Fluorinated Beta-diketo Phosphorus Ylides Are Novel Efflux Pump Inhibitors in Bacteria
BACKGROUND: One of the most important resistance mechanisms in bacteria is the increased expression of multidrug efflux pumps. To combat efflux-related resistance, the development of new efflux pump inhibitors is essential. MATERIALS AND METHODS: Ten phosphorus ylides were compared based on their MD...
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| Dokumentumtípus: | Cikk |
| Megjelent: |
2016
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| Sorozat: | IN VIVO
30 No. 6 |
| doi: | 10.21873/invivo.10999 |
| mtmt: | 3135011 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/10423 |
| LEADER | 02233nab a2200289 i 4500 | ||
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| 001 | publ10423 | ||
| 005 | 20190606155200.0 | ||
| 008 | 170202s2016 hu o 0|| zxx d | ||
| 022 | |a 0258-851X | ||
| 024 | 7 | |a 10.21873/invivo.10999 |2 doi | |
| 024 | 7 | |a 3135011 |2 mtmt | |
| 040 | |a SZTE Publicatio Repozitórium |b hun | ||
| 041 | |a zxx | ||
| 100 | 1 | |a Kincses Annamária | |
| 245 | 1 | 0 | |a Fluorinated Beta-diketo Phosphorus Ylides Are Novel Efflux Pump Inhibitors in Bacteria |h [elektronikus dokumentum] / |c Kincses Annamária |
| 260 | |c 2016 | ||
| 300 | |a 813-817 | ||
| 490 | 0 | |a IN VIVO |v 30 No. 6 | |
| 520 | 3 | |a BACKGROUND: One of the most important resistance mechanisms in bacteria is the increased expression of multidrug efflux pumps. To combat efflux-related resistance, the development of new efflux pump inhibitors is essential. MATERIALS AND METHODS: Ten phosphorus ylides were compared based on their MDR-reverting activity in multidrug efflux pump system consisting of the subunits acridine-resistance proteins A and B (AcrA and AcrB) and the multidrug efflux pump outer membrane factor TolC (TolC) of Escherichia coli K-12 AG100 strain and its AcrAB-TolC-deleted strain. Efflux inhibition was assessed by real-time fluorimetry and the inhibition of quorum sensing (QS) was also investigated. The relative gene expression of efflux QS genes was determined by real-time reverse transcriptase quantitative polymerase chain reaction. RESULTS: The most potent derivative was Ph3P=C(COC2F5)CHO and its effect was more pronounced on the AcrAB-TolC-expressing E. coli strain, furthermore the most active compounds, Ph3P=C(COCF3)OMe, Ph3P=C(COC2F5)CHO and Ph3P=C(COCF3)COMe, reduced the expression of efflux pump and QS genes. CONCLUSION: Phosphorus ylides might be valuable EPI compounds to reverse efflux related MDR in bacteria. | |
| 700 | 0 | 1 | |a Szabó Ágnes Míra |e aut |
| 700 | 0 | 1 | |a Saijo Ryosuke |e aut |
| 700 | 0 | 1 | |a Watanabe Genki |e aut |
| 700 | 0 | 1 | |a Kawase Masami |e aut |
| 700 | 0 | 1 | |a Molnár József |e aut |
| 700 | 0 | 1 | |a Spengler Gabriella |e aut |
| 856 | 4 | 0 | |u http://publicatio.bibl.u-szeged.hu/10423/1/INVIVO_30_6_813_817_u.pdf |z Dokumentum-elérés |
| 856 | 4 | 0 | |u http://publicatio.bibl.u-szeged.hu/10423/7/813.full.pdf |z Dokumentum-elérés |