Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Antibacterial Activity of Two Alkylamines Integrated an Indane Scaffold : Mimicry of a Complementary Unit on Magainin 2
Naganori NUMAOAkiyo IWAHORIYukiko HIROTAMasanori SASATSUIsamu KONDOKenjiro ONIMURARuriko SAMPEShinji YAMANESachiko ITOHTadashi KATOHSusumu KOBAYASHI
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1997 Volume 20 Issue 7 Pages 800-804

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Abstract

Based on the antibacterial activity of 9-phenylnonylamine (pC9a) against Escherichia coli (ATCC29522) and Staphylococcus aureus (ATCC25923), we have further tested the inhibitory ability of the growth of the bacteria by (±)1-(4-aminobutyl)-6-benzylindane (PM2) and (±)1-benzyl-6-(4-aminobutyl) indane (PM3), that is, two kinds of 1, 6-disubstituted indanes. In an in vivo assay, they showed almost the same antibacterial activities against the bacteria as pC9a, as well as that of magainin 2 analogs (i.e., the peptides MSI-78 and 87-ISM), except in the case of 87-ISM against S. aureus. At the MIC (minimum inhibitory concentration) values, however, their killing rate of E.coli is actually quicker than pC9a. This indicates that an indane scaffold, used as a template to mimic a part of the α-helical structure of magainin 2, can accelerate the killing rate. At present, however, it is unknown wherther either the hydrophobicity or the α-helical structure, or both, of the indane scaffold is involved in accelerating the rate. Moreover, these two indanes also showed stronger antibacterial activity against two strains of Helicobacter pylori (ATCC43526, ATCC43579) than either pC9a or magainin 2 related peptides.

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