Nα - B1，Nε - B29 - 双（叔丁氧羰基）胰岛素的制备与应用

Preparation and application of Nalpha-B1,Nepsilon-B29-bis (ter.-butyloxycarbonyl)insulin.

作者信息

Friesen H J, Naithani V K, Gattner H G

出版信息

Hoppe Seylers Z Physiol Chem. 1978 Jan;359(1):103-11.

Abstract

Two methods are described for the preparation of NalphaB1,Nepsilon29-Boc2-insulin from Nalpha A1-trifluoroacetyl-insulin and Nalpha A1-citraconyl-insulin in 80 - 90% and 65% yields, respectively. Removal of the Boc protections afforded the fully active insulin. Application of this derivative was demonstrated by the preparations of des-GlyA1-insulin and [A1-guanidinoacetyl]insulin. The former compount exhibited 2% activity in the in vitro free fat cell assay and the latter 88 +/- 5% while NalphaB1-NepsilonB29-Boc2-insulin showed 45 +/- 3% activity only.

摘要

描述了两种从NαA1 - 三氟乙酰胰岛素和NαA1 - 柠康酰胰岛素分别以80 - 90%和65%的产率制备NαB1,Nε29 - Boc2 - 胰岛素的方法。去除Boc保护基得到了完全活性的胰岛素。通过制备去甘氨酸A1 - 胰岛素和[A1 - 胍基乙酰基]胰岛素证明了该衍生物的应用。前一种化合物在体外游离脂肪细胞测定中表现出2%的活性，后一种为88±5%，而NαB1 - NεB29 - Boc2 - 胰岛素仅显示45±3%的活性。