In Vitro Antimicrobial Effects and Inactivation Mechanisms of 5,8-Dihydroxy-1,4-Napthoquinone
Naphthoquinones are an important class of natural organic compounds that have antimicrobial effects. However, the mechanisms of their action remain to be elucidated. Therefore, the antimicrobial activity of the chemically synthesized naphthoquinone derivative, 5,8-dihydroxy-1,4-naphthoquinone, was i...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-11-01
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| Series: | Antibiotics |
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| Online Access: | https://www.mdpi.com/2079-6382/11/11/1537 |
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| author | Seray Topçu Mine Gül Şeker |
| author_facet | Seray Topçu Mine Gül Şeker |
| author_sort | Seray Topçu |
| collection | DOAJ |
| description | Naphthoquinones are an important class of natural organic compounds that have antimicrobial effects. However, the mechanisms of their action remain to be elucidated. Therefore, the antimicrobial activity of the chemically synthesized naphthoquinone derivative, 5,8-dihydroxy-1,4-naphthoquinone, was investigated in this study against 10 different microorganisms. Its inhibitory activity was evident against <i>Bacillus cereus</i>, <i>Proteus vulgaris</i>, <i>Salmonella enteritidis</i>, <i>Staphylococcus epidermidis</i>, <i>S. aureus</i>, and <i>Candida albicans</i>, and its MIC<sub>50</sub> values were determined to be 14, 10, 6, 2, 4, 1.2, and <0.6 µg/mL, respectively. Moreover, the crystal violet uptake, TTC dehydrogenase activity, protein/DNA leakage, and DNA damage of the compound in these microorganisms were also investigated to reveal the antimicrobial mechanisms. In addition, scanning electron microscopy was used to detect physiological damage to the cell membrane of <i>S. epidermidis</i>, <i>S. aureus</i>, and <i>C. albicans</i>, which was most severe in the crystal violet uptake assay. The overall results showed that 5,8-dihydroxy-1,4-naphthoquinone exhibited its effects on <i>S. aureus</i>, <i>S. epidermidis</i>, and <i>C. albicans</i> by various mechanisms, especially membrane damage and membrane integrity disruption. It also caused DNA leakage and damage along with respiratory chain disruption (78%) in <i>C. albicans</i>. Similarly, it caused varying degrees of reduction in the respiratory activity of <i>S. aureus</i> (47%), <i>S. epidermidis</i> (16%), <i>B. cereus</i> (12%), <i>S. enteritidis</i> (9%), and <i>P. vulgaris</i> (8%). Therefore, 5,8-dihydroxy-1,4-naphthoquinone proved to be a very effective antifungal and antibacterial agent and could be considered a new potential drug candidate, inspiring further discoveries in these microorganisms. |
| first_indexed | 2024-03-09T19:19:54Z |
| format | Article |
| id | doaj.art-4086500649674f7b97a0f24a4e3c4233 |
| institution | Directory Open Access Journal |
| issn | 2079-6382 |
| language | English |
| last_indexed | 2024-03-09T19:19:54Z |
| publishDate | 2022-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Antibiotics |
| spelling | doaj.art-4086500649674f7b97a0f24a4e3c42332023-11-24T03:28:01ZengMDPI AGAntibiotics2079-63822022-11-011111153710.3390/antibiotics11111537In Vitro Antimicrobial Effects and Inactivation Mechanisms of 5,8-Dihydroxy-1,4-NapthoquinoneSeray Topçu0Mine Gül Şeker1Department of Molecular Biology and Genetics, Gebze Technical University, Gebze 41 400, Kocaeli, TürkiyeDepartment of Molecular Biology and Genetics, Gebze Technical University, Gebze 41 400, Kocaeli, TürkiyeNaphthoquinones are an important class of natural organic compounds that have antimicrobial effects. However, the mechanisms of their action remain to be elucidated. Therefore, the antimicrobial activity of the chemically synthesized naphthoquinone derivative, 5,8-dihydroxy-1,4-naphthoquinone, was investigated in this study against 10 different microorganisms. Its inhibitory activity was evident against <i>Bacillus cereus</i>, <i>Proteus vulgaris</i>, <i>Salmonella enteritidis</i>, <i>Staphylococcus epidermidis</i>, <i>S. aureus</i>, and <i>Candida albicans</i>, and its MIC<sub>50</sub> values were determined to be 14, 10, 6, 2, 4, 1.2, and <0.6 µg/mL, respectively. Moreover, the crystal violet uptake, TTC dehydrogenase activity, protein/DNA leakage, and DNA damage of the compound in these microorganisms were also investigated to reveal the antimicrobial mechanisms. In addition, scanning electron microscopy was used to detect physiological damage to the cell membrane of <i>S. epidermidis</i>, <i>S. aureus</i>, and <i>C. albicans</i>, which was most severe in the crystal violet uptake assay. The overall results showed that 5,8-dihydroxy-1,4-naphthoquinone exhibited its effects on <i>S. aureus</i>, <i>S. epidermidis</i>, and <i>C. albicans</i> by various mechanisms, especially membrane damage and membrane integrity disruption. It also caused DNA leakage and damage along with respiratory chain disruption (78%) in <i>C. albicans</i>. Similarly, it caused varying degrees of reduction in the respiratory activity of <i>S. aureus</i> (47%), <i>S. epidermidis</i> (16%), <i>B. cereus</i> (12%), <i>S. enteritidis</i> (9%), and <i>P. vulgaris</i> (8%). Therefore, 5,8-dihydroxy-1,4-naphthoquinone proved to be a very effective antifungal and antibacterial agent and could be considered a new potential drug candidate, inspiring further discoveries in these microorganisms.https://www.mdpi.com/2079-6382/11/11/1537antimicrobial effectsMIC<sub>50</sub>5,8-dihydroxy-1,4-naphthoquinoneinactivation mechanisms |
| spellingShingle | Seray Topçu Mine Gül Şeker In Vitro Antimicrobial Effects and Inactivation Mechanisms of 5,8-Dihydroxy-1,4-Napthoquinone Antibiotics antimicrobial effects MIC<sub>50</sub> 5,8-dihydroxy-1,4-naphthoquinone inactivation mechanisms |
| title | In Vitro Antimicrobial Effects and Inactivation Mechanisms of 5,8-Dihydroxy-1,4-Napthoquinone |
| title_full | In Vitro Antimicrobial Effects and Inactivation Mechanisms of 5,8-Dihydroxy-1,4-Napthoquinone |
| title_fullStr | In Vitro Antimicrobial Effects and Inactivation Mechanisms of 5,8-Dihydroxy-1,4-Napthoquinone |
| title_full_unstemmed | In Vitro Antimicrobial Effects and Inactivation Mechanisms of 5,8-Dihydroxy-1,4-Napthoquinone |
| title_short | In Vitro Antimicrobial Effects and Inactivation Mechanisms of 5,8-Dihydroxy-1,4-Napthoquinone |
| title_sort | in vitro antimicrobial effects and inactivation mechanisms of 5 8 dihydroxy 1 4 napthoquinone |
| topic | antimicrobial effects MIC<sub>50</sub> 5,8-dihydroxy-1,4-naphthoquinone inactivation mechanisms |
| url | https://www.mdpi.com/2079-6382/11/11/1537 |
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