| 第 50 卷第 2 期 |  | Vol. 50 No. 2 | | 2020 年 4 月 | Apr 2020 |
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所屬欄目：醫藥及中間體
線(xiàn)粒體靶向白楊素的設計、合成與抗缺氧活性研究 |
| 楊立超1，2，邵 瑾2，趙 彤2，馬慧萍2，景臨林1，2*
（1. 聯(lián)勤保障部隊第九四〇醫院衛勤訓練中心，甘肅 蘭州 730000；2. 聯(lián)勤保障部隊第九四〇醫院藥劑科，甘肅 蘭州 730050） |
| 摘 要：為了提高天然產(chǎn)物白楊素的生物活性，以長(cháng)鏈烷基為橋聯(lián)基，通過(guò)2步反應將白楊素與線(xiàn)粒體靶向配體三苯基膦偶聯(lián)得到了3個(gè)線(xiàn)粒體靶向白楊素衍生物。目標化合物分子結構經(jīng)紅外光譜（IR）、核磁共振譜（1H NMR和13C NMR）和質(zhì)譜（MS）分析確證。常壓密閉缺氧實(shí)驗結果表明：3個(gè)衍生物均能延長(cháng)缺氧小鼠的存活時(shí)間，且活性顯著(zhù)優(yōu)于白楊素。 |
| 關(guān)鍵詞：白楊素；三苯基膦；線(xiàn)粒體靶向；缺氧 |
| 中圖分類(lèi)號：R914.5 文獻標識碼：A 文章編號：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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基金項目：國家自然科學(xué)基金項目（81872796），甘肅省自然科學(xué)基金項目（18JR3RA408）。
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作者簡(jiǎn)介：楊立超（1987-），男，陜西銅川人，研究方向：高原藥學(xué)研究（E-mail：563231403@qq.com）。
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聯(lián) 系 人：景臨林，副主任藥師，研究方向：高原藥學(xué)研究（E-mail：lfjinglinlin@163.com）。
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收稿日期：2020-04-15
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