一种水相反应制备胰岛素衍生物的方法

A procedure to prepare insulin derivatives based on aqueous reaction

目的建立一种简易的制备去B30及去B23-30肽胰岛素的方法。方法在转肽方法基础上,改变胰蛋白酶反应条件,在水相反应系统中,使得小C肽猪胰岛素原生成去B30及去B23-30肽胰岛素。阴离子交换层析进行产物分离,并结合HPLC纯度分析及质谱鉴定。结果胰蛋白酶催化猪胰岛素原生成去B30及去B23-30肽胰岛素。离子交换层析可以对两者进行基线分离。结论成功建立了一种制备胰岛素衍生物的方法,并对产物进行有效纯化。

[Objective] To set up a simple way to prepare Deletion Alanine and Deletion Octagopeptide Insulin. [Methods] Based on transpeptidation and changing reaction conditions, porcine insulin precursor is transformed into Deletion Alanine and Deletion Octagopeptide Insulin in aqueous solution, which are purified with anion ex- change chromatography, and identified by HPLC and MS. [Results] Porcine insulin precursor can be converted into Deletion Alanine and Deletion Oetagopeptide Insulin by tryptic hydrolysis, which are baseline separated with anion exchange chromatography. [Conclusion] A procedure to prepare insulin derivatives has been successfully established, and products were purified.