Journal of Advanced Research ( IF 11.4 ) Pub Date : 2023-05-01 , DOI: 10.1016/j.jare.2023.04.017 Zebin Weng 1 , Fei Zeng 2 , Minxin Wang 1 , Sheng Guo 1 , Zhijuan Tang 1 , Kiyoshi Itagaki 3 , Yajuan Lin 1 , Xinchun Shen 4 , Yaqi Cao 5 , Jin-Ao Duan 1 , Fang Wang 6
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Introduction
The continuous emergence and rapid spread of multidrug-resistant bacteria have accelerated the demand for the discovery of alternative antibiotics. Natural plants contain a variety of antibacterial components, which is an important source for the discovery of antimicrobial agents.
Objective
To explore the antimicrobial activities and related mechanisms of two lavandulylated flavonoids, sophoraflavanone G and kurarinon in Sophora flavescens against methicillin-resistant Staphylococcus aureus.
Methods
The effects of sophoraflavanone G and kurarinone on methicillin-resistant Staphylococcus aureus were comprehensively investigated by a combination of proteomics and metabolomics studies. Bacterial morphology was observed by scanning electron microscopy. Membrane fluidity, membrane potential, and membrane integrity were determined using the fluorescent probes Laurdan, DiSC3(5), and propidium iodide, respectively. Adenosine triphosphate and reactive oxygen species levels were determined using the adenosine triphosphate kit and reactive oxygen species kit, respectively. The affinity activity of sophoraflavanone G to the cell membrane was determined by isothermal titration calorimetry assays.
Results
Sophoraflavanone G and kurarinone showed significant antibacterial activity and anti-multidrug resistance properties. Mechanistic studies mainly showed that they could target the bacterial membrane and cause the destruction of the membrane integrity and biosynthesis. They could inhibit cell wall synthesis, induce hydrolysis and prevent bacteria from synthesizing biofilms. In addition, they can interfere with the energy metabolism of methicillin-resistant Staphylococcus aureus and disrupt the normal physiological activities of the bacteria. In vivo studies have shown that they can significantly improve wound infection and promote wound healing.
Conclusion
Kurarinone and sophoraflavanone G showed promising antimicrobial properties against methicillin-resistant Staphylococcus aureus, suggesting that they may be potential candidates for the development of new antibiotic agents against multidrug-resistant bacteria.
中文翻译：
苦参中薰衣草苷化黄酮类化合物通过膜破坏对耐甲氧西林金黄色葡萄球菌的抗菌活性
介绍
多重耐药细菌的不断出现和快速传播加速了对替代抗生素发现的需求。天然植物含有多种抗菌成分，是发现抗菌药物的重要来源。
客观的
探讨苦参中两种薰衣草苷化黄酮苦参黄酮G和苦参酮对耐甲氧西林金黄色葡萄球菌的抗菌活性及相关机制。
方法
通过蛋白质组学和代谢组学相结合的研究，全面研究了槐黄酮 G 和苦参酮对耐甲氧西林金黄色葡萄球菌的影响。通过扫描电子显微镜观察细菌形态。分别使用荧光探针Laurdan、DiSC3(5) 和碘化丙啶测定膜流动性、膜电位和膜完整性。分别使用三磷酸腺苷试剂盒和活性氧试剂盒测定三磷酸腺苷和活性氧试剂盒。通过等温滴定量热法测定槐黄酮 G 对细胞膜的亲和活性。
结果
槐黄酮 G 和苦参酮表现出显着的抗菌活性和抗多药耐药性。机理研究主要表明它们可以靶向细菌膜并导致膜完整性和生物合成的破坏。它们可以抑制细胞壁合成、诱导水解并阻止细菌合成生物膜。此外，它们还能干扰耐甲氧西林金黄色葡萄球菌的能量代谢，扰乱细菌的正常生理活动。体内研究表明它们可以显着改善伤口感染并促进伤口愈合。
结论
苦参酮和槐黄酮 G 对耐甲氧西林金黄色葡萄球菌表现出良好的抗菌特性，这表明它们可能是开发针对多重耐药细菌的新型抗生素药物的潜在候选者。
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