黄酮类化合物在许多生物活性合成和天然化合物中代表结构支架。它们展示了各种各样的生物活性,包括抗癌,抗糖尿病药,抗结核药,抗疟药,和抗生物膜活性。研究了一系列新的查耳酮和黄酮醇对临床上显着的铜绿假单胞菌PAO1菌株的抗生物膜活性。通过分析化合物对毒力因子产生的影响来筛选抗毒力活性,LasA蛋白酶,细胞表面疏水性,还有鼠李糖脂.群体感应蛋白LasR的最佳配体,RhlR,使用分子对接研究识别PqsR。在群体感应基因上评估用测试化合物处理后铜绿假单胞菌中的基因表达,包括rhlA,LasB,和pqsE。通过有效减少毒力因子的产生和基因表达的下调,证实了查耳酮和黄酮醇的抗生物膜潜力。
Flavonoids epitomize structural scaffolds in many biologically active synthetic and natural compounds. They showcase a diverse spectrum of biological activities including anticancer, antidiabetic, antituberculosis, antimalarial, and antibiofilm activities. The antibiofilm activity of a series of new chalcones and flavonols against clinically significant Pseudomonas aeruginosa PAO1 strain was studied.
Antivirulence activities were screened by analysing the effect of compounds on the production of virulence factors like pyocyanin, LasA protease, cell surface hydrophobicity, and rhamnolipid. The best ligands towards the quorum sensing proteins LasR, RhlR, and PqsR were recognised using a molecular docking study. The gene expression in P. aeruginosa after treatment with test compounds was evaluated on quorum sensing genes including rhlA, lasB, and pqsE. The antibiofilm potential of chalcones and flavonols was confirmed by the efficient reduction in the production of virulence factors and downregulation of gene expression.