| 氨甲喋呤-α-肽的固相合成 |
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| 引用本文： | 施溥涛,郝晓柯,陈颖,张盈华,陶秦渝.氨甲喋呤-α-肽的固相合成[J].药学学报,1997,32(2):106-109. |
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| 作者姓名： | 施溥涛 郝晓柯 陈颖 张盈华 陶秦渝 |
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| 作者单位： | 中国科学院上海生化研究所，第四军医大学唐都医院中心实验室 |
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| 基金项目： | 国家自然科学基金,青年基金 |
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| 摘 要： | 用固相肽合成法合成了氨甲喋呤(MTX)与MTX-α-苯丙氨酸及精氨酸衍生物,产物不经进一步分离纯化即可达到HPLC单峰,质谱分析其分子量符合理论值。MTX-α-苯丙氨酸经羧肽酶-A处理后,可完全降解为MTX。体外细胞毒性试验,两者活性差异在100倍以上,提示MTX-α-苯丙氨酸是一理想的前体药物。
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| 关 键 词： | 固相合成 MTX MTX-α-苯丙氨酸 羧肽酶 细胞毒性 |
| 收稿时间： | 1996-01-16 |
The solid-phase synthesis of methotrexate-alpha-peptides] |
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| PT Shi,XK Hao,Y Chen,YH Zhang and QY Tao.The solid-phase synthesis of methotrexate-alpha-peptides][J].Acta Pharmaceutica Sinica,1997,32(2):106-109. |
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| Authors: | PT Shi XK Hao Y Chen YH Zhang and QY Tao |
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| Institution: | Shanghai Institute of Biochemistry, Chinese Academy of Sciences, Shanghai 200031. |
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| Abstract: | Methotrexate(MTX) and the methotrexate-alpha-peptides(MTX-alpha-phenylalanine and MTX-alpha-arginine i.e. MTX-alpha-Phe and MTX-alpha-Arg) were prepared with the technique of solid-phase peptide synthesis. Its purity was verified as a single peak by HPLC and its molecular weight was measured by mass spectrometry. MTX-alpha-Phe could be hydrolyzed to MTX by carboxypeptidase A. The cytotoxic effect of released MTX was found to be 100 times stronger than that of the peptide in vitro. It is suggested that MTX-alpha-Phe is a satisfactory prodrug in the treatment of cancer. |
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| Keywords: | Solid phase synthesis Methotrexate Phenylalanine Carboxypeptidase Cytotoxic Prodrug |
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