期刊
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
卷 514, 期 2, 页码 497-502出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bbrc.2019.04.153
关键词
Antibacterial activity; Bactenecin analog; D-enantiomeric lipopeptide; Fatty acid conjugation
资金
- Basic Science Research Program through the National Research Foundation of Korea - Ministry of Education [NRF-2015M3A9E7029172, NRF-2017R1D1A1B03033063]
- GIST Research Institute (GRI) - GIST
Cationic antimicrobial peptides (CAMPs) are important antibiotics because they possess a broad spectrum of activity against both Gram-positive and Gram-negative bacteria, including those resistant to traditional antibiotics. The cyclic peptide bactenecin is a 12-amino acid CAMP that contains one intramolecular disulfide bond. To improve the antibacterial activity of bactenecin, we designed and synthesized several bactenecin analogs by applying multiple approaches, including amino acid substitution, use of the D-enantiomeric form, and lipidation. Among the synthetic analogs, D-enantiomeric bactenecin conjugated to capric acid, which we named dBacK-(cap), exhibited a significantly enhanced antibacterial spectrum with MIC values ranging from 1 to 8 mu M against both Gram-positive and Gram-negative bacteria, including some drug-resistant bacteria. Upon exposure to dBacK-(cap), S. aureus cells were killed within 1 hat the MIC value, but full inactivation of E. coli required over 2 h. These results indicate that covalent addition of a D-amino acid and a fatty acid to bactenecin is the most effective approach for enhancing its antibacterial activity. (C) 2019 Elsevier Inc. All rights reserved.
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