Neves Patrícia, Berkane Emir, Gameiro Paula, Winterhalter Mathias, de Castro Baltazar
Requimte, Departamento de Química, Faculdade de Ciências, R: Campo Alegre, 4169-007 Porto, Portugal.
Biophys Chem. 2005 Feb 1;113(2):123-8. doi: 10.1016/j.bpc.2004.08.004.
In these work, we try to establish a relation between the hydrophobicity of some quinolones and their interaction with OmpF. In order to do that, the values of the binding constant of some quinolones of different "generations" with OmpF were determined by UV-visible spectrophotometry and by fluorimetry. Our results show that there is a strong interaction between all the drugs and the protein and that it becomes larger for the last "generation" fluoroquinolones. These results were compared with previous ones obtained for the interaction of these drugs with simpler biomembrane models (liposomes) and it is possible to conclude that some of the quinolones associate preferably with the protein than with these models. This suggests that an interaction drug/porin is, probably, the preferentially used for the latest fluoroquinolones what makes reasonable to believe that a strong affinity for OmpF means a better capacity to transpose the barrier formed by the outer membrane.
在这些工作中，我们试图建立某些喹诺酮类药物的疏水性与其与外膜孔蛋白F（OmpF）相互作用之间的关系。为了实现这一点，通过紫外可见分光光度法和荧光法测定了不同“代”的一些喹诺酮类药物与OmpF的结合常数。我们的结果表明，所有药物与蛋白质之间都存在强烈的相互作用，并且对于最后一代氟喹诺酮类药物，这种相互作用更强。将这些结果与之前这些药物与更简单的生物膜模型（脂质体）相互作用所获得的结果进行比较，可以得出结论，一些喹诺酮类药物与蛋白质的结合优于与这些模型的结合。这表明药物/孔蛋白之间的相互作用可能是最新一代氟喹诺酮类药物优先采用的方式，这使得我们有理由相信，对OmpF的强亲和力意味着更好的跨越外膜形成的屏障的能力。
