| 聚乙二醇氨基酸衍生物的合成及其对紫杉醇的修饰 |
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| 引用本文： | 田 浤,金宇灏,陈阳建,高向东,姚文兵.聚乙二醇氨基酸衍生物的合成及其对紫杉醇的修饰[J].中国药科大学学报,2011,42(1):78-82. |
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| 作者姓名： | 田 浤 金宇灏 陈阳建 高向东 姚文兵 |
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| 作者单位： | 中国药科大学生命科学与技术学院; |
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| 基金项目： | 国家自然科学基金资助项目(No.30772679); 国家高技术研究发展计划(“八六三”计划)资助项目(No.2007AA02Z101)~~ |
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| 摘 要： | 为获得可溶性聚乙二醇(PEG)化紫杉醇,制备了不同相对分子质量的PEG氨基酸衍生物,并通过氨基酸连接臂将PEG连接到紫杉醇上,获得了具有特殊连接臂的PEG化紫杉醇。PEG化紫杉醇水溶性较天然紫杉醇提高了约1000倍,且对MCF-7和SGC-7901等肿瘤细胞都具有显著抑制作用,并呈现出明显的浓度依赖性。研究结果显示:PEG氨基酸衍生物对紫杉醇的化学修饰能够显著提高紫杉醇的水溶性,并保留其体外抗肿瘤活性,此类PEG氨基酸衍生物可以用于设计具有特殊连接臂的紫杉醇前药。
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| 关 键 词： | 紫杉醇 PEG化 聚乙二醇氨基酸衍生物 抗肿瘤活性 |
Modification of Taxol with amino acids derivatives of polyethylene glycol |
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| TIAN Hong,JIN Yu-hao,CHEN Yang-jian,GAO Xiang-dong and YAO Wen-bing.Modification of Taxol with amino acids derivatives of polyethylene glycol[J].Journal of China Pharmaceutical University,2011,42(1):78-82. |
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| Authors: | TIAN Hong JIN Yu-hao CHEN Yang-jian GAO Xiang-dong and YAO Wen-bing |
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| Institution: | TIAN Hong,JIN Yu-hao,CHEN Yang-jian,GAO Xiang-dong,YAO Wen-bing School of Life Science and Technology,China Pharmaceutical University,Nanjing 210009,China |
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| Abstract: | Water-soluble Taxol prodrugs were prepared by attaching Taxol to PEG chain with different molecular weight through different amino acid spacers.The water-solubility of PEGylated Taxol increased more than 1 000 times compared with Taxol.In vitro antitumor test of PEGylated Taxol against MCF-7 and SGC-7901 cell lines showed good antitumor activity in a concentration-dependent manner.The water-solubility of Taxol was improved significantly by modification with amino acid derivatives of polyethylene glycol whil... |
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| Keywords: | Taxol PEGylation amino acid derivatives of polyethylene glycol antitumor activity |
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