[色氨酸3，精氨酸5] -胃饥饿素（1-5）通过生长激素促分泌素（GHS）受体刺激生长激素分泌和食物摄入。

[Trp3, Arg5]-ghrelin(1-5) stimulates growth hormone secretion and food intake via growth hormone secretagogue (GHS) receptor.

作者信息

Ohinata Kousaku, Kobayashi Kanako, Yoshikawa Masaaki

机构信息

Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University, Gokasho Uji, Kyoto 611-0011, Japan.

出版信息

Peptides. 2006 Jul;27(7):1632-7. doi: 10.1016/j.peptides.2006.01.022. Epub 2006 Mar 13.

DOI:10.1016/j.peptides.2006.01.022

PMID:16530883

Abstract

Ghrelin, a 28 amino acid peptide identified as an endogenous ligand for growth hormone secretagogue (GHS) receptor, stimulates food intake and growth hormone (GH) secretion. We designed low molecular weight peptides with affinity for the GHS receptor based on the primary structure of ghrelin. We found that [Trp3, Arg5]-ghrelin(1-5) (GSWFR), a novel pentapeptide composed of all L-amino acids, had affinity for the GHS receptor (IC50 = 10 microM). GSWFR stimulated GH secretion after intravenous or oral administration. Centrally administered GSWFR increased food intake in non-fasted mice. The orexigenic action of GSWFR was inhibited by a GHS receptor antagonist, [D-Lys3]-GH-releasing peptide-6, suggesting that GSWFR stimulated food intake through the GHS receptor. The orexigenic action of GSWFR was also inhibited by a neuropeptide Y (NPY) Y1 receptor antagonist, BIBO3304. These results suggest that the GSWFR-induced feeding is mediated by the NPY Y1 receptor.

摘要

胃饥饿素是一种由28个氨基酸组成的肽，被确定为生长激素促分泌素（GHS）受体的内源性配体，可刺激食物摄入和生长激素（GH）分泌。我们基于胃饥饿素的一级结构设计了对GHS受体具有亲和力的低分子量肽。我们发现，[色氨酸3，精氨酸5]-胃饥饿素（1-5）（GSWFR），一种由所有L-氨基酸组成的新型五肽，对GHS受体具有亲和力（IC50 = 10微摩尔）。静脉注射或口服GSWFR后可刺激GH分泌。向非禁食小鼠中枢给药GSWFR可增加食物摄入量。GSWFR的促食欲作用被GHS受体拮抗剂[D-赖氨酸3]-生长激素释放肽-6抑制，这表明GSWFR通过GHS受体刺激食物摄入。GSWFR的促食欲作用也被神经肽Y（NPY）Y1受体拮抗剂BIBO3304抑制。这些结果表明，GSWFR诱导的进食是由NPY Y1受体介导的。