Benzoxazole-Based Metal Complexes to Reverse Multidrug Resistance in Bacteria
Bacteria often show resistance against antibiotics due to various mechanisms such as the expression of efflux pumps, biofilm formation, or bacterial quorum sensing (QS) controls. For successful therapy, the discovery of alternative agents is crucial. The objective of this study was to evaluate the e...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-09-01
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| Series: | Antibiotics |
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| Online Access: | https://www.mdpi.com/2079-6382/9/10/649 |
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| author | Annamária Kincses Stefánia Szabó Bálint Rácz Nikoletta Szemerédi Genki Watanabe Ryosuke Saijo Hiroshi Sekiya Eiji Tamai Joseph Molnár Masami Kawase Gabriella Spengler |
| author_facet | Annamária Kincses Stefánia Szabó Bálint Rácz Nikoletta Szemerédi Genki Watanabe Ryosuke Saijo Hiroshi Sekiya Eiji Tamai Joseph Molnár Masami Kawase Gabriella Spengler |
| author_sort | Annamária Kincses |
| collection | DOAJ |
| description | Bacteria often show resistance against antibiotics due to various mechanisms such as the expression of efflux pumps, biofilm formation, or bacterial quorum sensing (QS) controls. For successful therapy, the discovery of alternative agents is crucial. The objective of this study was to evaluate the efflux pump, anti-biofilm, and QS inhibiting, as well as antibacterial effects of 2-trifluoroacetonylbenzoxazole ligands (<b>1–3</b>) and their metal complexes (<b>4–12</b>) in bacteria. The ligand <b>2</b> and its Zn(II) complex <b>5</b>, and furthermore the Cu(II) complex <b>7</b> of ligand <b>1</b>, exerted remarkable antibacterial activity on the <i>Staphylococcus aureus</i> 272123 (MRSA) strain. In the minimum inhibitory concentration (MIC) reduction assay the ligand <b>3</b>, the Zn(II) complex <b>5</b> of ligand <b>2</b>, and the Cu(II), Ni(II), Mg(II), Fe(III) complexes (<b>7</b>, <b>8</b>, <b>9</b>, <b>12</b>) of ligand <b>1</b> enhanced the antibacterial activity of ciprofloxacin in MRSA. An increased ethidium bromide accumulation was detected for ligand <b>3</b> in MRSA while the Fe(III) complex <b>12</b> of ligand <b>1</b> decreased the biofilm formation of the reference <i>S. aureus</i> ATCC 25923 strain. The Zn(II) and Ag(II) complexes (<b>3</b> and <b>4</b>) of ligand <b>1</b> and ligand <b>3</b> inhibited the QS. Based on our results, the ligands and their metal complexes could be potential alternative drugs in the treatment of infectious diseases. |
| first_indexed | 2024-03-10T16:00:17Z |
| format | Article |
| id | doaj.art-e4e096c52f7847f1a8051a62c19f7b3f |
| institution | Directory Open Access Journal |
| issn | 2079-6382 |
| language | English |
| last_indexed | 2024-03-10T16:00:17Z |
| publishDate | 2020-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Antibiotics |
| spelling | doaj.art-e4e096c52f7847f1a8051a62c19f7b3f2023-11-20T15:21:17ZengMDPI AGAntibiotics2079-63822020-09-0191064910.3390/antibiotics9100649Benzoxazole-Based Metal Complexes to Reverse Multidrug Resistance in BacteriaAnnamária Kincses0Stefánia Szabó1Bálint Rácz2Nikoletta Szemerédi3Genki Watanabe4Ryosuke Saijo5Hiroshi Sekiya6Eiji Tamai7Joseph Molnár8Masami Kawase9Gabriella Spengler10Department of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, H-6720 Szeged, HungaryDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, H-6720 Szeged, HungaryDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, H-6720 Szeged, HungaryDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, H-6720 Szeged, HungaryCollege of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama 790-8578, JapanCollege of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama 790-8578, JapanDepartment of Infectious Diseases, College of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama 790-8578, JapanDepartment of Infectious Diseases, College of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama 790-8578, JapanDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, H-6720 Szeged, HungaryCollege of Pharmaceutical Sciences, Matsuyama University, 4-2 Bunkyo-cho, Matsuyama 790-8578, JapanDepartment of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Dóm tér 10, H-6720 Szeged, HungaryBacteria often show resistance against antibiotics due to various mechanisms such as the expression of efflux pumps, biofilm formation, or bacterial quorum sensing (QS) controls. For successful therapy, the discovery of alternative agents is crucial. The objective of this study was to evaluate the efflux pump, anti-biofilm, and QS inhibiting, as well as antibacterial effects of 2-trifluoroacetonylbenzoxazole ligands (<b>1–3</b>) and their metal complexes (<b>4–12</b>) in bacteria. The ligand <b>2</b> and its Zn(II) complex <b>5</b>, and furthermore the Cu(II) complex <b>7</b> of ligand <b>1</b>, exerted remarkable antibacterial activity on the <i>Staphylococcus aureus</i> 272123 (MRSA) strain. In the minimum inhibitory concentration (MIC) reduction assay the ligand <b>3</b>, the Zn(II) complex <b>5</b> of ligand <b>2</b>, and the Cu(II), Ni(II), Mg(II), Fe(III) complexes (<b>7</b>, <b>8</b>, <b>9</b>, <b>12</b>) of ligand <b>1</b> enhanced the antibacterial activity of ciprofloxacin in MRSA. An increased ethidium bromide accumulation was detected for ligand <b>3</b> in MRSA while the Fe(III) complex <b>12</b> of ligand <b>1</b> decreased the biofilm formation of the reference <i>S. aureus</i> ATCC 25923 strain. The Zn(II) and Ag(II) complexes (<b>3</b> and <b>4</b>) of ligand <b>1</b> and ligand <b>3</b> inhibited the QS. Based on our results, the ligands and their metal complexes could be potential alternative drugs in the treatment of infectious diseases.https://www.mdpi.com/2079-6382/9/10/649<i>E. coli</i><i>Staphylococcus aureus</i>multidrug resistancebenzoxazole skeletonmetal complexesefflux pump |
| spellingShingle | Annamária Kincses Stefánia Szabó Bálint Rácz Nikoletta Szemerédi Genki Watanabe Ryosuke Saijo Hiroshi Sekiya Eiji Tamai Joseph Molnár Masami Kawase Gabriella Spengler Benzoxazole-Based Metal Complexes to Reverse Multidrug Resistance in Bacteria Antibiotics <i>E. coli</i> <i>Staphylococcus aureus</i> multidrug resistance benzoxazole skeleton metal complexes efflux pump |
| title | Benzoxazole-Based Metal Complexes to Reverse Multidrug Resistance in Bacteria |
| title_full | Benzoxazole-Based Metal Complexes to Reverse Multidrug Resistance in Bacteria |
| title_fullStr | Benzoxazole-Based Metal Complexes to Reverse Multidrug Resistance in Bacteria |
| title_full_unstemmed | Benzoxazole-Based Metal Complexes to Reverse Multidrug Resistance in Bacteria |
| title_short | Benzoxazole-Based Metal Complexes to Reverse Multidrug Resistance in Bacteria |
| title_sort | benzoxazole based metal complexes to reverse multidrug resistance in bacteria |
| topic | <i>E. coli</i> <i>Staphylococcus aureus</i> multidrug resistance benzoxazole skeleton metal complexes efflux pump |
| url | https://www.mdpi.com/2079-6382/9/10/649 |
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