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J Antibiot (Tokyo). 2014 May;67(5):373-7. doi: 10.1038/ja.2014.9. Epub 2014 Feb 12.

Potent and selective inhibitors of class A β-lactamase: 7-prenyloxy coumarins.

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  • 1Department of Laboratory Sciences, School of Paramedical Sciences, Mashhad University of Medical Sciences, Mashhad, Iran.
  • 2Student Research Committee, Department of Laboratory Sciences, School of Paramedical Sciences, Mashhad University of Medical Sciences, Mashhad, Iran.
  • 3Antimicrobial Resistance Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
  • 4Biotechnology Research Center, Department of Pharmacognosy, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
  • 51] Department of Laboratory Sciences, School of Paramedical Sciences, Mashhad University of Medical Sciences, Mashhad, Iran [2] Antimicrobial Resistance Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.

Abstract

Class A and D β-lactamases are the main causes of resistance against β-lactam antibiotics, especially the penam group, in Staphylococcus aureus. On the basis of the potentiator property of ethanolic extracts of Ferula szowitsiana root on penicillin, MIC values observed for resistant S. aureus, the main naturally occurring compounds in these extracts, auraptene, umbelliprenin and galbanic acid, were evaluated for β-lactamase inhibitory activity. Amongst them auraptene showed the most potent inhibitory activity (IC50=21±1.5 μM) toward class A β-lactamase, whereas no inhibition was observed for class D β-lactamase. To obtain the structure activity relationship of the mentioned compounds and rationalize the enzyme inhibitory results, docking analysis was performed for both groups of β-lactamases. Docking analysis showed that the compounds have 100-500-fold lower bonding affinity toward the class D β-lactamase than toward the class A enzyme.

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