Easter B R, Drewes S E
Hoppe Seylers Z Physiol Chem. 1979 Sep;360(9):1335-42. doi: 10.1515/bchm2.1979.360.2.1335.
[O-(2-Nitro-4-trimethylammoniophenyl)-TyrA 14]insulin (bovine) is a product formed on reaction of bovine insulin with the hydrophilic reagent 1-fluoro-2-nitro-4-trimethyl-ammoniobenzene iodide (TAN-F) in an aqueous buffer at pH 8.00. The derivative was isolated and its purity established by standard procedures. The identity of the derivative was determined by degrative studies with alpha-chymotrypsin. The addition of zinc to the above reaction decreases the yield of the title derivative, but increases the yield of the [N alpha-TAN-GlyA1] derivative. [N alpha-Boc-GlyA1]insulin was also reacted with the above mentioned reagent in an attempt to improve the yield of the A14-tyrosine derivative. The biological activity of this microcrystalline derivative was found to be 12.4 units/mg as measured by the mouse convulsion assay.
[O-(2-硝基-4-三甲基铵苯基)-酪氨酰A14]胰岛素（牛胰岛素）是牛胰岛素与亲水性试剂1-氟-2-硝基-4-三甲基铵苯碘化物（TAN-F）在pH 8.00的水性缓冲液中反应生成的产物。通过标准程序分离该衍生物并确定其纯度。通过用α-胰凝乳蛋白酶进行降解研究确定该衍生物的身份。向上述反应中添加锌会降低标题衍生物的产率，但会提高[Nα-TAN-甘氨酰A1]衍生物的产率。[Nα-Boc-甘氨酰A1]胰岛素也与上述试剂反应，试图提高A14-酪氨酸衍生物的产率。通过小鼠惊厥试验测定，这种微晶衍生物的生物活性为12.4单位/毫克。
