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Molecules 2017, 22(7), 1072; doi:10.3390/molecules22071072

Labradorins with Antibacterial Activity Produced by Pseudomonas sp.

1
Department of Molecular Sciences, Uppsala BioCenter, the Swedish University of Agricultural Sciences, P.O. Box 7015, SE-750 07 Uppsala, Sweden
2
Medivir AB, P.O. Box 1086, SE-141 22 Huddinge, Sweden
*
Author to whom correspondence should be addressed.
Received: 11 May 2017 / Revised: 11 June 2017 / Accepted: 21 June 2017 / Published: 27 June 2017
(This article belongs to the Collection Bioactive Compounds)
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Abstract

The urgent need for new antibacterial drugs has led to renewed interest in microorganisms, which historically have been the main source of previously discovered antibiotics. The present study describes the discovery of two new antibacterial oxazolylindole type alkaloids, labradorins 5 (1) and 6 (2), which were isolated and characterized from two isolates of Pseudomonas sp., along with four previously known tryptophane derived alkaloids. The structures of 1 and 2 were determined by NMR spectroscopy and MS, and confirmed by synthesis. During bioassay-guided isolation using several human bacterial pathogens, 1 and 2 displayed activity towards Staphylococcus aureus and Acinetobacter baumannii. The minimal inhibitory concentrations (MIC) of compounds 1 and 2 against S. aureus were 12 μg·mL−1 and 50 μg·mL−1, respectively, whereas the MICs against A. baumannii were >50 μg·mL−1. The CC50 values of compound 1 towards a liver cell line (HEP-G2) and a T-cell line (MT4) were 30 μg·mL−1 and 20 μg·mL−1, respectively, and for compound 2 were >100 μg·mL−1 and 20 μg·mL−1, respectively. Due to the limited potency of compounds 1 and 2, along with their toxicity, the compounds do not warrant further development towards new antibiotics. View Full-Text
Keywords: antibiotics; secondary metabolites; labradorin; oxazolylindole; antibiotic resistant bacteria; Pseudomonas; Staphylococcus aureus; Acinetobacter baumannii antibiotics; secondary metabolites; labradorin; oxazolylindole; antibiotic resistant bacteria; Pseudomonas; Staphylococcus aureus; Acinetobacter baumannii
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Broberg, A.; Bjerketorp, J.; Andersson, P.; Sahlberg, C.; Levenfors, J.J. Labradorins with Antibacterial Activity Produced by Pseudomonas sp.. Molecules 2017, 22, 1072.

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