NITTE (Deemed to be University), Nitte University Centre for Science Education and Research, Paneer campus, Deralakatte, Mangaluru 575018, Karnataka, India.
NITTE (Deemed to be University), Nitte Gulabi Shetty Memorial Institute of Pharmaceutical Sciences, Paneer campus, Deralakatte, Mangaluru 575018, Karnataka, India.
Life Sci. 2021 Feb 15;267:118878. doi: 10.1016/j.lfs.2020.118878. Epub 2020 Dec 27.
The study aimed at isolating and identifying potential anti-quorum sensing (QS) compounds from Cinnamomum verum leaves against Pseudomonas aeruginosa.
Isolation of anti-QS compounds from C. verum leaf ethanol extract was carried out by column chromatography. The bioactive fraction was analysed by UV, IR, and GCMS spectroscopy. Various virulence assays were performed to assess the QS quenching ability of the purified compounds. In vivo toxicity of the purified compounds was examined in zebrafish model. The expression of the virulence genes was evaluated by qPCR analysis and in silico assessment was accomplished to check the binding ability of the compounds with the autoinducer molecule.
The QS inhibitors isolated and identified showed a remarkable ability in reducing the production of elastase, pyocyanin, swarming motility and biofilm formation in P. aeruginosa. In the presence of the characterized compounds, the expression of virulence genes of P. aeruginosa was significantly reduced. Toxicity studies in zebrafish model indicated no effects on development and organogenesis at a concentration below 100 mg/l. Further, in silico analysis demonstrated the binding efficiency of the anti-QS compounds to AHL molecules, thus proving the QS quenching ability of the isolated compounds.
To the best of our knowledge this is the first report of isolation of anti-QS compounds from C. verum leaves against P. aeruginosa. The identified compounds qualify as potential QS antagonists. Further studies on these compounds can pave way for an effective and attractive anti-pathogenic therapy, to overcome the emergence of antibiotic resistance in bacteria.
本研究旨在从肉桂叶中分离并鉴定潜在的抗群体感应（QS）化合物，以抑制铜绿假单胞菌。
采用柱层析法从肉桂叶乙醇提取物中分离抗 QS 化合物。通过紫外、红外和 GCMS 光谱分析生物活性馏分。进行各种毒力测定实验，以评估纯化化合物的 QS 淬灭能力。在斑马鱼模型中检测纯化化合物的体内毒性。通过 qPCR 分析评估毒力基因的表达，并进行计算机模拟评估以检查化合物与自动诱导分子的结合能力。
分离和鉴定的 QS 抑制剂在降低铜绿假单胞菌弹性蛋白酶、绿脓菌素、泳动运动和生物膜形成方面表现出显著的能力。在特征化合物存在的情况下，铜绿假单胞菌的毒力基因表达显著降低。在斑马鱼模型中的毒性研究表明，在低于 100mg/L 的浓度下，对发育和器官发生没有影响。此外，计算机模拟分析证明了抗 QS 化合物与 AHL 分子的结合效率，从而证明了分离化合物的 QS 淬灭能力。
据我们所知，这是首次从肉桂叶中分离出抗 QS 化合物来抑制铜绿假单胞菌。鉴定出的化合物可作为潜在的 QS 拮抗剂。对这些化合物的进一步研究可以为有效的、有吸引力的抗致病治疗方法铺平道路，以克服细菌对抗生素耐药性的出现。
