期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 61, 期 34, 页码 8185-8190出版社
AMER CHEMICAL SOC
DOI: 10.1021/jf402222v
关键词
Flavonoids; DNA gyrase; Escherichia coli; antibacterial; structure activity relationships
资金
- National Natural Science Foundation of China [31171756]
- Scientific Research Foundation for the Returned Overseas Chinese Scholars, State Education Ministry
Flavonoids are potential sources of natural preservatives. The inhibitory activities of three polymethoxylated flavones (PMFs), three flavones, and four flavonols against Escherichia coli were determined using the microbroth dilution method. Flavonoid inhibitory activities against DNA gyrase from E. coli were estimated by DNA supercoiling. Kaempferol exhibited the greatest antibacterial activity [minimal inhibitory concentration (MIC) = 25 mu g/mL], while nobiletin showed the lowest activity (MIC = 177 mu g/mL). A good correlation was found between the pIC(50) values and the corresponding pMIC values for the purified DNA gyrase (r = 0.9582). The structure activity relationship analysis suggests that, for a good inhibitory effect, the hydroxyl group substitution at C-5 in the A ring and C-4' in the B ring and the methoxyl group substitution at C-3 and C-8 in the A ring are essential. The presence of the hydroxyl group at C-6 in the A ring, C-3' and C-5' in the B ring, and C-3 in the C ring and the methoxyl group at C-3' in the B ring greatly reduced inhibition of bacteria. These findings provide a theoretical basis for the development of high-bioactive and low-toxicity natural preservatives.
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