In vitro antibacterial activity of dinuclear thiolato-bridged ruthenium(II)-arene compounds
ABSTRACT The antibacterial activity of 22 thiolato-bridged dinuclear ruthenium(II)-arene compounds was assessed in vitro against Escherichia coli, Streptococcus pneumoniae, and Staphylococcus aureus. None of the compounds efficiently inhibited the growth of the three E. coli strains tested, and only...
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| Format: | Article |
| Language: | English |
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American Society for Microbiology
2023-12-01
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| Series: | Microbiology Spectrum |
| Subjects: | |
| Online Access: | https://journals.asm.org/doi/10.1128/spectrum.00954-23 |
| _version_ | 1797393617791221760 |
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| author | Quentin Bugnon Camilo Melendez Oksana Desiatkina Louis Fayolles de Chaptes Isabelle Holzer Emilia Păunescu Markus Hilty Julien Furrer |
| author_facet | Quentin Bugnon Camilo Melendez Oksana Desiatkina Louis Fayolles de Chaptes Isabelle Holzer Emilia Păunescu Markus Hilty Julien Furrer |
| author_sort | Quentin Bugnon |
| collection | DOAJ |
| description | ABSTRACT The antibacterial activity of 22 thiolato-bridged dinuclear ruthenium(II)-arene compounds was assessed in vitro against Escherichia coli, Streptococcus pneumoniae, and Staphylococcus aureus. None of the compounds efficiently inhibited the growth of the three E. coli strains tested, and only compound 5 exhibited a medium activity against this bacterium [MIC (minimum inhibitory concentration) of 25 µM]. However, a significant antibacterial activity was observed against S. pneumoniae, with MIC values ranging from 1.3 to 2.6 µM for compounds 1–3, 5, and 6. Similarly, compounds 2, 5–7, and 20–22 had MIC values ranging from 2.5 to 5 µM against S. aureus. The tested diruthenium compounds have a bactericidal effect significantly faster than that of penicillin. Fluorescence microscopy assays performed on S. aureus using the BODIPY-tagged diruthenium complex 15 showed that this type of metal compound enters the bacteria and does not accumulate in the cell wall of gram-positive bacteria. Cellular internalization was further confirmed by inductively coupled plasma mass spectrometry experiments. The nature of the substituents anchored on the bridging thiols and the compounds molecular weight appears to significantly influence the antibacterial activity. Thus, if overall a decrease of the bactericidal effect with the increase of compounds’ molecular weight is observed, however, the complexes bearing larger benzo-fused lactam substituents had low MIC values. This first antibacterial activity screening demonstrated that the thiolato-diruthenium compounds exhibit promising activity against S. aureus and S. pneumoniae and deserve to be considered for further studies. IMPORTANCE The in vitro assessment of diruthenium(II)-arene compounds against Escherichia coli, Streptococcus pneumoniae, and Staphylococcus aureus showed a significant antibacterial activity of some compounds against S. pneumoniae, with minimum inhibitory concentration (MIC) values ranging from 1.3 to 2.6 µM, and a medium activity against E. coli, with MIC of 25 µM. The nature of the substituents anchored on the bridging thiols and the compounds molecular weight appear to significantly influence the antibacterial activity. Fluorescence microscopy showed that these ruthenium compounds enter the bacteria and do not accumulate in the cell wall of gram-positive bacteria. These diruthenium(II)-arene compounds exhibit promising activity against S. aureus and S. pneumoniae and deserve to be considered for further studies, especially the compounds bearing larger benzo-fused lactam substituents. |
| first_indexed | 2024-03-09T00:05:11Z |
| format | Article |
| id | doaj.art-9c1d98f75af44e11bccb57734ac7d10e |
| institution | Directory Open Access Journal |
| issn | 2165-0497 |
| language | English |
| last_indexed | 2024-03-09T00:05:11Z |
| publishDate | 2023-12-01 |
| publisher | American Society for Microbiology |
| record_format | Article |
| series | Microbiology Spectrum |
| spelling | doaj.art-9c1d98f75af44e11bccb57734ac7d10e2023-12-12T13:17:21ZengAmerican Society for MicrobiologyMicrobiology Spectrum2165-04972023-12-0111610.1128/spectrum.00954-23In vitro antibacterial activity of dinuclear thiolato-bridged ruthenium(II)-arene compoundsQuentin Bugnon0Camilo Melendez1Oksana Desiatkina2Louis Fayolles de Chaptes3Isabelle Holzer4Emilia Păunescu5Markus Hilty6Julien Furrer7Department of Medicine, Institute for Infectious Diseases, University of Bern , Bern, SwitzerlandDepartment of Chemistry, Biochemistry and Pharmaceuticals Sciences, University of Bern , Bern, SwitzerlandDepartment of Chemistry, Biochemistry and Pharmaceuticals Sciences, University of Bern , Bern, SwitzerlandDepartment of Chemistry, Biochemistry and Pharmaceuticals Sciences, University of Bern , Bern, SwitzerlandDepartment of Chemistry, Biochemistry and Pharmaceuticals Sciences, University of Bern , Bern, SwitzerlandDepartment of Chemistry, Biochemistry and Pharmaceuticals Sciences, University of Bern , Bern, SwitzerlandDepartment of Medicine, Institute for Infectious Diseases, University of Bern , Bern, SwitzerlandDepartment of Chemistry, Biochemistry and Pharmaceuticals Sciences, University of Bern , Bern, SwitzerlandABSTRACT The antibacterial activity of 22 thiolato-bridged dinuclear ruthenium(II)-arene compounds was assessed in vitro against Escherichia coli, Streptococcus pneumoniae, and Staphylococcus aureus. None of the compounds efficiently inhibited the growth of the three E. coli strains tested, and only compound 5 exhibited a medium activity against this bacterium [MIC (minimum inhibitory concentration) of 25 µM]. However, a significant antibacterial activity was observed against S. pneumoniae, with MIC values ranging from 1.3 to 2.6 µM for compounds 1–3, 5, and 6. Similarly, compounds 2, 5–7, and 20–22 had MIC values ranging from 2.5 to 5 µM against S. aureus. The tested diruthenium compounds have a bactericidal effect significantly faster than that of penicillin. Fluorescence microscopy assays performed on S. aureus using the BODIPY-tagged diruthenium complex 15 showed that this type of metal compound enters the bacteria and does not accumulate in the cell wall of gram-positive bacteria. Cellular internalization was further confirmed by inductively coupled plasma mass spectrometry experiments. The nature of the substituents anchored on the bridging thiols and the compounds molecular weight appears to significantly influence the antibacterial activity. Thus, if overall a decrease of the bactericidal effect with the increase of compounds’ molecular weight is observed, however, the complexes bearing larger benzo-fused lactam substituents had low MIC values. This first antibacterial activity screening demonstrated that the thiolato-diruthenium compounds exhibit promising activity against S. aureus and S. pneumoniae and deserve to be considered for further studies. IMPORTANCE The in vitro assessment of diruthenium(II)-arene compounds against Escherichia coli, Streptococcus pneumoniae, and Staphylococcus aureus showed a significant antibacterial activity of some compounds against S. pneumoniae, with minimum inhibitory concentration (MIC) values ranging from 1.3 to 2.6 µM, and a medium activity against E. coli, with MIC of 25 µM. The nature of the substituents anchored on the bridging thiols and the compounds molecular weight appear to significantly influence the antibacterial activity. Fluorescence microscopy showed that these ruthenium compounds enter the bacteria and do not accumulate in the cell wall of gram-positive bacteria. These diruthenium(II)-arene compounds exhibit promising activity against S. aureus and S. pneumoniae and deserve to be considered for further studies, especially the compounds bearing larger benzo-fused lactam substituents.https://journals.asm.org/doi/10.1128/spectrum.00954-23ruthenium complexesEscherichia coliStreptococcus pneumoniaeStaphylococcus aureusMICfluorescence |
| spellingShingle | Quentin Bugnon Camilo Melendez Oksana Desiatkina Louis Fayolles de Chaptes Isabelle Holzer Emilia Păunescu Markus Hilty Julien Furrer In vitro antibacterial activity of dinuclear thiolato-bridged ruthenium(II)-arene compounds Microbiology Spectrum ruthenium complexes Escherichia coli Streptococcus pneumoniae Staphylococcus aureus MIC fluorescence |
| title | In vitro antibacterial activity of dinuclear thiolato-bridged ruthenium(II)-arene compounds |
| title_full | In vitro antibacterial activity of dinuclear thiolato-bridged ruthenium(II)-arene compounds |
| title_fullStr | In vitro antibacterial activity of dinuclear thiolato-bridged ruthenium(II)-arene compounds |
| title_full_unstemmed | In vitro antibacterial activity of dinuclear thiolato-bridged ruthenium(II)-arene compounds |
| title_short | In vitro antibacterial activity of dinuclear thiolato-bridged ruthenium(II)-arene compounds |
| title_sort | in vitro antibacterial activity of dinuclear thiolato bridged ruthenium ii arene compounds |
| topic | ruthenium complexes Escherichia coli Streptococcus pneumoniae Staphylococcus aureus MIC fluorescence |
| url | https://journals.asm.org/doi/10.1128/spectrum.00954-23 |
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