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两性分子与有序磷脂膜的相互作用模式

孙进*, 程刚, 何仲贵, 王淑君, 陈济民   

  1. 沈阳药科大学生物药剂研究室, 沈阳 110016
  • 收稿日期:2002-09-09 修回日期:2003-02-10 出版日期:2003-03-15 发布日期:2003-03-15
  • 通讯作者: 孙进*

Interactions Mode of Amphoteric Molecules with Ordered Phospholipid Membrane

SUN Jin*, CHENG Gang, HE Zhong-gui, WANG Shu-jun, CHEN Ji-min   

  1. Department of Biopharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China
  • Received:2002-09-09 Revised:2003-02-10 Online:2003-03-15 Published:2003-03-15
  • Contact: SUN Jin*

摘要: 目的 揭示两性分子与有序磷脂膜的作用模式。方法 分别使用磷脂膜色谱和正辛醇水系统测定药物的膜亲和性和疏水性参数。结果 两性分子与有序磷脂膜存在吸引性极性附加作用力, 其测定的膜亲和性参数要明显比由疏水性参数预测的值高。结论 结合两性分子复杂的微观质子平衡, 不仅其中性、阳性而且两性的微观离子可能通过匹配的构象和能量有利的作用模式而有效的分布到有序的两性磷脂膜中, 并且后两者的分配产生了与有序磷脂膜的吸引性极性附加作用力。

关键词: 与磷脂膜作用, 两性分子, 极性附加作用力, 磷脂膜色谱

Abstract: Aim To explore interaction mode between amphoteric molecules with the ordered phospholipid membrane. Methods Membrane interactions were determined by immobilized artificial membrane (IAM) chromatography and solutes'hydrophobicity was measured by n-octanol/buffer system. Results The ampholytes, similar to bases, generally exhibitedhigher membrane affinity than expected from their hydrophobicity, resulting from the attractive polar interaction with phospholipid membrane. Furthermore, the strength of additional polar interaction with membrane (△lg kIAM) was then calculated. The △lg kIAM values were far greater for bases and ampholytes ranging from 0.50-1.39, than those for acids and neutrals with the scope from -0.55-0.44. Conclusion Considering the microspecies distribution of amphoteric molecules, itwas assumed that not only neutral and positive but also zwitterionic microspecies are capable of partitioning into ordered amphoteric lipid membrane with complementarily conformational and energetically favorable interactions.

Key words: membrane interactions, membrane interactions, amphoteric molecules, amphoteric molecules, polar extra interaction, polar extra interaction, immobilized artificial membrane chromatography, immobilized artificial membrane chromatography

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Supporting: *Corresponding author. Tel.: 86-024-23953083; fax: (024) 23841116