外排泵参与了革兰氏阴性菌对天然产物异甘草素和地奥配酮的防御。
Efflux pumps are involved in the defense of Gram-negative bacteria against the natural products isobavachalcone and diospyrone.
机构信息
Department of Biochemistry, Faculty of Science, University of Dschang, Dschang, Cameroon.
出版信息
Antimicrob Agents Chemother. 2010 May;54(5):1749-52. doi: 10.1128/AAC.01533-09. Epub 2010 Feb 16.
Abstract
The activities of two naturally occurring compounds, isobavachalcone and diospyrone, against documented strains and multidrug-resistant (MDR) Gram-negative bacterial isolates were evaluated. The results indicated that the two compounds exhibited intrinsic antibacterial activity against several Gram-negative bacteria, and their activities were significantly improved in the presence of an efflux pump inhibitor (MIC values decreased to below 10 microg/ml). In addition, the activities of isobavachalcone and diospyrone against various strains exhibiting deletions of the major efflux pump components (AcrAB, TolC) were significantly increased. The overall results indicate that isobavachalcone and diospyrone could be candidates for the development of new drugs against MDR strains and that their use in combination with efflux pump inhibitors reinforces their activity.
摘要
两种天然存在的化合物，异甘草素和地奥配酮，对已记录的菌株和多药耐药（MDR）革兰氏阴性细菌分离株的活性进行了评估。结果表明，这两种化合物对几种革兰氏阴性菌表现出内在的抗菌活性，并且在存在外排泵抑制剂的情况下，其活性显著提高（MIC 值降低至低于 10μg/ml）。此外，异甘草素和地奥配酮对各种缺失主要外排泵成分（AcrAB、TolC）的菌株的活性显著增加。总体结果表明，异甘草素和地奥配酮可能是开发针对 MDR 菌株的新药的候选药物，并且它们与外排泵抑制剂联合使用可以增强其活性。
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