School of Pharmaceutical, Henan University, Kaifeng 475004, China.
Institute of Microbial Engineering, Laboratory of Bioresource and Applied Microbiology, School of Life Sciences, Hennan Univeristy, Kaifeng 475004, China.
Molecules. 2020 Oct 15;25(20):4727. doi: 10.3390/molecules25204727.
Chinese herbs are a useful resource bank for natural drug development, and have attracted considerable attention to exploit quorum sensing inhibitors (QSIs). This study was designed to screen QSIs from raw Chinese herb materials. Of the 38 common herbs examined, the ethanol extract of flower had the strongest QSI activity. The flower ethanol extract (CFEE) was purified by HPD600, and the QSI activities were examined in further detail. CFEE inhibited violacein production of 026 in a dose-dependent manner, and inhibit the swarming abilities of K-12 and PAO1. Furthermore, CFEE could inhibited biofilm formation and destroyed mature biofilms of K-12 and PAO1. The composition of CFEE was determined by UPLC-MS/MS to distinguish active QSI compounds, and 21 compounds were identified. In addition to gallic acid and caffeic acid, two organic acids, malic acid and succinic acid, were confirmed for the first time to have autoinducer type 1 QSI activities. Therefore, CFEE is a potential QSI that could be used as a novel antimicrobial agent and should be considered for medicinal development.
中草药是天然药物开发的有用资源库，已引起人们的广泛关注，以开发群体感应抑制剂（QSIs）。本研究旨在从天然草药材料中筛选 QSIs。在所检查的 38 种常见草药中， 花的乙醇提取物具有最强的 QSI 活性。通过 HPD600 对 花乙醇提取物（CFEE）进行纯化，并进一步详细检查其 QSI 活性。CFEE 以剂量依赖的方式抑制 026 的紫色素产生，并抑制 K-12 和 PAO1 的群集能力。此外，CFEE 可以抑制生物膜的形成并破坏 K-12 和 PAO1 的成熟生物膜。通过 UPLC-MS/MS 确定 CFEE 的组成，以区分活性 QSI 化合物，并鉴定出 21 种化合物。除了没食子酸和咖啡酸这两种有机酸外，两种有机酸，苹果酸和琥珀酸，也被首次证实具有 1 型群体感应 QSI 活性。因此，CFEE 是一种潜在的 QSI，可以用作新型抗菌剂，应考虑用于药物开发。
