Design, synthesis and antibacterial activity studies of model peptidess of proline/arginine-rich region in bactenecin7.
Bactenecin 7 (Bac7), a cationic antibacterial peptide, contains a repeating region of Xaa-Pro-Arg-Pro (Xaa = hydrophobic residue). To investigate the structure and property of a Pro/Arg-rich region, e synthesized a series of peptides, Xaa-Pro-Arg-Pro (Xaa = Gly, Arg, Leu, Ile, and Phe) as models and characterized . The conformational preferences of these peptides in water and trifluoroethanol were examined by circular dichroism. The results suggest the presence of largely poly(Pro)-II helical conformation in aqueous and trifluoroethanol solutions. Their antibacterial activity against gram-negative bacteria such as Escherichia coli, Klebsiella Pneumoniae, Pseudomonas aeruginosa, and Escherichia coliHB101, and gram-positive bacteria such as Staphylococcus aureus were measured at various peptide concentrations. Two of our synthetic tetrapeptide fragments containing Gly and Arg were efficiently killed with gram-positive bacteria, Staphylococcus aureus, at the concentration level of 200 microg/mL.
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Karnataka, India.
K
K
Abiraj
H S
HS
Prasad
A S Prakasha
AS
Gowda
D Channe
DC
Gowda
D000595:Amino Acid Sequence; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001120:Arginine / Q000737:chemistry*; D002942:Circular Dichroism; D015195:Drug Design; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D010446:Peptide Fragments / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D010456:Peptides, Cyclic / Q000737:chemistry*; D011392:Proline / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D010446:Peptide Fragments; D010456:Peptides, Cyclic; C056454:bactenecin; D001120:Arginine; D011392:Proline