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吸入麻醉剂和醇类在水与不同酰基链长度的磷脂膜之间的分配平衡。

Partition equilibrium of inhalation anesthetics and alcohols between water and membranes of phospholipids with varying acyl chain-lengths.

作者信息

Kamaya H, Kaneshina S, Ueda I

出版信息

Biochim Biophys Acta. 1981 Aug 6;646(1):135-42. doi: 10.1016/0005-2736(81)90280-7.

Abstract

From the depression of the phase-transition temperature of phospholipid membranes, the partition coefficients of inhalation anesthetics (methoxyflurane, halothane, enflurane, chloroform and diethyl ether) and alcohols (benzyl alcohol and homologous n-alcohols up to C = 7) between phospholipid vesicle membranes and water were determined. The phospholipids used were dimyristoyl-, dipalmitoyl- and distearoylphosphatidylcholines. It was found that the difference in the acyl chain length of the three phospholipids did not affect the partition coefficients of the inhalation anesthetics and benzyl alcohol. The actions of these drugs are apparently directed mainly to the interfacial region. In contrast, n-alcohols tend to bind more tightly to the phospholipid vesicles with longer acyl chains. The absolute values of the transfer free energies of n-alcohols increased with the increase of the length of the alkyl chain of the alcohols. The increment was 3.43 kJ per each carbon atom. The numerical values of the partition coefficients are not identical when different expressions for solute concentrations (mole fraction, molality and molarity) are employed. The conversion factors among these values were estimated from the molecular weights and the partial molal volumes of the phospholipids in aqueous solution determined by oscillation densimetry.

摘要

通过磷脂膜相变温度的降低,测定了吸入麻醉剂(甲氧氟烷、氟烷、恩氟烷、氯仿和乙醚)以及醇类(苯甲醇和碳数直至C = 7的正构醇同系物)在磷脂囊泡膜与水之间的分配系数。所用的磷脂为二肉豆蔻酰磷脂酰胆碱、二棕榈酰磷脂酰胆碱和二硬脂酰磷脂酰胆碱。结果发现,这三种磷脂的酰基链长度差异并不影响吸入麻醉剂和苯甲醇的分配系数。这些药物的作用显然主要针对界面区域。相比之下,正构醇倾向于与酰基链更长的磷脂囊泡结合得更紧密。正构醇转移自由能的绝对值随着醇类烷基链长度的增加而增加。每增加一个碳原子,增量为3.43 kJ。当采用溶质浓度的不同表达式(摩尔分数、质量摩尔浓度和摩尔浓度)时,分配系数的数值并不相同。这些数值之间的转换因子是根据通过振动密度测定法测定的磷脂在水溶液中的分子量和偏摩尔体积估算得出的。

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