Chantres J R, Sainz M C
Departamento de Química Física Farmacéutica, Facultad de Farmacia (UCM), Madrid, Spain.
J Pharm Sci. 1992 Jan;81(1):74-8. doi: 10.1002/jps.2600810115.
Phenylbutazone (PhB), a powerful anti-inflammatory drug, is able to modify the phase transition of phospholipid bilayers without changing its calorimetric enthalpy (delta Hcal), as can be shown by differential scanning calorimetry (DSC) experiments. Under PhB interaction, dimiristoyl phosphatidylcholine (DMPC) multilamellar liposomes (MLV) undergo lateral phase separation as a result of immiscibility in the bilayer plane. On the other hand, the binding of the anionic fluorescent probe 8-anilino-1-naphthalene sulfonate (ANS) to the surface of DMPC liposomes is altered by PhB. Even though the quantum efficacy of the probe fluorescence emission remains unaffected, the negative cooperativity of the binding process disappears, with the intrinsic dissociation constant showing only a minor variation. From these results it is concluded that PhB would be most likely located close to the lipid:water interface.
保泰松（PhB）是一种强效抗炎药物，通过差示扫描量热法（DSC）实验表明，它能够改变磷脂双层的相变，而不改变其量热焓（ΔHcal）。在PhB相互作用下，二肉豆蔻酰磷脂酰胆碱（DMPC）多层脂质体（MLV）由于双层平面内的不混溶性而发生横向相分离。另一方面，阴离子荧光探针8-苯胺基-1-萘磺酸盐（ANS）与DMPC脂质体表面的结合会被PhB改变。尽管探针荧光发射的量子效率不受影响，但结合过程的负协同性消失，固有解离常数仅显示出微小变化。从这些结果可以得出结论，PhB很可能位于脂质 - 水界面附近。
