Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Synthesis of Reversed Magainin 2 Analogs Enhanced Antibacterial Activity
Akiyo IWAHORIYukiko HIROTARuriko SAMPESanae MIYANONaganori NUMAO
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ジャーナル フリー

1997 年 20 巻 3 号 p. 267-270

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抄録
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 α-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 inhibitoy 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.
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© The Pharmaceutical Society of Japan
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