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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 benzocaine with model membranes
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Interaction of benzocaine with model membranes

机译：苯佐卡因与模型膜的相互作用

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摘要

We measured the absorption properties, water solubility and partition coefficients (P) between n-octanol, egg phosphatidylcholine (EPC) liposomes and erythrocyte ghosts/water for benzocaine (BZC), an ester-type always uncharged local anesthetic. The interaction of BZC with EPC liposomes was followed using Electron Paramagnetic Resonance, with spin labels at different positions in the acyl chain (5, 7, 12, 16-doxylstearic acid methyl eater). Changes in lipid organization upon BZC addition allowed the determination of P values, without phase separation. The effect of BZC in decreasing membrane organization (maximum of 11.6% at approx. 0.8:1 BZC:EPC) was compared to those caused by the local anesthetics tetracaine and lidocaine. Hemolytic tests revealed a biphasic (protective/inductive) concentration-dependent hemolytic effect for BZC upon rat erythrocytes, with an effective BZC:lipid molar ratio in the membrane for protection (Re-PROT), onset of hemolysis (Re-SAT) and 100% membrane solubilization (Re-SOL) of 1.0:1, 1.1:1 and 1.3:1, respectively. The results presented here reinforce the importance of considering hydrophobic interactions in the interpretation of the effects of anesthetics on membranes. (C) 2000 Elsevier Science B.V. All rights reserved. [References: 45]
机译：我们测量了正辛醇，卵磷脂酰胆碱（EPC）脂质体和红血球鬼魂/水对苯佐卡因（BZC）（一种酯型始终不带电的局麻药）的吸收性能，水溶性和分配系数（P）。使用电子顺磁共振追踪BZC与EPC脂质体的相互作用，并在酰基链的不同位置（5、7、12、16-双氧硬脂酸甲基酯）带有自旋标记。加入BZC后脂质组织的变化允许测定P值，而没有相分离。与局部麻醉剂丁卡因和利多卡因引起的效果相比，BZC对降低膜组织的效果（在大约0.8：1 BZC：EPC时最大11.6％）进行了比较。溶血试验显示BZC对大鼠红血球具有双相（保护性/诱导性）浓度依赖性溶血作用，在保护膜中有效的BZC：脂质摩尔比（Re-PROT），溶血发作（Re-SAT）和100膜溶解度（Re-SOL）的％分别为1.0∶1、1.1∶1和1.3∶1。本文介绍的结果强调了在解释麻醉药对膜的影响时考虑疏水相互作用的重要性。 （C）2000 Elsevier Science B.V.保留所有权利。 [参考：45]

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