In vivo biological activity of exendin (1-30)

Endocrine. 2005 Jun;27(1):1-9. doi: 10.1385/ENDO:27:1:001.

Abstract

Activation of the glucagon-like peptide-1 (GLP-1) receptor on pancreatic beta cells by GLP-1 and exendin-4 increases insulin secretion. Exendin-4 is 39 amino acids long, unlike GLP-1 which has 30 amino acids. Because of its non-mammalian (lizard) origin and unique C-terminal sequence, exendin-4 may be immunogenic in humans. We showed previously that the C terminally truncated exendin peptide exendin (1-30) has a reduced affinity for the GLP-1 receptor and a diminished ability to increase intracellular cAMP in insulinoma cells. Here we show that daily intraperitoneal injection of exendin (1-30) (1 nmol/kg) for 20 d followed by 31 d twice daily to Lepr(db)/Lepr(db) (db/db) mice significantly reduced the amount of visceral fat relative to saline-treated controls and improved HbA1C (control 9.5 +/- 0.2% vs treated 7.9 +/- 0.2%, p = 0.001) but was not as effective as exendin-4. To examine the ability of exendin (1-30) to stimulate beta-cell growth, we injected one group of 3-mo-old Fisher rats with exendin (1-30) (1 nmol/kg) and another group with saline for 8 d. We observed no change in beta-cell area, but did see a change in the number of islets with nuclei positive for BrdU [10.7 +/- 1.8% exendin (1-30) vs 6.5 +/- 0.5% control].

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adipose Tissue / drug effects
  • Amino Acid Sequence
  • Animals
  • Blood Glucose / metabolism
  • Body Composition / drug effects
  • Bromodeoxyuridine / metabolism
  • Cell Proliferation / drug effects
  • Diabetes Mellitus / blood
  • Diabetes Mellitus / genetics
  • Eating / drug effects
  • Exenatide
  • Glycated Hemoglobin / metabolism
  • Immunoenzyme Techniques
  • Injections, Intraperitoneal
  • Insulin / metabolism
  • Islets of Langerhans / drug effects
  • Magnetic Resonance Imaging
  • Mice
  • Mice, Inbred C57BL
  • Mice, Inbred Strains
  • Microscopy, Confocal
  • Molecular Sequence Data
  • Peptides / physiology*
  • Rats
  • Rats, Inbred F344
  • Venoms
  • Weight Gain / drug effects*

Substances

  • Blood Glucose
  • Glycated Hemoglobin A
  • Insulin
  • Peptides
  • Venoms
  • Exenatide
  • Bromodeoxyuridine