Polyacylated Oligosaccharides from Medicinal Mexican Morning Glory Species as Antibacterials and Inhibitors of Multidrug Resistance in Staphylococcus aureus⊥

Pereda-Miranda, Rogelio, Kaatz, Glenn W. and Gibbons, Simon (2006) Polyacylated Oligosaccharides from Medicinal Mexican Morning Glory Species as Antibacterials and Inhibitors of Multidrug Resistance in Staphylococcus aureus⊥. Journal of Natural Products, 69 (3). pp. 406-409. ISSN 0163-3864

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Abstract

Twenty-two convolvulaceous oligosaccharides selected from the tricolorin (1−7), scammonin (8, 9), and orizabin (10−22) series were evaluated for activity against a panel of Staphylococcus aureus strains possessing or lacking specific efflux pumps. The minimum inhibitory concentrations (MIC values) for most of the amphipatic compounds ranged from 4 to 32 μg/mL against XU-212 (possessing the TetK multidrug efflux pump) and SA-1199B (overexpressing the NorA multidrug efflux pump), compared with 64 and 0.25 μg/mL, respectively, for tetracycline. This activity was shown to be bactericidal. Two microbiologically inactive members of the orizabin series (10, 20) increased norfloxacin susceptibility of strain SA-1199B. At low concentrations, compound 10 was a more potent inhibitor of multidrug pump-mediated EtBr efflux than reserpine. The wide range of antimicrobial activity displayed by these compounds is an example of synergy between related components occurring in the same medicinal crude drug extract, i.e., microbiologically inactive components disabling a resistance mechanism, potentiating the antibiotic properties of the active substances. These results provide an insight into the antimicrobial potential of these complex macrocyclic lactones and open the possibility of using these compounds as starting points for the development of potent inhibitors of S. aureus multidrug efflux pumps.

Item Type: Article
Faculty \ School: Faculty of Science > School of Pharmacy
Related URLs:
Depositing User: LivePure Connector
Date Deposited: 27 Jun 2020 00:02
Last Modified: 27 Jun 2020 00:02
URI: https://ueaeprints.uea.ac.uk/id/eprint/75796
DOI: 10.1021/np050227d

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