Department of Physical Chemistry and Electrochemistry, Faculty of Chemistry, Jagiellonian University, ul. R. Ingardena 3, 30-060 Krakow, Poland.
J Phys Chem B. 2011 Jul 28;115(29):9290-8. doi: 10.1021/jp202716k. Epub 2011 Jul 7.
Three nonsteroidal anti-inflammatory oxicam drugs, namely meloxicam, piroxicam, and tenoxicam, were used to modify the properties of monomolecular films formed with 1,2-dilauroyl-sn-glycero-3-phosphocholine, 1,2-dilauroyl-sn-glycero-3-phosphoethanolamine, or 1,2-dilauroyl-sn-glycero-3-phospho-(1-rac-glycerol). These systems were examined via surface pressure and surface electrical potential measurements, polarization modulation infrared reflection absorption spectroscopy, and Brewster angle microscopy. Moreover, phospholipase A2 activity was used to differentiate between the three drugs. Our results reveal that the oxicams studied modify membrane properties, namely hydration of the lipid polar heads, orientation of the molecules, and morphology of the domains. Phospholipase A2 was shown to be sensitive to the presence of the drugs in the systems studied; the activity of the enzyme correlates with the effect of meloxicam, piroxicam, and tenoxicam on the monolayer properties. The latter indicates that the anti-inflammatory action of oxicams may be related to interference with phospholipase activity in addition to cyclooxygenase inhibition.
三种非甾体类抗炎药（oxicam），即美洛昔康、吡罗昔康和替诺昔康，被用于修饰由 1,2-二月桂酰基-sn-甘油-3-磷酸胆碱、1,2-二月桂酰基-sn-甘油-3-磷酸乙醇胺或 1,2-二月桂酰基-sn-甘油-3-磷酸-(1-rac-甘油)形成的单分子膜的性质。这些系统通过表面压力和表面电势测量、偏振调制红外反射吸收光谱和布鲁斯特角显微镜进行了研究。此外，还使用了磷脂酶 A2 活性来区分这三种药物。我们的结果表明，研究中的 oxicams 会改变膜性质，即脂质极性头部的水合作用、分子的取向和域的形态。研究表明，磷脂酶 A2 对系统中药物的存在很敏感；该酶的活性与美洛昔康、吡罗昔康和替诺昔康对单层性质的影响相关。这表明 oxicams 的抗炎作用可能与除了环氧化酶抑制之外，还与干扰磷脂酶活性有关。
