Polyacylated neohesperidosides from Geranium caespitosum: bacterial multidrug resistance pump inhibitors.
Bioassay-directed fractionation for Staphylococcus aureus multidrug resistance efflux pump inhibitors resulted in isolation of novel acylated neohesperidosides from Geranium caespitosum. The more highly acylated compounds had no direct activity against S. aureus, but potentiated activity of the antibiotics berberine, rhein, ciprofloxacin and norfloxacin. Cellular concentrations of berberine were greatly increased in the presence of active esters.
Stermitz
Frank R
FR
Department of Chemistry, Colorado State University, Fort Collins, CO 80523, USA. frslab@lamar.colostate.edu
Cashman
Kevin K
KK
Halligan
Kathleen M
KM
Morel
Cécile
C
Tegos
George P
GP
Lewis
Kim
K
D000215:Acylation; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D001410:Bacillus megaterium / Q000187:drug effects / Q000254:growth & development / Q000378:metabolism; D001412:Bacillus subtilis / Q000187:drug effects / Q000254:growth & development / Q000378:metabolism; D024901:Drug Resistance, Multiple, Bacterial; D031315:Geranium / Q000737:chemistry*; D006569:Hesperidin / Q000031:analogs & derivatives* / Q000302:isolation & purification / Q000494:pharmacology*; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins / Q000037:antagonists & inhibitors*; D008826:Microbial Sensitivity Tests; D019906:Nuclear Magnetic Resonance, Biomolecular; D013211:Staphylococcus aureus / Q000187:drug effects / Q000254:growth & development / Q000378:metabolism
D000900:Anti-Bacterial Agents; D049990:Membrane Transport Modulators; D026901:Membrane Transport Proteins; D006569:Hesperidin