A novel polycationic analogue of gratisin with antibiotic activity against both Gram-positive and Gram-negative bacteria

Makoto Tamaki; Manabu Kokuno; Yumiko Suzuki; Mitsuko Iwama; Mitsuno Shindo; Yoshiki Uchida

doi:10.1038/ja.2008.106

A novel polycationic analogue of gratisin with antibiotic activity against both Gram-positive and Gram-negative bacteria

J Antibiot (Tokyo). 2008 Jan;61(1):33-5. doi: 10.1038/ja.2008.106.

Authors

Makoto Tamaki¹, Manabu Kokuno, Yumiko Suzuki, Mitsuko Iwama, Mitsuno Shindo, Yoshiki Uchida

Affiliation

¹ Department of Chemistry, Toho University, Funabashi, Chiba, Japan. tamaki@chem.sci.toho-u.ac.jp

PMID: 18305357
DOI: 10.1038/ja.2008.106

Abstract

A novel polycationic analogue of gratisin, cyclo(-Val-Orn-Leu-D-Phe-Pro-D-Lys-)2, was designed and synthesized, which exhibited strong activity against all Gram-positive and Gram-negative bacteria tested. Its activity against Pseudomonas aeruginosa IFO 3080 was two times higher than gramicidin S.

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry*
Anti-Bacterial Agents / pharmacology*
Antimicrobial Cationic Peptides / chemical synthesis
Antimicrobial Cationic Peptides / chemistry*
Antimicrobial Cationic Peptides / pharmacology*
Circular Dichroism
Drug Design
Gram-Negative Bacteria / drug effects*
Gram-Positive Bacteria / drug effects*
Microbial Sensitivity Tests
Peptides / chemical synthesis
Peptides / chemistry*
Peptides / pharmacology*
Peptides, Cyclic / chemical synthesis
Peptides, Cyclic / chemistry*
Peptides, Cyclic / pharmacology*
Pseudomonas aeruginosa / drug effects

Substances

Anti-Bacterial Agents
Antimicrobial Cationic Peptides
Peptides
Peptides, Cyclic
cyclo(valyl-ornithyl-leucyl-phenylalanyl-prolyl-lysyl)2
gratisin