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Flavonoids from Praxelis clematidea R.M. King and Robinson Modulate Bacterial Drug Resistance

机译:桔梗R.M.金和鲁滨逊调节细菌耐药性

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摘要

Chemical studies of Praxelis clematidea R.M. King & Robinson resulted in the isolation of six flavones: Apigenine, genkwanine, 7,4’-dimethylapigenin, trimethylapigenin, cirsimaritin and tetramethylscutellarein, which were tested for their toxicity against Staphylococcus aureus SA-1199B, a strain possessing the NorA efflux pump. Efflux pumps are integral proteins of the bacterial membrane and are recognized as one of the main causes of bacterial drug resistance, since they expel antibiotics from the cell. The inhibition of this transporter is one form of modulating bacterial resistance to antimicrobial drugs. The flavones tested did not show any significant antibacterial activity against the Staphylococcus aureus strain used, but were able to modulate bacterial drug resistance. This property might be related to the degree of lipophilicity of the flavones conferred by the methoxyl groups, since 4’,5,6,7 tetramethoxyflavone the most methoxylated compound, reduced the minimal inhibitory concentration of the drug 16-fold.
机译:Praxelis clematidea R.M.的化学研究King&Robinson分离出六种黄酮:芹菜碱,genkwanine,7,4′-二甲基芹菜素,三甲基芹菜素,西西马汀和四甲基黄cut苷,它们对金黄色葡萄球菌SA-1199B(具有NorA外排泵的菌株)具有毒性。外排泵是细菌膜的必需蛋白,被认为是细菌耐药性的主要原因之一,因为它们将抗生素从细胞中排出。抑制这种转运蛋白是调节细菌对抗菌药物耐药性的一种形式。测试的黄酮对所使用的金黄色葡萄球菌菌株没有显示任何显着的抗菌活性,但是能够调节细菌的耐药性。该性质可能与甲氧基所赋予的黄酮的亲脂性程度有关,因为4',5,6,7四甲氧基黄酮是最被甲氧基化的化合物,其最低抑菌浓度降低了16倍。

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