Antibacterial Activity and Mechanisms of Plant Flavonoids against Gram-Negative Bacteria Based on the Antibacterial Statistical Model
The antimicrobial quantitative structure–activity relationship of plant flavonoids against Gram-positive bacteria was established in our previous works, and the cell membrane was confirmed as a major site of action. To investigate whether plant flavonoids have similar antibacterial effects and mecha...
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MDPI AG
2024-02-01
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| Series: | Pharmaceuticals |
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| author | Yu Yan Xuexue Xia Aiman Fatima Li Zhang Ganjun Yuan Fengxian Lian Yu Wang |
| author_facet | Yu Yan Xuexue Xia Aiman Fatima Li Zhang Ganjun Yuan Fengxian Lian Yu Wang |
| author_sort | Yu Yan |
| collection | DOAJ |
| description | The antimicrobial quantitative structure–activity relationship of plant flavonoids against Gram-positive bacteria was established in our previous works, and the cell membrane was confirmed as a major site of action. To investigate whether plant flavonoids have similar antibacterial effects and mechanisms against both Gram-negative and Gram-positive bacteria, here, the minimum inhibitory concentrations (MICs) of 37 plant flavonoids against <i>Escherichia coli</i> were determined using the microdilution broth method, and then the correlation between their lipophilic parameter ACD/LogP or LogD<sub>7.40</sub> value and their MIC was analyzed. Simultaneously, the correlation between the ACD/LogP or LogD<sub>7.40</sub> value and the MIC of 46 plant flavonoids reported in the literature against <i>E. coli</i> was also analyzed. Both sets of results showed that there is a significant correlation between the LogP value and the MIC of plant flavonoids against Gram-negative bacteria. However, it is difficult to effectively predict the MIC of plant flavonoids against Gram-negative bacteria from their lipophilic parameters. By comparing two regression curves derived from plant flavonoids against Gram-negative and Gram-positive bacteria, it was further discovered that the antibacterial activities of most plant flavonoids against Gram-negative bacteria are stronger than those against Gram-positive bacteria when their LogP values are less than approximately 3.0, but the opposite is true when their LogP values are more than approximately 3.6. Moreover, this comparison also suggests that unlike mainly acting on the cell membrane of Gram-positive bacteria, plant flavonoids have multiple mechanisms against Gram-negative species, while the cell membrane is also an important action site among them. Combined with the correlation analyses between the enzyme inhibitory activity and the LogP value of the reported flavonoids, it was further suggested that DNA gyrase is another important target of plant flavonoids against Gram-negative bacteria. |
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| spelling | doaj.art-c3f498714e3d4b48834ad6e22f1c90642024-03-27T13:59:12ZengMDPI AGPharmaceuticals1424-82472024-02-0117329210.3390/ph17030292Antibacterial Activity and Mechanisms of Plant Flavonoids against Gram-Negative Bacteria Based on the Antibacterial Statistical ModelYu Yan0Xuexue Xia1Aiman Fatima2Li Zhang3Ganjun Yuan4Fengxian Lian5Yu Wang6Biotechnological Engineering Center for Pharmaceutical Research and Development, Jiangxi Agricultural University, Nanchang 330045, ChinaBiotechnological Engineering Center for Pharmaceutical Research and Development, Jiangxi Agricultural University, Nanchang 330045, ChinaBiotechnological Engineering Center for Pharmaceutical Research and Development, Jiangxi Agricultural University, Nanchang 330045, ChinaLaboratory of Natural Medicine and Microbiological Drug, College of Bioscience and Bioengineering, Jiangxi Agricultural University, Nanchang 330045, ChinaBiotechnological Engineering Center for Pharmaceutical Research and Development, Jiangxi Agricultural University, Nanchang 330045, ChinaLaboratory of Natural Medicine and Microbiological Drug, College of Bioscience and Bioengineering, Jiangxi Agricultural University, Nanchang 330045, ChinaLaboratory of Natural Medicine and Microbiological Drug, College of Bioscience and Bioengineering, Jiangxi Agricultural University, Nanchang 330045, ChinaThe antimicrobial quantitative structure–activity relationship of plant flavonoids against Gram-positive bacteria was established in our previous works, and the cell membrane was confirmed as a major site of action. To investigate whether plant flavonoids have similar antibacterial effects and mechanisms against both Gram-negative and Gram-positive bacteria, here, the minimum inhibitory concentrations (MICs) of 37 plant flavonoids against <i>Escherichia coli</i> were determined using the microdilution broth method, and then the correlation between their lipophilic parameter ACD/LogP or LogD<sub>7.40</sub> value and their MIC was analyzed. Simultaneously, the correlation between the ACD/LogP or LogD<sub>7.40</sub> value and the MIC of 46 plant flavonoids reported in the literature against <i>E. coli</i> was also analyzed. Both sets of results showed that there is a significant correlation between the LogP value and the MIC of plant flavonoids against Gram-negative bacteria. However, it is difficult to effectively predict the MIC of plant flavonoids against Gram-negative bacteria from their lipophilic parameters. By comparing two regression curves derived from plant flavonoids against Gram-negative and Gram-positive bacteria, it was further discovered that the antibacterial activities of most plant flavonoids against Gram-negative bacteria are stronger than those against Gram-positive bacteria when their LogP values are less than approximately 3.0, but the opposite is true when their LogP values are more than approximately 3.6. Moreover, this comparison also suggests that unlike mainly acting on the cell membrane of Gram-positive bacteria, plant flavonoids have multiple mechanisms against Gram-negative species, while the cell membrane is also an important action site among them. Combined with the correlation analyses between the enzyme inhibitory activity and the LogP value of the reported flavonoids, it was further suggested that DNA gyrase is another important target of plant flavonoids against Gram-negative bacteria.https://www.mdpi.com/1424-8247/17/3/292action modeantimicrobial<i>Escherichia coli</i>flavonoidsGram-negative bacteriaGram-positive bacteria |
| spellingShingle | Yu Yan Xuexue Xia Aiman Fatima Li Zhang Ganjun Yuan Fengxian Lian Yu Wang Antibacterial Activity and Mechanisms of Plant Flavonoids against Gram-Negative Bacteria Based on the Antibacterial Statistical Model Pharmaceuticals action mode antimicrobial <i>Escherichia coli</i> flavonoids Gram-negative bacteria Gram-positive bacteria |
| title | Antibacterial Activity and Mechanisms of Plant Flavonoids against Gram-Negative Bacteria Based on the Antibacterial Statistical Model |
| title_full | Antibacterial Activity and Mechanisms of Plant Flavonoids against Gram-Negative Bacteria Based on the Antibacterial Statistical Model |
| title_fullStr | Antibacterial Activity and Mechanisms of Plant Flavonoids against Gram-Negative Bacteria Based on the Antibacterial Statistical Model |
| title_full_unstemmed | Antibacterial Activity and Mechanisms of Plant Flavonoids against Gram-Negative Bacteria Based on the Antibacterial Statistical Model |
| title_short | Antibacterial Activity and Mechanisms of Plant Flavonoids against Gram-Negative Bacteria Based on the Antibacterial Statistical Model |
| title_sort | antibacterial activity and mechanisms of plant flavonoids against gram negative bacteria based on the antibacterial statistical model |
| topic | action mode antimicrobial <i>Escherichia coli</i> flavonoids Gram-negative bacteria Gram-positive bacteria |
| url | https://www.mdpi.com/1424-8247/17/3/292 |
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