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A Supramolecular Approach for Enhanced Antibacterial Activity and Extended Shelf-life of Fluoroquinolone Drugs with Cucurbit7uril

机译:一种超分子方法增强葫芦丝氟喹诺酮类药物的抗菌活性和延长保质期7 uril

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摘要

The host-guest interactions of a third-generation fluoroquinone, danofloxacin (DOFL), with the macrocyclic host cucurbit[7]uril (CB7) have been investigated at different pH values (~3.5, 7.5, and 10). The photophysical properties have been positively affected, that is, the fluorescence yield and lifetime increased, as well as the photostability of DOFL improved in the presence of CB7. The antibacterial activity of DOFL is enhanced in the presence of CB7, as tested against four pathogenic bacteria; highest activity has been found towards B. cereus and E. coli, and lower activity towards S. aureus and S. typhi. The antibacterial activity of two additional second-generation fluoroquinones, i.e., norfloxacin and ofloxacin, has also been investigated in the absence as well as the presence of CB7 and compared with that of DOFL. In case of all drugs, the minimum inhibitory concentration (MIC) was reduced 3–5 fold in the presence of CB7. The extended shelf-life (antibacterial activity over time) of the fluoroquinone drugs in the presence of CB7, irrespective of four types of bacteria, can be attributed to the enhanced photostability of their CB7 complexes, which can act as better antibiotics with a longer expiry date than uncomplexed DOFL.
机译:在不同的pH值(〜3.5、7.5和10)下,已经研究了第三代氟醌丹诺沙星(DOFL)与大环葫芦葫芦[7] uril(CB7)的宿主-客体相互作用。光物理性质受到积极影响,即在CB7存在下,荧光产量和寿命增加,以及DOFL的光稳定性得到改善。如针对四种病原菌所测试,在CB7存在下,DOFL的抗菌活性得以增强。已发现对蜡状芽孢杆菌和大肠杆菌的活性最高,而对金黄色葡萄球菌和伤寒链球菌的活性较低。在不存在和存在CB7的情况下,还研究了另外两种第二代氟醌即诺氟沙星和氧氟沙星的抗菌活性,并将其与DOFL进行了比较。对于所有药物,在存在CB7的情况下,最低抑菌浓度(MIC)降低3-5倍。在不考虑四种细菌的情况下,在存在CB7的情况下,氟醌药物的货架期延长(随着时间的推移具有抗菌活性)可以归因于其CB7复合物的光稳定性增强,这可以作为具有更长使用寿命的更好的抗生素日期比没有复杂的DOFL。

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