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某些黄酮类化合物及其磺酸衍生物抗菌活性的比较研究。

Comparative study on the antibacterial activity of some flavonoids and their sulfonic derivatives.

作者信息

Woźnicka Elzbieta, Kuźniar Anna, Nowak Dorota, Nykiel Elzbieta, Kopacz Maria, Gruszecka Jolanta, Golec Krzysztof

机构信息

Department of Inorganic and Analytical Chemistry, Faculty of Chemistry, Rzeszów University of Technology, 6 Powstańców Warszawy St., 35-959 Rzeszów, Poland.

出版信息

Acta Pol Pharm. 2013 May-Jun;70(3):567-71.

PMID:23757948
Abstract

The antibacterial activity of quercetin, morin, sodium salt of quercetin-5'-sulfonic acid (NaQSA) and sodium salt of morin-5'-sulfonic acid (NaMSA) were tested against six bacterial strains: Escherichia coli (ATCC 25922 and clinical isolates--ESBL), Pseudomonas aeruginosa (ATCC 27853 and clinical isolates--carbapenem resistant), Staphylococcus aureus (ATCC 29213 and clinical isolats- MRSA). The most effective inhibitors against the model strain S. aureus are NaQSA and NaMSA (MIC = 3.9 microg/mL). Among polyhydroxyflavones used in this investigation, morin exhibits the highest antibacterial activity against tested strains. The structure-activity relationship indicates that 2',4'-dihydroxylation of the B ring in the flavanone structure is important for significant antibacterial activity and that substitution of the sulfo group at position 5' on the lateral phenyl ring enhances antistaphylococcal activity of flavonoids.

摘要

测试了槲皮素、桑色素、槲皮素 - 5'-磺酸的钠盐(NaQSA)和桑色素 - 5'-磺酸的钠盐(NaMSA)对六种细菌菌株的抗菌活性:大肠杆菌(ATCC 25922和临床分离株 - ESBL)、铜绿假单胞菌(ATCC 27853和临床分离株 - 耐碳青霉烯类)、金黄色葡萄球菌(ATCC 29213和临床分离株 - MRSA)。对模式菌株金黄色葡萄球菌最有效的抑制剂是NaQSA和NaMSA(MIC = 3.9微克/毫升)。在本研究中使用的多羟基黄酮中,桑色素对测试菌株表现出最高的抗菌活性。构效关系表明,黄酮酮结构中B环的2',4'-二羟基化对于显著的抗菌活性很重要,并且在侧链苯环的5'位上磺基的取代增强了黄酮类化合物的抗葡萄球菌活性。

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