REQUIMTE, Departamento de Química, Faculdade de Farmácia, Universidade do Porto, Rua Aníbal Cunha 164, 4090-030 Porto, Portugal.
Biophys Chem. 2010 Nov;152(1-3):109-17. doi: 10.1016/j.bpc.2010.08.006. Epub 2010 Aug 25.
The present study describes the interaction of two nonsteroidal anti-inflammatory drugs (ibuprofen and piroxicam) with PLA(2) from Naja mossambica mossambica and seeks to deepen the knowledge about the influence of the biophysical properties of biomembranes, and the inhibitory effect of the drugs on the enzymatic activity. Fluorescent techniques with and without the use of probes, surface pressure/molecular area isotherms, surface pressure/time and molecular area/time measurements combined with circular dichroism spectroscopy and direct techniques of visualization of lipid membranes (Brewster angle microscopy), revealed that both drugs inhibit PLA(2). Additionally, the structure and characteristics of the lipid bilayer, as well as, the direct interaction of drugs with the enzyme seem to play an important role on the hydrolytic activity of PLA(2) towards membrane model systems. These results open a way of finding new and better strategies that can contribute to the development of suitable agents for relieving inflammatory conditions.
本研究描述了两种非甾体抗炎药（布洛芬和吡罗昔康）与来自 Naja mossambica mossambica 的 PLA（2）的相互作用，并试图加深对生物膜的生物物理特性的影响以及药物对酶活性的抑制作用的认识。使用和不使用探针的荧光技术、表面压力/分子面积等温线、表面压力/时间和分子面积/时间测量结合圆二色性光谱和脂质膜的直接可视化技术（布鲁斯特角显微镜）表明，这两种药物都抑制 PLA（2）。此外，脂质双层的结构和特性以及药物与酶的直接相互作用似乎对 PLA（2）对膜模型系统的水解活性起着重要作用。这些结果为寻找新的更好的策略开辟了道路，这些策略可以为开发缓解炎症状况的合适药物做出贡献。
