Antibacterial and anti-biofilm activities of cinchona alkaloid derivatives against Staphylococcus aureus

A1 Journal article (refereed)


Internal Authors/Editors


Publication Details

List of Authors: ME Skogman, J Kujala, I Busygin, R Leino, P Vuorela, A Fallarero
Publisher: GEORG THIEME VERLAG KG
Publication year: 2012
Journal: Planta Medica
Journal acronym: PLANTA MED
Volume number: 78
Issue number: 11
Start page: 1101
End page: 1101
Number of pages: 1
ISSN: 0032-0943
eISSN: 1439-0221


Abstract

Biofilms is the predominant bacterial lifestyle in nature and they are
resistant to commonly available antibacterials. Thus, an enormous need
exists to find new effective anti-biofilm therapy. Here a library of
cinchona alkaloids was screened for activity against Staphylococcus aureus
biofilms. Crystal violet and resazurin assays were used to measure
effects on biomass and viability, respectively. One derivative, 11-TPSCD
(structure), was found effective against planktonic bacteria and in
preventing biofilm formation (IC50 ˜ 6µM) but higher
concentrations were required to eradicate mature biofilms. An
exploration of the chemical space occupied by the active derivative (red
dot) in comparison to the cinchona alkaloid library and the
structurally related quinolone antibiotics was made using the principal
component analysis (PCA)-based model ChemGPS-NP. The results suggest
that another interesting region exists for antibacterial and
anti-biofilm activity that can be populated by quinine-type
antimicrobials, outside of the one defined by quinolone antibiotics.


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