Metronidazole–Flavonoid Derivatives as Anti‐Helicobacter pylori Agents with Potent Inhibitory Activity against HPE‐Induced Interleukin‐8 Production by AGS Cells
Metronidazole–Flavonoid Derivatives as Anti‐Helicobacter pylori Agents with Potent Inhibitory Activity against HPE‐Induced Interleukin‐8 Production by AGS Cells
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DOI：
10.1002/cmdc.200700097
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发表时间：
2007-09
期刊：
影响因子：
3.4
通讯作者：
Huan-qiu Li;Chen Xu;Hong‐Sen Li;Zhu-Ping Xiao;Lei Shi;Hailiang Zhu
中科院分区：
文献类型：
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作者：
Huan-qiu Li;Chen Xu;Hong‐Sen Li;Zhu-Ping Xiao;Lei Shi;Hailiang Zhu
本文合成了三个系列的甲硝唑类黄酮衍生物，并对它们进行了体外抗菌活性的研究。幽门。在这些化合物中，高抗H.幽门螺杆菌的活性在马槟榔酮衍生物4-7、19和20中观察到，但对其它种类的细菌和真菌，例如肺炎链球菌、枯草芽孢杆菌、大肠杆菌、荧光假单胞菌和尼日尔曲霉没有表现出抑制活性。染料木黄酮衍生物6具有强效活性（MIC=0.39 μg mL-1），是甲硝唑的50倍以上，并且与阳性对照阿莫西林相当。此外，化合物6可以显著减弱由H. pylori水提取物（HPE）浓度为15、30和60 μmol L-1，对细胞活力没有任何影响。
Three series of metronidazole–flavonoid derivatives were generated and evaluated for antimicrobial activity against H. pylori. Among these compounds, high anti‐H. pylori activities were observed in isoflavones derivatives 4–7, 19, and 20 but exhibited no inhibitory activity against other sorts of bacteria and fungi, for example, Streptococcus pneumoniae, Bacillus subtilis, Escherichia coli, Pseudomonas fluorescence, and Aspergillus niger. Genistein derivative 6 with the potent activity (MIC=0.39 μg mL−1) was >50‐fold more than metronidazole, and comparable to the positive control amoxicillin. Additionally, compound 6 can significantly attenuate the increase in interleukin‐8 (IL‐8) levels in the AGS cells stimulated by H. pylori water extract (HPE) at concentrations of 15, 30, and 60 μmol L−1, which did not show any effects on the cell viability.