背景:生物膜的形成是导致类石病的慢性感染和耐药性的一个因素。生物膜形成和许多毒力因子的产生受群体感应(QS)调节。因此,QS抑制剂减少抗生素滥用的发现引起了很多关注。在这种情况下,一种独特的民族药用植物part茶的甲醇提取物(Mallotusoblongifolius(Miq.)穆勒。Arg.)及其分离的活性化合物被用作生物膜和QS抑制剂,以对抗泰国伯克霍尔德氏菌。
目的:本研究的目的是研究民族药用植物part茶及其活性化合物对B.thailandensis的抗生物膜和抗QS作用。
方法:在活性跟踪下使用经典的植物化学分离技术分离活性化合物。生物膜和毒力因子(蛋白酶,脂肪酶,鼠李糖脂,和运动性)用于评估粗提物和分离化合物的活性。
结果:在这项研究中,part茶和MG的提取物对B.thailandensisE264具有良好的QS抑制剂活性。研究了MG抑制QS相关毒力因子和针对泰国芽孢杆菌E264的生物膜形成。在150μg/mL时,B.thailandensisE264的脂肪酶活性降低了49.41%。在75μg/mL和150μg/mL时,成熟生物膜的擦除率分别达到28.18%和70.87%,分别。相应地,150μg/mLMG可使btaR1和btaR3显著降低55.78%和56.24%,分别。矛盾的是,在150μg/mLMG时,B.thailandensisE264的鼠李糖脂产量是对照组的1.67倍。
结论:通过分子对接分析和生物学表型数据,我们推测MG可能通过干扰两个QS系统来抑制B.thailandensisE264的生物膜和毒力因子,BtaI1/R1和BtaI3/R3。因此,MG应该是治疗伯克霍尔德氏菌病原体的潜在QSI。
BACKGROUND: 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.
OBJECTIVE: 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.
METHODS: 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.
RESULTS: 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.
CONCLUSIONS: 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.