| 第 50 卷第 2 期 |  | Vol. 50 No. 2 | | 2020 年 4 月 | Apr 2020 |
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所属栏目：医药及中间体
线粒体靶向白杨素的设计、合成与抗缺氧活性研究 |
| 杨立超1，2，邵 瑾2，赵 彤2，马慧萍2，景临林1，2*
（1. 联勤保障部队第九四〇医院卫勤训练中心，甘肃 兰州 730000；2. 联勤保障部队第九四〇医院药剂科，甘肃 兰州 730050） |
| 摘 要：为了提高天然产物白杨素的生物活性，以长链烷基为桥联基，通过2步反应将白杨素与线粒体靶向配体三苯基膦偶联得到了3个线粒体靶向白杨素衍生物。目标化合物分子结构经红外光谱（IR）、核磁共振谱（1H NMR和13C NMR）和质谱（MS）分析确证。常压密闭缺氧实验结果表明：3个衍生物均能延长缺氧小鼠的存活时间，且活性显著优于白杨素。 |
| 关键词：白杨素；三苯基膦；线粒体靶向；缺氧 |
| 中图分类号：R914.5 文献标识码：A 文章编号：1009-9212（2020）02-0026-04 |
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| Design, Synthesis and Anti-hypoxia Activity of Mitochondria-targeted Chrysin Derivatives |
| YANG Li-chao1,2, SHAO Jin2, ZHAO Tong2, MA Hui-ping2, JING Lin-lin1,2*
(1. Medicine Training Support Center, The 940th Hospital of Joint Logistics Support force of PLA, Lanzhou 730000, China; 2. Department of Pharmacy,The 940 th Hospital of Joint Logistics Support force of PLA, Lanzhou 730050, China) |
| Abstract：In order to enhance the bioavailability of natural chrysin, three mitochondria-targeted chrysin derivatives comprising a mitochondria-targeting moiety (triphenylphosphonium; TPP+) attached to the chrysin by different alkyl linker were designed and synthesized via a two-step process in this study. The structures were characterized by IR, 1H NMR, 13C NMR and MS, which were consistent with the target compounds. Then, the anti-hypoxia activities were accessed by normobaric hypoxia tests. The results showed that all the three derivatives could prolong the survival time of mice under hypoxia condition and the activity was better than chrysin. |
| Key words：chrysin; triphenylphosphine; mitochondria-targeted; hypoxia |
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基金项目：国家自然科学基金项目（81872796），甘肃省自然科学基金项目（18JR3RA408）。
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作者简介：杨立超（1987-），男，陕西铜川人，研究方向：高原药学研究（E-mail：563231403@qq.com）。
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联 系 人：景临林，副主任药师，研究方向：高原药学研究（E-mail：lfjinglinlin@163.com）。
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收稿日期：2020-04-15
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