Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors
Bacterial multidrug resistance is becoming a growing problem for public health, due to the development and spreading of bacterial strains resistant to antimicrobials. In this study, the antibacterial and multidrug resistance reversing activity of a series of seleno-carbonyl compounds has been evalua...
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| Format: | Article |
| Language: | English |
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MDPI AG
2019-04-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/24/8/1487 |
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| author | Tímea Mosolygó Annamária Kincses Andrea Csonka Ádám Szabó Tönki Karolina Witek Carmen Sanmartín Małgorzata Anna Marć Jadwiga Handzlik Katarzyna Kieć-Kononowicz Enrique Domínguez-Álvarez Gabriella Spengler |
| author_facet | Tímea Mosolygó Annamária Kincses Andrea Csonka Ádám Szabó Tönki Karolina Witek Carmen Sanmartín Małgorzata Anna Marć Jadwiga Handzlik Katarzyna Kieć-Kononowicz Enrique Domínguez-Álvarez Gabriella Spengler |
| author_sort | Tímea Mosolygó |
| collection | DOAJ |
| description | Bacterial multidrug resistance is becoming a growing problem for public health, due to the development and spreading of bacterial strains resistant to antimicrobials. In this study, the antibacterial and multidrug resistance reversing activity of a series of seleno-carbonyl compounds has been evaluated. The effects of eleven selenocompounds on bacterial growth were evaluated in <i>Staphylococcus aureus</i>, methicillin resistant <i>S. aureus</i> (MRSA), <i>Enterococcus faecalis, Escherichia coli</i>, and <i>Chlamydia trachomatis</i> D. The combination effect of compounds with antibiotics was examined by the minimum inhibitory concentration reduction assay. Their efflux pump (EP) inhibitory properties were assessed using real-time fluorimetry. Relative expressions of EP and quorum-sensing genes were studied by quantitative PCR. Results showed that a methylketone selenoester had remarkable antibacterial activity against Gram-positive bacteria and potentiated the activity of oxacillin in MRSA. Most of the selenocompounds showed significant anti-chlamydial effects. The selenoanhydride and the diselenodiester were active inhibitors of the AcrAB-TolC system. Based on these results it can be concluded that this group of selenocompounds can be attractive potential antibacterials and EP inhibitors. The discovery of new derivatives with a significant antibacterial activity as novel selenocompounds, is of high impact in the fight against resistant pathogens. |
| first_indexed | 2024-04-11T22:55:53Z |
| format | Article |
| id | doaj.art-e074743c03164049a19744ee87fb7f36 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-04-11T22:55:53Z |
| publishDate | 2019-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-e074743c03164049a19744ee87fb7f362022-12-22T03:58:25ZengMDPI AGMolecules1420-30492019-04-01248148710.3390/molecules24081487molecules24081487Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump InhibitorsTímea Mosolygó0Annamária Kincses1Andrea Csonka2Ádám Szabó Tönki3Karolina Witek4Carmen Sanmartín5Małgorzata Anna Marć6Jadwiga Handzlik7Katarzyna Kieć-Kononowicz8Enrique Domínguez-Álvarez9Gabriella Spengler10Department of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, 6720 Szeged, HungaryDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, 6720 Szeged, HungaryDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, 6720 Szeged, HungaryDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, 6720 Szeged, HungaryDepartment of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, PolandDepartment of Pharmaceutical Technology and Chemistry, School of Pharmacy and Nutrition, University of Navarra, Irunlarrea 1, 31008 Pamplona, SpainDepartment of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, PolandDepartment of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, PolandDepartment of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, PolandInstituto de Química Orgánica General (IQOG-CSIC), Consejo Superior de Investigaciones Científicas, Juan de la Cierva 3, 28006 Madrid, SpainDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, 6720 Szeged, HungaryBacterial multidrug resistance is becoming a growing problem for public health, due to the development and spreading of bacterial strains resistant to antimicrobials. In this study, the antibacterial and multidrug resistance reversing activity of a series of seleno-carbonyl compounds has been evaluated. The effects of eleven selenocompounds on bacterial growth were evaluated in <i>Staphylococcus aureus</i>, methicillin resistant <i>S. aureus</i> (MRSA), <i>Enterococcus faecalis, Escherichia coli</i>, and <i>Chlamydia trachomatis</i> D. The combination effect of compounds with antibiotics was examined by the minimum inhibitory concentration reduction assay. Their efflux pump (EP) inhibitory properties were assessed using real-time fluorimetry. Relative expressions of EP and quorum-sensing genes were studied by quantitative PCR. Results showed that a methylketone selenoester had remarkable antibacterial activity against Gram-positive bacteria and potentiated the activity of oxacillin in MRSA. Most of the selenocompounds showed significant anti-chlamydial effects. The selenoanhydride and the diselenodiester were active inhibitors of the AcrAB-TolC system. Based on these results it can be concluded that this group of selenocompounds can be attractive potential antibacterials and EP inhibitors. The discovery of new derivatives with a significant antibacterial activity as novel selenocompounds, is of high impact in the fight against resistant pathogens.https://www.mdpi.com/1420-3049/24/8/1487selenocompoundsselenoestersAcrAB-TolC efflux pump<i>Chlamydia trachomatis</i> D<i>Escherichia coli</i> K-12 AG100<i>Staphylococcus aureus</i> |
| spellingShingle | Tímea Mosolygó Annamária Kincses Andrea Csonka Ádám Szabó Tönki Karolina Witek Carmen Sanmartín Małgorzata Anna Marć Jadwiga Handzlik Katarzyna Kieć-Kononowicz Enrique Domínguez-Álvarez Gabriella Spengler Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors Molecules selenocompounds selenoesters AcrAB-TolC efflux pump <i>Chlamydia trachomatis</i> D <i>Escherichia coli</i> K-12 AG100 <i>Staphylococcus aureus</i> |
| title | Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors |
| title_full | Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors |
| title_fullStr | Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors |
| title_full_unstemmed | Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors |
| title_short | Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors |
| title_sort | selenocompounds as novel antibacterial agents and bacterial efflux pump inhibitors |
| topic | selenocompounds selenoesters AcrAB-TolC efflux pump <i>Chlamydia trachomatis</i> D <i>Escherichia coli</i> K-12 AG100 <i>Staphylococcus aureus</i> |
| url | https://www.mdpi.com/1420-3049/24/8/1487 |
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