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本文引用的文献

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Natural product drug discovery in the next millennium.下一个千年的天然产物药物发现。
Pharm Biol. 2001;39 Suppl 1:8-17. doi: 10.1076/phbi.39.s1.8.0009.
2
Efflux-mediated drug resistance in bacteria: an update.细菌中由外排介导的耐药性:最新进展
Drugs. 2009 Aug 20;69(12):1555-623. doi: 10.2165/11317030-000000000-00000.
3
Diospyrone, crassiflorone and plumbagin: three antimycobacterial and antigonorrhoeal naphthoquinones from two Diospyros spp.柿酮、粗花醌和白花丹素:来自两种柿属植物的三种抗分枝杆菌和抗淋病萘醌类化合物
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Geraniol restores antibiotic activities against multidrug-resistant isolates from gram-negative species.香叶醇可恢复针对革兰氏阴性菌的多重耐药菌株的抗生素活性。
Antimicrob Agents Chemother. 2009 May;53(5):2209-11. doi: 10.1128/AAC.00919-08. Epub 2009 Mar 2.
5
Mechanisms of drug efflux and strategies to combat them: challenging the efflux pump of Gram-negative bacteria.药物外排机制及其应对策略:挑战革兰氏阴性菌的外排泵
Biochim Biophys Acta. 2009 May;1794(5):826-33. doi: 10.1016/j.bbapap.2008.12.011. Epub 2008 Dec 25.
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Antimicrobial activity of the crude extracts and five flavonoids from the twigs of Dorstenia barteri (Moraceae).巴氏肉托果(桑科)嫩枝粗提物及五种黄酮类化合物的抗菌活性
J Ethnopharmacol. 2008 Mar 28;116(3):483-9. doi: 10.1016/j.jep.2007.12.017. Epub 2008 Jan 11.
7
Antitumor, antioxidant and antimicrobial activities of Bersama engleriana (Melianthaceae).非洲梨木(蜜花科)的抗肿瘤、抗氧化和抗菌活性。
J Ethnopharmacol. 2008 Feb 12;115(3):494-501. doi: 10.1016/j.jep.2007.10.027. Epub 2007 Oct 26.
8
Isobavachalcone, a chalcone constituent of Angelica keiskei, induces apoptosis in neuroblastoma.异补骨脂查耳酮,一种明日叶中的查耳酮成分,可诱导神经母细胞瘤细胞凋亡。
Biol Pharm Bull. 2007 Oct;30(10):1878-83. doi: 10.1248/bpb.30.1878.
9
Susceptibility and intrinsic tolerance of Pseudomonas aeruginosa to selected plant volatile compounds.铜绿假单胞菌对选定植物挥发性化合物的敏感性和内在耐受性。
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10
Pandrug-resistant Gram-negative bacteria: the dawn of the post-antibiotic era?泛耐药革兰氏阴性菌:抗生素后时代的曙光?
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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.

DOI:10.1128/AAC.01533-09
PMID:20160051
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2863662/
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。