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菘蓝裂碱 D:一种具有辐射防护活性的新型 2-哌嗪酮融合 5-氮杂胞嘧啶型生物碱,来源于菘蓝的种子。

Orychophragine D:A new 2-piperazinone fused 5-azacytosine type alkaloid with radioprotective activity from the seeds of Orychophragmus violaceus.

机构信息

Beijing Institute of Radiation Medicine, Beijng 100850, China.

Beijing Institute of Radiation Medicine, Beijng 100850, China.

出版信息

Fitoterapia. 2023 Jul;168:105544. doi: 10.1016/j.fitote.2023.105544. Epub 2023 May 12.

Abstract

A new alkaloid, Orychophragine D (1), together with three known alkaloids, were isolated from the seeds of Orychophragmus violaceus. Orychophragine D represented the first example of 2-piperazinone fused 5-azacytosine skeleton. Their structures and absolute configurations were determined by spectroscopic analyses and X-ray crystallography. Compared to Ex-RAD, compound 1 exhibited a significant radioprotective activity on cell survival of irradiated HUVEC. In vivo experiments showed that 1 not only remarkably enhanced the survival of irradiated mice in 30 days, but also significantly promoted the recovery of the blood system of irradiated mice. These results suggested that 1 was valuable for further research as promising radioprotectors.

摘要

从菘蓝籽中分离得到一个新的生物碱,Orychophragmine D(1),以及三个已知的生物碱。Orychophragmine D 代表了第一个 2-哌嗪酮融合 5-氮胞嘧啶骨架的例子。通过光谱分析和 X 射线晶体学确定了它们的结构和绝对构型。与 Ex-RAD 相比,化合物 1 在照射后的 HUVEC 细胞存活率方面表现出显著的放射保护活性。体内实验表明,1 不仅显著提高了照射后小鼠 30 天的存活率,而且还显著促进了照射后小鼠血液系统的恢复。这些结果表明,1 作为有前途的放射保护剂具有进一步研究的价值。

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