STRUCTURAL REQUIREMENTS FOR THE BIOLOGICAL-ACTIVITY OF ENTEROSTATIN

被引：53

作者：

LIN, L ^{[1
]}

OKADA, S ^{[1
]}

YORK, DA ^{[1
]}

BRAY, GA ^{[1
]}

机构：

[1] PENNINGTON BIOMED RES CTR, BATON ROUGE, LA 70808 USA

来源：

PEPTIDES | 1994年 / 15卷 / 05期

关键词：

FOOD INTAKE; ENTEROSTATIN ANALOGS; DIETARY FAT; CYCLO-DIKETOPIPERAZINES; CYCLO-ASPARTYL-PROLINE; MACRONUTRIENT;

D O I：

10.1016/0196-9781(94)90041-8

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of enterostatin analogues were tested to investigate the minimal structure required for activity to suppress the intake of high-fat (HF) diets. The dose-response curve to intracerebroventricular (ICV) enterostatin was U-shaped (maximal inhibition at 1 nmol). Removal or modification of the N-terminal valine from enterostatin (Val-Pro-Asp-Pro-Arg) abolished activity, as did C-terminal amidation. The tripeptide (Pro-Asp-Pro) and the cyclo-diketopiperazine cyclo-Asp-Pro retained activity whereas the linear Asp-Pro dipeptide was inactive. In rats adapted to a three-choice macronutrient diet, cyclo-Asp-Pro specifically inhibited fat intake and had near maximal inhibition (50%) at the 0.03 nmol dose. The enterostatin inhibitory effect on fat intake may reside in the cyclo-diketopiperazine molecule, cyclo-Asp-Pro.

引用

页码：849 / 854

页数：6

共 27 条

[1] BOWYER R C, 1991, Digestion, V49, P10
[2] ERLANSONALBERTS.C, 1980, BIOCHIMIE, V70, P1245
[3] ERLANSONALBERTS.C, 1990, INT J OBES S2, V14, P162
[4] THE ACTIVATION PEPTIDE OF PANCREATIC PROCOLIPASE DECREASES FOOD-INTAKE IN RATS
ERLANSONALBERTSSON, C
LARSSON, A
[J]. REGULATORY PEPTIDES, 1988, 22 (04) : 325 - 331
[5] THE EXISTENCE OF PRO-COLIPASE IN PANCREATIC-JUICE
ERLANSONALBERTSSON, C
[J]. BIOCHIMICA ET BIOPHYSICA ACTA, 1981, 666 (02) : 299 - 300
[6] PANCREATIC PROCOLIPASE PROPEPTIDE, ENTEROSTATIN, SPECIFICALLY INHIBITS FAT INTAKE
ERLANSONALBERTSSON, C
MEI, J
OKADA, S
YORK, D
BRAY, GA
[J]. PHYSIOLOGY & BEHAVIOR, 1991, 49 (06) : 1191 - 1194
[7] HENSCHEN A, 1979, H-S Z PHYSIOL CHEM, V360, P1217
[8] KEYS A, 1970, CIRCULATION, V41, pI1
[9] THE EFFECTS OF THE TRH METABOLITE CYCLO(HIS-PRO) AND ITS ANALOGS ON FEEDING
KOW, LM
PFAFF, DW
[J]. PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 1991, 38 (02) : 359 - 364
[10] THE PEPTIDE ENTEROSTATIN MAY PRODUCE EARLY SATIETY
LIN, L
MCCLANAHAN, S
YORK, DA
BRAY, GA
[J]. PHYSIOLOGY & BEHAVIOR, 1993, 53 (04) : 789 - 794

← 1 2 3 →