Syntheses of low-hemolytic antimicrobial gratisin peptides |
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| Authors: | Makoto Tamaki Manabu Kokuno Ichiro Sasaki Yumiko Suzuki Michiko Iwama Kenichi Saegusa Yusuke kikuchi Mitsuno Shindo Masahiro Kimura Yoshiki Uchida |
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| Institution: | 1. Department of Chemistry, Toho University, Funabashi, Chiba 274-8510, Japan;2. Department of Food Science and Nutrition, Osaka Shoin Women’s University, Higashi-Osaka, Osaka 577-8550, Japan |
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| Abstract: | Antibiotic and hemolytic activities of gratisin (GR), cyclo(-Val1-Orn2-Leu3-d-Phe4-Pro5-d-Tyr6-)2, and fifteen GR analogues, which have various d-amino acid residues in place of d-Tyr6,6′ residues, were examined. Among them, d-Orn6,6′]-GR, d-Lys6,6′]-GR and d-Arg6,6′]-GR showed the strong activity against both Gram-positive and Gram-negative bacteria. In addition, the antibiotics showed significantly reduced toxicity against human blood cells compared with gramicidin S, cyclo(-Val1-Orn2-Leu3-d-Phe4-Pro5-)2. |
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