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Table 1. MIC (µM) and hemolytic activity (50 µM) of the analoguesMRSAVISAVREVanAE. coliPs.aeruginosaC.neoformansC. albicans% HA1 ≤12.5 12.5 ≤1.25 25 25-50 50 50 192 100 100 100 100 100 100 100 53 100 100 100 100 100 100 100 14 3.12 6.25 ≤1.25 ≤1.25 3.12 25 12.5 915 100 100 25 6.25 100 50 25 26 100 100 50-100 100 100 100 50 3HA:Hemolytic activity at 50µM peptideThe most active was <strong>com</strong>pound 4, which displayed excellent activity against theGram-positive bacteria methicillin-resistant S. aureus (3.12 µM); van<strong>com</strong>ycin intermediateS. aureus (6.25µM), van<strong>com</strong>ycin resistant E. faecium VRE ( 1.25 µM ), the Gram-negativebacteria E.coli ( 1.25 µM), P. aeruginosa (3.12 µM) and the fungi amphotericin B resistantC. albicans (12.5 µM) and C. neoformans (25 µM). However, <strong>com</strong>pound 4, was alsohemolytic towards red blood cells (91%).In conclusion, the results presented here suggest that small 3-(2-naphthyl)-L-alaninecontaining peptides are promising lead structures for developing future antibacterial agents.AcknowledgementsWe thank Jette Petersen and Frank Hansen for excellent technical assistance. This work was supportedby the Danish Council for Strategic Research, the Augustinus Foundation, the Frimodt–HeinekeFoundation, the Family Hede Nielsen Foundation, the JS Foundation and the Aase & Ejnar DanielsensFoundation.References1. Kumarasamy, K., et al. Lancet Infect. Dis. 10, 597-602 (2010).2. Matzusaki, K. Biochimica et Biophysica Acta 1788, 1687-169 (2009).3. Ryge T.S., Frimodt-Møller, N., Hansen, P.R. Chemotherapy 54, 152-156 (2008).4. http://www.cmdr.ubc.ca/bobh/methods.htm5. Ryge, T.S., Hansen, P.R. J. Peptide Science 11, 727-734 (2005).379

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