猪胃泌酸调节素C末端八肽的合成。赖氨酸-精氨酸-天冬酰胺-赖氨酸-天冬酰胺-天冬酰胺-异亮氨酸-丙氨酸：一种有效的五肽胃泌素诱导胃酸分泌抑制剂。

Synthesis of the C-terminal octapeptide of pig oxyntomodulin. Lys-Arg-Asn-Lys-Asn-Asn-Ile-Ala: a potent inhibitor of pentagastrin-induced acid secretion.

作者信息

Audousset-Puech M P, Jarrousse C, Dubrasquet M, Aumelas A, Castro B, Bataille D, Martinez J

出版信息

J Med Chem. 1985 Oct;28(10):1529-33. doi: 10.1021/jm00148a027.

Abstract

The synthesis of Lys-Arg-Asn-Lys-Asn-Asn-Ile-Ala representing the C-terminal octapeptide of oxyntomodulin isolated from pig intestine is described. Its structure was confirmed by its 360-MHz 1H NMR spectra. The octapeptide was tested for its ability to inhibit pentagastrin-induced acid secretion, in the anaesthetized rat, in the conscious rat with chronic gastric fistula, and in the conscious cat with gastric chronic fistula. The octapeptide inhibits pentagastrin-induced acid secretion in all three models. Compared to oxyntomodulin, the parent hormone, the synthetic peptide was approximately 150 times less potent but has the same efficacy. Biological data are presented and discussed.

摘要

本文描述了从猪小肠中分离出的胃泌酸调节素C末端八肽Lys-Arg-Asn-Lys-Asn-Asn-Ile-Ala的合成。通过其360-MHz 1H NMR光谱确认了其结构。在麻醉大鼠、患有慢性胃瘘的清醒大鼠以及患有慢性胃瘘的清醒猫中，测试了该八肽抑制五肽胃泌素诱导胃酸分泌的能力。该八肽在所有三种模型中均能抑制五肽胃泌素诱导的胃酸分泌。与母体激素胃泌酸调节素相比，合成肽的效力约低150倍，但具有相同的功效。文中给出并讨论了生物学数据。