葫芦[7]脲增强氟喹诺酮类药物抗菌活性和延长货架期的超分子方法。
A Supramolecular Approach for Enhanced Antibacterial Activity and Extended Shelf-life of Fluoroquinolone Drugs with Cucurbit[7]uril.
机构信息
Institute of Nanoscience & Nanotechnology, Kafrelsheikh University, 33516, Kafrelsheikh, Egypt.
Chemistry Department, Faculty of Science, Kafrelsheikh University, 33516, Kafrelsheikh, Egypt.
出版信息
Sci Rep. 2018 Sep 17;8(1):13925. doi: 10.1038/s41598-018-32312-6.
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.
第三代氟喹诺酮丹氟沙星（DOFL）与大环主体瓜环（CB7）在不同 pH 值（~3.5、7.5 和 10）下的主体-客体相互作用已经过研究。在 CB7 的存在下，光物理性质得到了积极的影响，即荧光产率和寿命增加，以及 DOFL 的光稳定性得到了改善。在 CB7 的存在下，DOFL 的抗菌活性得到了增强，对四种致病菌进行了测试；对蜡状芽孢杆菌和大肠杆菌的活性最高，对金黄色葡萄球菌和伤寒沙门氏菌的活性较低。还研究了另外两种第二代氟喹诺酮类药物，即诺氟沙星和氧氟沙星，在不存在和存在 CB7 的情况下的抗菌活性，并与 DOFL 进行了比较。对于所有药物，在 CB7 的存在下，最低抑菌浓度（MIC）降低了 3-5 倍。在 CB7 的存在下，氟喹诺酮类药物的保质期（随时间的抗菌活性）延长，与四种类型的细菌无关，这可以归因于它们的 CB7 配合物的增强的光稳定性，与未配位的 DOFL 相比，它们可以作为更好的抗生素，具有更长的有效期。
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