| 水蛭素聚乙二醇化及其体外抗凝活力分析 |
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| 引用本文： | 秦海娜,修志龙,张代佳,包永明,李晓晖,韩国柱.水蛭素聚乙二醇化及其体外抗凝活力分析[J].中国化学工程学报,2007,15(4):586-590. |
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| 作者姓名： | 秦海娜 修志龙 张代佳 包永明 李晓晖 韩国柱 |
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| 作者单位： | [1]Department of Bioscience and Biotechnology, School of Environmental and Biological Science and Technology,Dalian University of Technology, Dalian 116024, China [2]Department of Pharmacology, Dalian Medical University, Dalian 116027, China |
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| 摘 要： | Hirudin is the most anticoagulant drug found in nature, but its short serum half-life significantly inhibits its clinical anpplication. The PEGvlation of hirudin, the most promising anticoagulant drug, was performed in this paper. The optimal reaction conditions for PEG ylated hirudin were investigated, wh.en the PEGylation react, on.wasconducted under 4℃ after 10h, in the borate buffer at pH 8.5 .with the molar ratio 230 ： 1 of PEG to hirudin, a higher modification extent was achieved. Finally, the bioactivity of PEGylated hirudin was measured in vitro.Compared with unmodified hirudin, 26% of anti-thrombin activity was retained.
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| 关 键 词： | 水蛭素 聚乙二醇化蛋白质混合物 抗凝血酶活性 分析 |
| 收稿时间： | 31 August 2006 |
| 修稿时间： | 2006-08-31 |
PEGylation of hirudin and analysis of its antithrombin activity in vitro |
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| QIN Haina,XIU Zhilong,ZHANG Daijia,BAO Yongming,LI Xiaohui,HAN Guozhu.PEGylation of hirudin and analysis of its antithrombin activity in vitro[J].Chinese Journal of Chemical Engineering,2007,15(4):586-590. |
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| Authors: | QIN Haina XIU Zhilong ZHANG Daijia BAO Yongming LI Xiaohui HAN Guozhu |
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| Affiliation: | a Department of Bioscience and Biotechnology, School of Environmental and Biological Science and Technology, Dalian University of Technology, Dalian 116024, China b Department of Pharmacology, Dalian Medical University, Dalian 116027, China |
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| Abstract: | Hirudin is the most anticoagulant drug found in nature, but its short serum half-life significantly inhibits its clinical application. The PEGylation of hirudin, the most promising anticoagulant drug, was performed in this paper. The optimal reaction conditions for PEGylated hirudin were investigated. When the PEGylation reaction was conducted under 4℃ after 10h, in the borate buffer at pH 8.5, with the molar ratio 250: 1 of PEG to hirudin, a higher modification extent was achieved. Finally, the bioactivity of PEGylated hirudin was measured in vitro.Compared with unmodified hirudin, 26% of anti-thrombin activity was retained. |
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| Keywords: | PEGylated protein hirudin analysis anti-thrombin activity |
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