| 细胞核靶向聚乙烯亚胺-地塞米松偶联物的制备及作为基因载体的应用 |
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| 引用本文： | 范颖,姚静,周建平.细胞核靶向聚乙烯亚胺-地塞米松偶联物的制备及作为基因载体的应用[J].高等学校化学学报,2011,32(12):2916-2622. |
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| 作者姓名： | 范颖 姚静 周建平 |
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| 作者单位： | 中国药科大学药学院, 南京 210009 |
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| 基金项目： | 国家重大新药创制科技重大专项，国家自然科学基金，江苏省“六大人才高峰”项目资助 |
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| 摘 要： | 采用地塞米松(Dex)和低分子量聚乙烯亚胺(PEI)经酰胺化反应, 合成了一种新型靶向基因载体PEI-Dex偶联物. 研究结果表明, PEI-Dex可结合DNA形成复合物, 在最佳制备条件下(N/P=12), PEI-Dex/DNA复合物粒径为(162±1.90) nm, 电位为(12.8±0.11) mV, 适用于基因转染. PEI-Dex的细胞毒性较低, 可促进复合物的细胞核转运, 从而显著提高转染效率.
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| 关 键 词： | 周建平 低分子量聚乙烯亚胺 地塞米松 细胞核靶向 基团传输载体 |
| 收稿时间： | 2010-12-27 |
Preparation of Nucleus-targeting Polyethyleneimine-dexamethasone Conjugates and Their Application for Gene Delivery |
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| FAN Ying,YAO Jing,ZHOU Jian-Ping.Preparation of Nucleus-targeting Polyethyleneimine-dexamethasone Conjugates and Their Application for Gene Delivery[J].Chemical Research In Chinese Universities,2011,32(12):2916-2622. |
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| Authors: | FAN Ying YAO Jing ZHOU Jian-Ping |
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| Institution: | School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China |
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| Abstract: | The study aimed to develop polyethyleneimine-dexamethasone(PEI-Dex) conjugates for the nucleus-targeting gene delivery by amidation reaction. The results showed that the PEI-Dex could effectively condense DNA and form the PEI-Dex/DNA complex. The size of the complex at the optimal N/P ratio was (162±1.90) nm and zeta potential was (12.8±0.11) mV, which could facilitate the gene transfection. Moreover, it exhibited much higher transfection efficiency compared with the PEI 1800/DNA complex due to efficient nuclear translocation and low cytotoxicity. In conclusion, PEI-Dex should be a promising non-viral gene vector. |
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| Keywords: | Low molecular weight polyethyleneimine Dexamethasone Nucleus-targeting Gene delivery |
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