Amylin(1-8) is devoid of anabolic activity in bone

Calcif Tissue Int. 2010 Mar;86(3):249-60. doi: 10.1007/s00223-010-9338-3. Epub 2010 Feb 3.

Abstract

Amylin(1-8), a cyclic peptide consisting of the eight N-terminal amino acids of the 37-amino acid peptide amylin, has been shown to induce proliferation of primary osteoblasts and to induce bone formation in healthy male mice, whereas no data on efficacy in bone disease-related models have been reported. Therefore, we evaluated any effects of amylin(1-8) in ovariectomized rats with established osteopenia, a model for postmenopausal osteoporosis. At doses up to 100 nmol/kg/day, a dose highly effective in healthy mice, amylin(1-8) was unable to increase bone mineral density in ovariectomized rats during an 8-week treatment period. Histomorphometric analysis of the tibia indicated that amylin(1-8) did not change bone histomorphometric parameters. In an attempt to verify any potential biological effects of amylin(1-8), we investigated the efficacy of this peptide in various in vitro assays. Experiments designed to confirm previously published results on the proliferative effects of amylin(1-8) on primary osteoblasts failed to show any response. Amylin(1-8) was able to partially displace (125)I-rat amylin(1-37) from amylin receptors composed of the calcitonin receptor and RAMP1, indicating specific interaction of the peptide with the amylin binding site. However, in vitro efficacy assays with amylin(1-8) in calcitonin receptor-RAMP-positive HEK293T and MCF7 cells failed to reveal any agonist activity of amylin(1-8), whereas amylin(1-37) showed the expected agonist activity. In conclusion, our results indicate that amylin(1-8) does not show agonist activity on amylin receptors, does not affect osteoblast proliferation, and is devoid of anabolic activity in bone.

MeSH terms

  • Amyloid / pharmacology*
  • Amyloid / therapeutic use
  • Anabolic Agents / pharmacology*
  • Anabolic Agents / therapeutic use
  • Animals
  • Animals, Newborn
  • Binding Sites / drug effects
  • Binding Sites / physiology
  • Bone Diseases, Metabolic / drug therapy
  • Bone Diseases, Metabolic / metabolism
  • Bone Diseases, Metabolic / physiopathology
  • Bone Regeneration / drug effects*
  • Bone Regeneration / physiology
  • Cell Line
  • Cell Line, Tumor
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Intracellular Signaling Peptides and Proteins / drug effects
  • Intracellular Signaling Peptides and Proteins / metabolism
  • Islet Amyloid Polypeptide
  • Membrane Proteins / drug effects
  • Membrane Proteins / metabolism
  • Mice
  • Osteoblasts / drug effects
  • Osteoblasts / metabolism
  • Osteogenesis / drug effects*
  • Osteogenesis / physiology
  • Ovariectomy
  • Peptide Fragments / pharmacology*
  • Peptide Fragments / therapeutic use
  • Peptides / pharmacology
  • Peptides / therapeutic use
  • Rats
  • Rats, Sprague-Dawley
  • Receptor Activity-Modifying Protein 1
  • Receptor Activity-Modifying Proteins
  • Receptors, Calcitonin / drug effects
  • Receptors, Calcitonin / metabolism

Substances

  • Amyloid
  • Anabolic Agents
  • Intracellular Signaling Peptides and Proteins
  • Islet Amyloid Polypeptide
  • Membrane Proteins
  • Peptide Fragments
  • Peptides
  • RAMP1 protein, human
  • Ramp1 protein, mouse
  • Ramp1 protein, rat
  • Receptor Activity-Modifying Protein 1
  • Receptor Activity-Modifying Proteins
  • Receptors, Calcitonin
  • amylin(1-8)