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前文中报导,我们曾经合成出和Sanger所提出的胰岛素B链氨基酸顺序相同的卅肽S-磺酸化衍生物,它与天然A链重组合后,能表现最高达4％的胰岛素活力。现在,我们又在合成方面作了一些改进,所得的B链S-磺酸化衍生物与天然A链进行重组合,能表现出较高的生物活力,而且此氧化粗产物经仲丁醇-醋酸抽提后,已经获得形状与天然胰岛素完全相同的结晶(图1)。重结晶产物的活力为25个国际单位/毫克(表1)。根据此结果,加上其它的一些分析数据,可以充分说明我们已经完成了胰岛素的半合成工作。
As reported previously, we have synthesized the same anthraquinone S-sulfonated derivatives of the insulin B-chain amino acid sequence proposed by Sanger that, when combined with the native A-chain, exhibits up to 4% insulin activity. Now, we made some improvements in the synthesis. The obtained S-sulfonic acid derivative of B-chain reorganized with natural A chain, which can show higher biological activity, and the oxidation of crude product by sec-butanol - acetic acid After extraction, crystals of exactly the same shape as native insulin have been obtained (Figure 1). The activity of the recrystallized product was 25 IU / mg (Table 1). Based on this result, plus some other analytical data, we can fully explain that we have completed the semi-synthesis of insulin.