-01
  • Supported by:
    Supported by the National Natural Science Foundation of China (No.21272272) and the Key Research and Development Program of Shaanxi Province (No.2019ZDLSF03-03)

摘要: 人在短暂时间之内受到高剂量辐射所导致的疾病称为急性辐射综合症(Acute Radiation Syndrome,ARS)。其多发于核辐射事故和较高辐射剂量的放射治疗,可造成神经和血管系统、胃肠道系统和造血系统等损伤。 本文通过引入邻二酚羟基基团设计合成了一种新型氮氧自由基化合物,并通过细胞辐射损伤保护实验,评价了其对不同剂量辐射损伤和不同给药时机下人胚肝细胞(L-02)和人肝癌细胞(HepG-2)的辐射损伤保护作用。 实验结果显示,该化合物对两类细胞不同剂量辐射均有较好的辐射损伤保护作用,对4和2 Gy中等和低剂量细胞辐射损伤保护具有更好的效果,照射组的细胞存活率比单照组提高10%~18%。 而且所设计的咪唑类氮氧自由基照射前给药(细胞存活率提高9%~20%)的辐射损伤防护作用优于辐射后给药(细胞存活率提高1%~6%),为其进一步的具体应用提供了实验支持,为研究新型辐射防护药物奠基了一定的基础。

关键词: 氮氧自由基, 辐射损伤防护, 辐射防护药物

Abstract: The disease caused by human being exposed to high dose radiation in a short period of time is called acute radiation syndrome (ARS). It mostly occurs in nuclear radiation accidents and radiotherapy by high dose radiation, which can cause damage to the nerve and vascular system, gastrointestinal system, and hematopoietic system. In this paper, a new type of titronyl nitroxide radicals was designed and synthesized by introducing o-diphenol hydroxyl group. Through the cell radiation damage protection experiment, the effect of different doses of radiation damage and radiation damage protection in human embryonic liver cells (L-02) and human liver cancer cells (HepG-2) was studied. The experimental results show that the compound has a better radiation damage protection effect on the two types of cells with different doses of radiation, and has a better effect on 4 and 2 Gy medium and low dose cell radiation damage. The cell survival rate of the irradiated group is better than that of the single shot(increased by 10%~18%). Moreover, administration of the designed titronyl nitroxide radicals before irradiation (the cell survival rate is increased by 9%~20%) is better than post-radiation administration (the cell survival rate is increased by 1% to 6%), which provides experimental support for the research of new radiation protection drugs.

Key words: Titronyl nitroxide radicals, Radiation damage protection, Radiation protection drugs

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