Antimicrobial Quantitative Relationship and Mechanism of Plant Flavonoids to Gram-Positive Bacteria.
Antimicrobial Quantitative Relationship and Mechanism of Plant Flavonoids to Gram-Positive Bacteria.
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DOI：
10.3390/ph15101190
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发表时间：
2022-09-27
期刊：
影响因子：
--
通讯作者：
Cao S
中科院分区：
文献类型：
--
作者：
Yuan G;Xia X;Guan Y;Yi H;Lai S;Sun Y;Cao S
抗菌药物耐药性（AMR）对人类健康构成严重威胁，迫切需要新的抗菌药物。植物黄酮类化合物因其抗菌活性、增强抗菌剂的抗菌活性、逆转抗生素耐药性而日益受到人们的关注。为了得到更科学可靠的回归方程，在文献报道的基础上，再次建立了最低抑菌浓度（MIC）（y）与亲脂性参数ACD/LogP或LogD 7.40（x）之间的回归方程。利用统计学方法，在4个回归方程中，最佳回归方程为y = −0.1285 x6 + 0.7944 x5 + 51.785 x4 − 947.64 x3 + 6638.7 x2 − 21，273 x +26，087;这里，x是LogP值。根据该方程可以计算出大多数植物黄酮类化合物对革兰氏阳性菌的MIC值，预测其最小MIC值约为0.9644 μM，可能在0.24 ~ 0.96 μM之间。这一更为可靠的方程进一步证明了亲脂性是植物黄酮类化合物抗革兰氏阳性菌的关键因素，这一点也被随后提供的更为直观的证据所进一步证实。在我们前期工作提出的抗菌机理的基础上，进一步证实了植物黄酮类化合物的抗菌机理：细胞膜是植物黄酮类化合物作用于革兰氏阳性菌的主要部位，这涉及到磷脂双分子层的破坏。这将极大地促进具有显著抑菌活性的植物黄酮类化合物的发现和应用，以及其抑菌机理的深入研究。
Antimicrobial resistance (AMR) poses a serious threat to human health, and new antimicrobial agents are desperately needed. Plant flavonoids are increasingly being paid attention to for their antibacterial activities, for the enhancing of the antibacterial activity of antimicrobials, and for the reversing of AMR. To obtain more scientific and reliable equations, another two regression equations, between the minimum inhibitory concentration (MIC) (y) and the lipophilicity parameter ACD/LogP or LogD7.40 (x), were established once again, based on the reported data. Using statistical methods, the best one of the four regression equations, including the two previously reported, with regard to the antimicrobial quantitative relationship of plant flavonoids to Gram-positive bacteria, is y = −0.1285 x6 + 0.7944 x5 + 51.785 x4 − 947.64 x3 + 6638.7 x2 − 21,273 x + 26,087; here, x is the LogP value. From this equation, the MICs of most plant flavonoids to Gram-positive bacteria can be calculated, and the minimum MIC was predicted as approximately 0.9644 μM and was probably from 0.24 to 0.96 μM. This more reliable equation further proved that the lipophilicity is a key factor of plant flavonoids against Gram-positive bacteria; this was further confirmed by the more intuitive evidence subsequently provided. Based on the antibacterial mechanism proposed in our previous work, these also confirmed the antibacterial mechanism: the cell membrane is the major site of plant flavonoids acting on the Gram-positive bacteria, and this involves the damage of the phospholipid bilayers. The above will greatly accelerate the discovery and application of plant flavonoids with remarkable antibacterial activity and the thorough research on their antimicrobial mechanism.
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DOI：
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发表时间：
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期刊：
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