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首页> 外文期刊>Biophysical Chemistry: An International Journal Devoted to the Physical Chemistry of Biological Phenomena >Interaction of two phenothiazine derivatives with phospholipid monolayers.
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Interaction of two phenothiazine derivatives with phospholipid monolayers.

机译：两种吩噻嗪衍生物与磷脂单层的相互作用。

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摘要

This paper addresses the cooperative interaction of two phenothiazine drugs, viz. trifluoperazine (TFP) and chlorpromazine (CPZ), with phospholipid monolayers as the model membrane system. Surface pressure and surface potential isotherms were obtained for mixed Langmuir monolayers of either dipalmitoyl-phosphatidyl-choline (DPPC) or dipalmitoyl-phosphatidyl-glycerol (DPPG) co-spread with TFP or CPZ. The changes in monolayer behavior caused by incorporation of a few molar ratio of drug molecules were practically within the experimental dispersion for the zwitterionic DPPC, and therefore a more refined analysis will be required to probe the interactions in an unequivocal way. For the charged DPPG, on the other hand, the surface pressure and the dipole moment were significantly affected even for TFP or CPZ concentrations as low as 0.002 molar ratio. Overall, the effects from CPZ and TFP are similar, but small differences exist which are probably due to the different protonation properties of the two drugs. For both drugs, changes are more prominent at the liftoff of the surface pressure, i.e. at the gas-condensed phase transition, with the surface pressure and surface potential isotherms becoming more expanded with the drug incorporation. With DPPG/CPZ monolayers, in particular, an additional phase transition appears at higher CPZ concentrations, which resembles the effects from increasing the subphase temperature for a pure DPPG monolayer. The dipole moment for DPPG/CPZ and DPPG/TFP monolayers decreases with the drug concentration, which means that the effects from the charged drugs are not associated with changes in the double-layer potential. Otherwise, the effective dipole moment should increase with the drug concentration. The changes caused in surface pressure and dipole moment by small concentrations of TFP or CPZ can only be explained by some cooperative effect through which the contribution from DPPG molecules changes considerably, i.e. even DPPG molecules that are not neighbor to a CPZ or TFP molecule are also affected. Such changes may occur either through a significant reorientation of the DPPG molecules or to a change in their hydration state. We discuss the cooperativity semi-quantitatively by estimating the number of lipid molecules affected by the drug interaction. CPZ and TFP also affect the morphology of DPPG monolayers, which was confirmed with Brewster angle microscopy. The biological implications from the cooperative, non-specific interaction of CPZ and TFP with membranes are also commented upon.
机译：本文探讨了两种吩噻嗪药物的协同相互作用。三氟拉嗪（TFP）和氯丙嗪（CPZ），以磷脂单层作为模型膜系统。获得了与TFP或CPZ共铺的二棕榈酰磷脂酰胆碱（DPPC）或二棕榈酰磷脂酰甘油（DPPG）的混合Langmuir单层的表面压力和表面电位等温线。两性离子DPPC的实验分散液实际上是由于掺入了几个摩尔比的药物分子而引起的单层行为的变化，因此需要更精细的分析以明确地检测相互作用。另一方面，对于带电的DPPG，即使当TFP或CPZ浓度低至0.002摩尔比时，表面压力和偶极矩也会受到显着影响。总体而言，CPZ和TFP的作用相似，但存在细微差异，这可能是由于两种药物的质子化特性不同所致。对于这两种药物，随着表面压力的升高，即在气相凝结的相变处，变化更明显，随着药物的结合，表面压力和表面电位等温线变得越来越大。特别是对于DPPG / CPZ单层，在更高的CPZ浓度下会出现额外的相变，这类似于增加纯DPPG单层的亚相温度所产生的影响。 DPPG / CPZ和DPPG / TFP单层的偶极矩随药物浓度而降低，这意味着带电药物的作用与双层电势的变化无关。否则，有效偶极矩应随药物浓度而增加。小浓度的TFP或CPZ引起的表面压力和偶极矩的变化只能通过某种协同效应来解释，通过这种协同效应，DPPG分子的贡献会发生显着变化，即，即使与CPZ或TFP分子不相邻的DPPG分子也可以受到影响。此类变化可能通过DPPG分子的明显重新定向或它们的水合状态发生变化而发生。我们通过估计受药物相互作用影响的脂质分子的数量来半定量地讨论协同性。 CPZ和TFP也会影响DPPG单层的形态，这一点已通过Brewster角显微镜得到了证实。还评论了CPZ和TFP与膜的合作性，非特异性相互作用的生物学意义。

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