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人胰岛素半合成方法的改进 被引量:3

Improvement of the Method for Semi-Synthesis of the Human Insulin
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摘要 本文对森原等人合成人胰岛素的方法进行了改进。用羧肽酶A和胰酶成功地实施了人胰岛素的半合成。精品的总收率为70%,高于1986年森原等报道的水平(50%)。 苏氨酸叔丁酯是半合成人胰岛素的主要原料之一。我们改进了它的合成方法。 Trypsin was used in catalysing the coupling between desalanine-B30-insulin(DAI) and Thr(Bu)OBu, DAI was obtained by digestion of porcine insulin with carboxypeptidase A. Thr(Bu)OBu was directly synthesized without N-terminal protection, different from general way and a high yield of human insulin was obtained. The purity of the semi-synthetic human insulin was one band of electrophoresis. It can be easily crystallized. The amino acid analysis of the semi-synthetic human insulin was identical with the theoretical value. The radiation inactivation test shows the semi-synthetic human insulin has the same insulin-binding activity with the porcine insulin.
出处 《高等学校化学学报》 SCIE EI CAS CSCD 北大核心 1989年第4期410-411,共2页 Chemical Journal of Chinese Universities
基金 国家自然科学基金
关键词 胰岛素 胰酶 半合成 羧肽酶A Insulin, Trypsin, Semi-synthesis, Carboxypeptidase A
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同被引文献13

  • 1姜文清,杨莉萍,马捷,邹定,李金娥.长效基础胰岛素类似物甘精胰岛素[J].中国新药杂志,2005,14(6):778-781. 被引量:60
  • 2何明磊,熊玉春,魏东芝.一种新型的蛋白质及多肽胍基的聚乙二醇化试剂的合成[J].药物生物技术,2005,12(4):224-226. 被引量:2
  • 3吕庆国,童南伟.胰岛素类型的研究进展[J].中国实用内科杂志,2006,26(9):1305-1308. 被引量:11
  • 4胰岛素生物测定法[M].中华人民共和国药典2005版二部附录ⅫG.
  • 5Hashimoto M, Takada K, Kiso Y, etal. Synthesis of palmitoyi derivatives of insulin and their biological activities[J].Pharmaceutical Research, 1989,6: 171.
  • 6Home P, Kurtzhals P. Insulin detemir: from concept to clinical experience[J].Expert Opin Pharmacother , 2006,7(3) 325.
  • 7Hordern SV, Wright JE, Umpleby AM, et al. Comparison of the effects on glucose and lipid metabolism of equipotent doses of insulin detemir and NPH insulin with a 16 h euglycaemic clamp[J]. Diabetologia, 2005,48 (3): 420.
  • 8何明磊.新型胰岛素衍生物及其制备方法[P].中国发明专利,200810011479.3(申请号).
  • 9胰岛素生物测定法[S].中华人民共和国药典,2005版二部附录ⅫG.
  • 10Hinds D, Sung Wan Kim. Effects of PEG conjugation on in sulin properties [J]. Advanced Drug Deliery Reviews, 2002,54(4) :505.

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