Molecular and cytotoxic properties of hIAPP17-29 and rIAPP17-29 fragments: a comparative study with the respective full-length parent polypeptides

Eur J Med Chem. 2014 Jun 23:81:442-55. doi: 10.1016/j.ejmech.2014.05.038. Epub 2014 May 14.

Abstract

The human islet polypeptide (hIAPP) or amylin is a 37-residue peptide hormone secreted by β-cells of the islet of Langerhans in the pancreas. Unlike the rat variant of IAPP (rIAPP), human amylin is highly amyloidogenic and is found as amyloid deposits in nearly 95% of patients afflicted with type 2 diabetes mellitus (T2DM). Human and rat IAPP have nearly identical primary sequence differing at only six positions which are encompassed within the 17-29 aminoacid region. Using Circular Dichroism (CD), Dynamic Light Scattering (DLS) and ThT-fluorescence (Th-T), we examined the aggregation properties of both full-length hIAPP1-37 and the related peptide fragment hIAPP17-29. For the sake of comparison, similar experiments were carried out on the respective rat variants rIAPP1-37 and rIAPP17-29. These studies were conducted at physiological pH in buffered solution not containing fluorinated co-solvents as well as in the presence of model membranes (LUV). In addition, the cytotoxic activity of the investigated peptides was determined toward different pancreatic β-cell lines. All the peptide studied in this work resulted cytotoxic despite β-sheet structure being observed, in vitro, for the hIAPP1-37 only. This suggests that β-sheet conformational transition that generally precedes the fibril formation, is not a prerequisite for toxicity towards β-cells. Interestingly, confocal microscopy indicated that the IAPP peptides can enter the cell and might exert their toxic action at an intracellular level.

Keywords: Amyloid; Confocal microscopy; Mitochondria; Model membranes; Spectroscopy; Type 2 diabetes.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Death / drug effects
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Islet Amyloid Polypeptide / chemistry
  • Islet Amyloid Polypeptide / pharmacology*
  • Peptide Fragments / chemistry
  • Peptide Fragments / pharmacology*
  • Protein Conformation
  • Rats
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Islet Amyloid Polypeptide
  • Peptide Fragments