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.
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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PT Shi, XK Hao, Y Chen, YH Zhang , QY Tao, . THE SOLID-PHASE SYNTHESIS OF METHOTREXATE-α-PEPTIDESJ. Acta Pharmaceutica Sinica, 1997, 32(2): 106-109.
Citation: PT Shi, XK Hao, Y Chen, YH Zhang , QY Tao, . THE SOLID-PHASE SYNTHESIS OF METHOTREXATE-α-PEPTIDESJ. Acta Pharmaceutica Sinica, 1997, 32(2): 106-109.
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氨甲喋呤-α-肽的固相合成

THE SOLID-PHASE SYNTHESIS OF METHOTREXATE-α-PEPTIDES

    摘要
  • 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。

     

    Abstract: Methotrexate(MTX) and the methotrexate-α-peptides(MTX-α-phenylalanine and MTX-α-arginine ie. MTX -α- Phe and MTX-α-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-α-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-α-Phe is a satisfactory prodrug in the treatment of cancer.

     

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