Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Polycationic Gramicidin S Analogues with Both High Antibiotic Activity and Very Low Hemolytic Activity
Makoto TamakiTakuji HaradaKenta FujinumaKazumasa TakanashiMitsuno ShindoMasahiro KimuraYoshiki Uchida
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2012 Volume 60 Issue 9 Pages 1134-1138

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Abstract

The substitution of each constituent amino acid residue of gramicidin S (GS), cyclo(-Val1,1′-Orn2,2′-Leu3,3′-D-Phe4,4′-Pro5,5′-)2 with Lys residue indicated that each side chain structure of the constituent amino acid residues affect largely the antibiotic activity and hemolytic activity of GS. Further, the substitution of D-Phe4,4′ and Pro5,5′ residues with basic amino acid residues as a Lys residue results the high antibiotic activity and the very low hemolytic activity. Thus, we have found novel positions on the scaffold of GS at D-Phe4,4′ and Pro5,5′ residues whose modification will significantly increase the therapeutic index.

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© 2012 The Pharmaceutical Society of Japan
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