文章基本信息

标题：A Practical Reagent for Reversible Amino-Protection of Insulin, 3, 4, 5, 6-Tetrahydrophthalic Anhydride
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作者：Yoshitada KIMURA ; Kiyoshi ZAITSU ; Yuji MOTOMURA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1994
卷号：17
期号：7
页码：881-885
DOI：10.1248/bpb.17.881
出版社：The Pharmaceutical Society of Japan
摘要：Of the examined dicarboxylic acid anhydrides, 3, 4, 5, 6-tetrahydrophthalic anhydride was found to be the best reagent in practical use for reversible amino-protection of insulin in terms of the rapidity of acid-deprotection. Twelve Gly (A1), Phe (B1), Lys (B29)-triacyl-insulins were prepared by reaction of porcine insulin with the dicarboxylic acid anhydrides and time courses for the deprotection of the acylated insulins with dilute acetic acid were investigated by means of capillary zone electrophoresis, and the tetrahydrophthalyl (THP)-insulin obtained with the reagent was the most rapidly deacylated (6h, 25°C, 0.1M acetic acid). Isolation of triacyl-insulins and Gly (A1)-THP-, Gly (A1), Phe (B1)-diTHP- and Gly (A1), Lys (B29)-diTHP-insulins using DEAE anion-exchange high-performance liquid chromatography is also described.
关键词：3, 4, 5, 6-tetrahydrophthalic anhydride;reversible amino-protection;insulin;dicarboxylic acid anhydride;HPLC;capillary electrophoresis