Conolysin-Mt: a conus peptide that disrupts cellular membranes

Biochemistry. 2007 Nov 6;46(44):12586-93. doi: 10.1021/bi700775p. Epub 2007 Oct 10.

Abstract

Conus venoms are estimated to comprise over 100,000 distinct pharmacologically active peptides, the majority probably targeting ion channels. Through the characterization of a cytolytic peptide from the venom of Conus mustelinus, conolysin-Mt, we expand the known conopeptide mechanisms to include association with and destruction of cellular membranes. A new 23AA conopeptide, conolysin-Mt has potent hemolytic activity when tested on human erythrocytes. At a concentration of 0.25 microM, the peptide permeabilized both negatively charged prokaryotic (PE:PG) and zwitterionic eukaryotic (PC:cholesterol) model membranes. The affinity constants (KA) of conolysin-Mt for PE:PG and PC:cholesterol model membranes were 0.9 +/- 0.3 x 10(7) and 3 +/- 1 x 10(7) M-1, respectively. In contrast, conolysin-Mt exhibited low antimicrobial activity (MIC > 50 microM) against two Escherichia coli strains, with an MIC for the Gram-positive S. aureus of 25-50 microM. The specificity of conolysin-Mt for native eukaryotic membranes is a novel feature of the peptide compared to other well-characterized cytolytic peptides such as melittin.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Cell Membrane / chemistry*
  • Cell Membrane / drug effects*
  • Conotoxins / chemistry
  • Conotoxins / pharmacology*
  • Conus Snail
  • Cytotoxins / pharmacology
  • Drug Evaluation
  • Eukaryotic Cells / chemistry
  • Eukaryotic Cells / drug effects
  • Eukaryotic Cells / ultrastructure
  • Humans
  • Melitten / chemistry
  • Mice
  • Molecular Sequence Data
  • Peptides / chemistry
  • Peptides / pharmacology
  • Prokaryotic Cells / chemistry
  • Prokaryotic Cells / drug effects
  • Prokaryotic Cells / ultrastructure
  • Sequence Homology, Amino Acid

Substances

  • Conotoxins
  • Cytotoxins
  • Peptides
  • conolysin-Mt, Conus mustelinus
  • Melitten