Interaction of alpha-helical peptides with phospholipid membrane: effects of chain length and hydrophobicity of peptides.
To investigate the interaction of amphiphilic alpha-helical peptides with phospholipid membranes, we synthesized Ac-(Leu-Ala-Arg-Leu)3-NHCH3 (4[3]) and three derivatives, in which the chain length and the size of the hydrophobic region of the peptides were different from each other. These peptides formed an alpha-helical structure in the presence of vesicles. In the membrane-perturbation measurement, only 43 showed a strong membrane-perturbation activity below phase-transition temperature (25 degrees C), but above phase-transition temperature (50 degrees C), most peptides showed similar strong activities. On the other hand, in membrane-fusion measurement the long peptides, e.g., Ac-(Leu-Ala-Arg-Leu)3-(Leu-Arg-Ala-Leu)3-NHCH3, had strong activities at low peptide concentrations at 25 degrees C. The present study indicated a parallel relationship did not always exist between membrane fusion and perturbation caused by peptides.
Ohmori
N
N
Department of Applied Chemistry, Faculty of Engineering, Nagasaki University, Japan.
Niidome
T
T
Hatakeyama
T
T
Mihara
H
H
Aoyagi
H
H
D015060:1,2-Dipalmitoylphosphatidylcholine; D000595:Amino Acid Sequence; D001412:Bacillus subtilis / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002942:Circular Dichroism; D004926:Escherichia coli / Q000187:drug effects; D006461:Hemolysis; D008081:Liposomes / Q000378:metabolism*; D008561:Membrane Fusion; D010455:Peptides / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D010715:Phosphatidylglycerols; D010743:Phospholipids / Q000378:metabolism*; D017433:Protein Structure, Secondary; D011514:Proteus vulgaris / Q000187:drug effects; D013050:Spectrometry, Fluorescence; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
D008081:Liposomes; D010455:Peptides; D010715:Phosphatidylglycerols; D010743:Phospholipids; D015060:1,2-Dipalmitoylphosphatidylcholine; C030345:1,2-dipalmitoylphosphatidylglycerol