| 甲氨蝶呤-聚乙二醇偶联物的合成及其体外抗肿瘤活性 |
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| 引用本文： | 张剑锋,魏东芝,周雄,江峰. 甲氨蝶呤-聚乙二醇偶联物的合成及其体外抗肿瘤活性[J]. 药学学报, 2007, 42(6): 607-610 |
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| 作者姓名： | 张剑锋 魏东芝 周雄 江峰 |
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| 作者单位： | 1. 新型功能材料及其制备科学国家重点实验室培育基地,宁波大学,材料科学与化学工程学院,浙江,宁波,315211
2. 生物反应器工程国家重点实验室,华东理工大学,生物化学研究所,上海,200237 |
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| 基金项目： | 浙江省宁波市青年科学基金;浙江省高等学校青年教师资助计划;浙江省教育厅资助项目 |
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| 摘 要： | 为了改善甲氨蝶呤的溶解性能和生物学性能，本工作在合成甲氨蝶呤-聚乙二醇偶联物的基础上，考察了该偶联物的溶解性和体外抗肿瘤活性。通过采用微波催化与化学催化相结合的方法，制备了新型甲氨蝶呤-聚乙二醇偶联物，其结构得到了紫外、红外和核磁共振谱的确证。测定了偶联物在水中的溶解度及其在辛醇/水中的分配系数，测得偶联物的水溶性和脂溶性均有明显增加，在纯水中的溶解度提高了128倍，分配系数提高了近5倍。以小鼠L1210白血病细胞作为研究对象，测定该偶联物的体外抗肿瘤活性，结果表明，偶联物的抗肿瘤活性与甲氨蝶呤基本接近。与文献相比，该甲氨蝶呤的聚乙二醇修饰方法具有快捷、方便的特点。
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| 关 键 词： | 甲氨蝶呤 聚乙二醇 偶联物 抗肿瘤活性 |
| 文章编号： | 0513-4870（2007）06-0607-04 |
| 收稿时间： | 2006-09-13 |
| 修稿时间： | 2006-09-13 |
Synthesis of methotrexate-poly(ethylene glycol) conjugate and their anti-tumor activity In vitro |
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| ZHANG Jian-feng,WEI Dong-zhi,ZHOU Xiong,JIANG Feng. Synthesis of methotrexate-poly(ethylene glycol) conjugate and their anti-tumor activity In vitro[J]. Acta pharmaceutica Sinica, 2007, 42(6): 607-610 |
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| Authors: | ZHANG Jian-feng WEI Dong-zhi ZHOU Xiong JIANG Feng |
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| Affiliation: | 1. State Key Laboratory Base of Novel Functional Materials and Preparation Science, Faculty of Materials Science and Chemical Engineering, Ningbo University, Ningbo 315211, China ; 2. State Key Laboratory of Bioreactor Engineering, Research Institute of Biochemistry, East China University of Science and Technology, Shanghai 200237, China |
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| Abstract: | To improve the physical property and bioactivity of methotrexate,this paper investigated the new formation of conjugate methotrexate-poly(ethylene glycol) and in vitro anti-tumor activity of the synthesized conjugate.The conjugate of methotrexate-poly(ethylene glycol),which was verified by the spectroscopy analysis of UV,IR and ~(13)C NMR,was synthesized by chemical catalysis and micro-wave irritation.The determination for the conjugate of solubility in water and distribution coefficient in octanol-water system of the conjugate was done to examine its deliquescence property.The solubility in water and the distribution coefficient of the conjugate was greatly improved,which was increased by 128 folds and 5 folds,respectively.The in vitro anti-tumor activity of the conjugate was tested by mouse L_(1210) leukaemia cells,and the synthesized conjugate showed the same anti-tumor activity as the original methotrexate.Compared to the reported literature,the modification of methotrexate by poly(ethylene glycol) is more rapid and convenient. |
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| Keywords: | methotrexate poly(ethylene glycol) conjugate in vitro anti-tumor activity |
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