Hainan General Hospital, Hainan Affiliated Hospital of Hainan Medical University, Haikou, 570311, China; Key Laboratory of Tropical Biological Resources of Ministry of Education, School of Pharmaceutical Sciences, Hainan University, Haikou, 570228, China.
Key Laboratory of Tropical Biological Resources of Ministry of Education, School of Pharmaceutical Sciences, Hainan University, Haikou, 570228, China.
J Ethnopharmacol. 2024 Feb 10;320:117422. doi: 10.1016/j.jep.2023.117422. Epub 2023 Nov 16.
The formation of biofilms is a factor leading to chronic infection and drug resistance in melioidosis. The production of biofilm formation and many virulence factors are regulated by quorum sensing (QS). Therefore, the discovery of QS inhibitors to reduce antibiotic abuse has attracted a lot of attention. In this case, the methanol extract of a unique ethnic medicinal plant partridge tea (Mallotus oblongifolius (Miq.) Müll.Arg.) and its isolated active compound were used as biofilms and QS inhibitors against Burkholderia thailandensis.
The purpose of this study is to investigate the anti-biofilm and anti-QS effect of the ethnic medicinal plant partridge tea and its active compounds against B. thailandensis.
Active compound was isolated using classical phytochemical separation techniques under activity tracking. The biofilm and virulence factors (Proteases, lipases, rhamnolipids, and motility) of B. thailandensis were used to evaluate the activity of crude extracts and isolated compounds.
In this study, the extract of partridge tea and MG had good QS inhibitors activity against B. thailandensis E264. MG was investigated to inhibit QS-related virulence factors and the biofilm formation against B. thailandensis E264. The lipase activity of B. thailandensis E264 decreased by 49.41% at 150 μg/mL. At 75 μg/mL and 150 μg/mL, the erasion of mature biofilms reached 28.18% and 70.87%, respectively. Correspondingly, 150 μg/mL MG could significantly decrease btaR1 and btaR3 by 55.78% and 56.24%, respectively. Contradictorily, the rhamnolipid production of B. thailandensis E264 was 1.67 folds that of the control group at 150 μg/mL MG.
Through molecular docking analysis and biological phenotype data, we speculate that MG may inhibit the biofilms and virulence factors of B. thailandensis E264 by interfering two QS systems, BtaI1/R1 and BtaI3/R3. Therefore, MG should be one potential QSI for the treatment of Burkholderia pathogens.
生物膜的形成是导致类鼻疽慢性感染和耐药的一个因素。生物膜的形成和许多毒力因子的产生受群体感应（QS）调节。因此，发现减少抗生素滥用的 QS 抑制剂引起了广泛关注。在这种情况下，独特的民族药用植物鹧鸪茶（Mallotus oblongifolius（Miq.）Müll.Arg.）甲醇提取物及其分离的活性化合物被用作针对伯克霍尔德氏菌的生物膜和 QS 抑制剂。
本研究旨在探讨民族药用植物鹧鸪茶及其活性化合物对伯克霍尔德氏菌的抗生物膜和抗 QS 作用。
采用经典的植物化学分离技术，在活性跟踪下分离活性化合物。使用生物膜和毒力因子（蛋白酶、脂肪酶、鼠李糖脂和运动性）来评估粗提取物和分离化合物的活性。
在这项研究中，鹧鸪茶提取物和 MG 对伯克霍尔德氏菌 E264 具有良好的 QS 抑制剂活性。MG 被研究用于抑制与 QS 相关的毒力因子和伯克霍尔德氏菌 E264 的生物膜形成。在 150μg/mL 时，B. thailandensis E264 的脂肪酶活性降低了 49.41%。在 75μg/mL 和 150μg/mL 时，成熟生物膜的消除率分别达到 28.18%和 70.87%。相应地，在 150μg/mL MG 时，btaR1 和 btaR3 的减少分别达到 55.78%和 56.24%。相反，在 150μg/mL MG 时，B. thailandensis E264 的鼠李糖脂产量是对照组的 1.67 倍。
通过分子对接分析和生物表型数据，我们推测 MG 可能通过干扰两个 QS 系统 BtaI1/R1 和 BtaI3/R3 来抑制 B. thailandensis E264 的生物膜和毒力因子。因此，MG 应该是治疗伯克霍尔德氏菌病原体的一种有潜力的 QSI。
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