Antimicrobial resistance seriously threatened human health, and new antimicrobial agents are desperately needed. As one of the largest classes of plant secondary metabolite, flavonoids can be widely found in various parts of the plant, and their antibacterial activities have been increasingly paid attention to. Based on the physicochemical parameters and antibacterial activities of sixty-six flavonoids reported, two regression equations between their ACD⁄LogP or LogD7.40 and their minimum inhibitory concentrations (MICs) to gram-positive bacteria were established with the correlation coefficients above 0.93, and then were verified by another sixty-eight flavonoids reported. From these two equations, the MICs of most flavonoids against gram-positive bacteria could be roughly calculated from their ACD⁄LogP or LogD7.40, and their minimum values were respectively predicted as approximately 1.7 or 3.0 μM, more likely fall into the range from 0.9 to 3.4 μM, or from 1.5 to 6.0 μM, respectively. Simultaneously, both tendentiously concave regression curves indicated that the lipophilicity is a key factor for flavonoids against gram-positive. Combined with the literature analyses, the results also suggested that the cell membrane is the main site of flavonoids acting on gram-positive bacteria, and which likely involves the damage of phospholipid bilayers, the inhibition of the respiratory chain or the ATP synthesis, or some others.
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No competing interests reported.
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Posted 15 Mar, 2021
Received 26 Mar, 2021
Received 26 Mar, 2021
Received 26 Mar, 2021
Received 26 Mar, 2021
On 18 Mar, 2021
On 18 Mar, 2021
On 18 Mar, 2021
On 18 Mar, 2021
On 18 Mar, 2021
Invitations sent on 17 Mar, 2021
On 17 Mar, 2021
On 04 Mar, 2021
On 04 Mar, 2021
On 01 Mar, 2021
Posted 15 Mar, 2021
Received 26 Mar, 2021
Received 26 Mar, 2021
Received 26 Mar, 2021
Received 26 Mar, 2021
On 18 Mar, 2021
On 18 Mar, 2021
On 18 Mar, 2021
On 18 Mar, 2021
On 18 Mar, 2021
Invitations sent on 17 Mar, 2021
On 17 Mar, 2021
On 04 Mar, 2021
On 04 Mar, 2021
On 01 Mar, 2021
Antimicrobial resistance seriously threatened human health, and new antimicrobial agents are desperately needed. As one of the largest classes of plant secondary metabolite, flavonoids can be widely found in various parts of the plant, and their antibacterial activities have been increasingly paid attention to. Based on the physicochemical parameters and antibacterial activities of sixty-six flavonoids reported, two regression equations between their ACD⁄LogP or LogD7.40 and their minimum inhibitory concentrations (MICs) to gram-positive bacteria were established with the correlation coefficients above 0.93, and then were verified by another sixty-eight flavonoids reported. From these two equations, the MICs of most flavonoids against gram-positive bacteria could be roughly calculated from their ACD⁄LogP or LogD7.40, and their minimum values were respectively predicted as approximately 1.7 or 3.0 μM, more likely fall into the range from 0.9 to 3.4 μM, or from 1.5 to 6.0 μM, respectively. Simultaneously, both tendentiously concave regression curves indicated that the lipophilicity is a key factor for flavonoids against gram-positive. Combined with the literature analyses, the results also suggested that the cell membrane is the main site of flavonoids acting on gram-positive bacteria, and which likely involves the damage of phospholipid bilayers, the inhibition of the respiratory chain or the ATP synthesis, or some others.
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6
Figure 7
Figure 8
Figure 9
Figure 10
Figure 11
Figure 12
Figure 13
Figure 14
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