Iwahori A, Hirota Y, Sampe R, Miyano S, Numao N
Sagami Chemical Research Center, Kanagawa, Japan.
Biol Pharm Bull. 1997 Mar;20(3):267-70. doi: 10.1248/bpb.20.267.
Magainin 2 is an antimicrobial peptide found in the skin of Xenopus laevis. To find a reversed peptide comparable to the antibacterial activity of magainin 2 analogs, we have synthesized three reversed analogs, the peptide 53D, 87-ISM and A87-ISM, corresponding to the normal peptide D35, MSI-78 and MSI-78A, respectively. We examined their ability to inhibit the growth of Escherichia coli and Staphylococcus aureus. Among the analogs, the A87-ISM, that is, the reverse of MSI-78A enhanced the amphiphilicity and the alpha-helical tendency of magainin 2, showed not only almost the same antibacterial activity against the bacteria as MSI-78A, but also stronger activity than other magainin 2 analogs. In addition, at the MIC (minimum inhibitory concentration) value, A87-ISM shows no hemolysis to human red blood cells, while both MSI-78 and MSI-78A cause strong hemolysis at the MIC value. This result indicates that a novel reversed peptide comparable or superior to normal magainin 2 analogs is available.
马盖宁2是一种在非洲爪蟾皮肤中发现的抗菌肽。为了找到一种与马盖宁2类似物的抗菌活性相当的反向肽，我们合成了三种反向类似物，即肽53D、87-ISM和A87-ISM，它们分别对应于正常肽D35、MSI-78和MSI-78A。我们检测了它们抑制大肠杆菌和金黄色葡萄球菌生长的能力。在这些类似物中，A87-ISM，即MSI-78A的反向肽，增强了马盖宁2的两亲性和α-螺旋倾向，不仅对细菌表现出与MSI-78A几乎相同的抗菌活性，而且比其他马盖宁2类似物具有更强的活性。此外，在最低抑菌浓度（MIC）值时，A87-ISM对人红细胞无溶血作用，而MSI-78和MSI-78A在MIC值时均会引起强烈溶血。这一结果表明，一种与正常马盖宁2类似物相当或更优的新型反向肽是存在的。
