Posgrado de Botánica y Colegio de Postgraduados, Campus Montecillo, Texcoco, Estado de México, México.
Instituto de Ciencias Básicas e Ingeniería, Universidad Autónoma del Estado de Hidalgo, Mineral de la Reforma, Hidalgo, México.
J Med Food. 2021 Sep;24(9):934-943. doi: 10.1089/jmf.2020.0135. Epub 2021 Mar 22.
L. () calyxes, rich in organic acids, are included in diets in different countries. In recent years, some phytochemicals have been shown to reduce bacterial virulence at sublethal concentrations by interfering with quorum sensing (QS) systems. Therefore, in this study the antivirulence properties of calyxes and two -lactones (hibiscus acid [HA] and its methyl ester) in were analyzed. Acetone and methanol extracts of showed anti-QS activity by inhibiting violacein production (60% to 80% with 250 g/mL). In molecular docking analysis, the -lactones registered a good binding score, which suggests strong interaction with the active site of LasR protein. To verify their effect , they were isolated from and evaluated in six QS-regulated phenotypes, as well as in ExoU toxin that is released by the type III secretion system (T3SS). At 500 g/mL they reduced alkaline protease (29-52%) and elastase (15-37%) activity, biofilm formation (∼75%), and swarming (50%), but there was no effect on pyocyanin production, hemolytic activity, or type III secretion. In a mouse abscess/necrosis model, HA at sublethal concentrations (15 and 31.2 g/mL) affected infection establishment and prevented damage and systemic spread. In conclusion, HA is the first molecule identified with antivirulence properties in with the potential to prevent infections caused by .
()萼片富含有机酸,在不同国家的饮食中都有包含。近年来,一些植物化学物质已被证明可以通过干扰群体感应(QS)系统在亚致死浓度下降低细菌的毒力。因此,在这项研究中,分析了 萼片中两种内酯(芙蓉酸[HA]及其甲酯)的抗毒力特性。()萼片的丙酮和甲醇提取物通过抑制紫斑素产生表现出抗 QS 活性(用 250μg/mL 抑制 60%至 80%)。在分子对接分析中,内酯类物质的结合评分较好,这表明它们与 LasR 蛋白的活性位点有很强的相互作用。为了验证它们的效果,从 中分离出它们,并在六个 QS 调控表型以及 III 型分泌系统(T3SS)释放的 ExoU 毒素中进行评估。在 500μg/mL 时,它们降低了碱性蛋白酶(29%-52%)和弹性蛋白酶(15%-37%)活性、生物膜形成(约 75%)和群集(50%),但对吡咯菌素产生、溶血活性或 III 型分泌没有影响。在小鼠脓肿/坏死模型中,亚致死浓度(15 和 31.2μg/mL)的 HA 影响感染的建立,并防止损伤和全身扩散。总之,HA 是在 中首次被鉴定出具有抗毒力特性的分子,有可能预防由 引起的感染。
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