顺式铂自旋标记配合物对人红细胞膜通透特性的研究  

STUDY OF PERMEABILITY OF CIS-SPIN LABELED PLATINUM COMPLEXES THROUGH HUMAN ERYTHROCYTE MEMBRANE

作　　者：卢景芬[1] 安佩东 马玉良[1] 杨正红[1] 张宇涛[1] 窦培延[1] 李刚[1] 

机构地区：[1]北京医科大学天然药物及仿生药物国家重点实验室,北医大药研所,北医大基础学院

出　　处：《生物物理学报》1995年第2期196-200,共5页Acta Biophysica Sinica

基　　金：国家自然科学基金

摘　　要：合成了顺式铂自旋标记配合物，实现了用电子顺磁共振方法直接研究药物通透人红细胞膜的特性。结果表明：２０μｍｏｌ／Ｌ的铂自旋标记配合物通透的半寿命为数分钟。不同的配体结构表现不同的通道特性，提示可能存在药物小分子与膜分子之间的静电相互作用及配位相互作用。从脂质体ＤＰＰＣ相交特性的研究可知：铂自旋标记配合物比之母体配合物．使ＤＰＰＣ相变温度升高更多，从而影响跨膜通透的速率，因此有助于降低药物毒性。Spin labeled analogues of cisplatin were synthsized and used to study the permeability of drugs across the human erythrocyte membrane with ESR (electron spin resonce) technique directly. The results indicated f the half-time for 20μmol/L drugs leaking out through membrane is about several minutes. The difference in permeability of various ligands suggests that electrostatic and binding interactions may exist between drugs and membrane molecules.The study of the phase transition of liposome DPPC showed f the spin labeled analogues can increase phase transitinn temperature much more than its parent Pt (Ⅱ) compound. These biophysical fcature can provide a theory basis of improve ment on drugs.

关 键 词：铂自旋标记 配合物 通透特性 红细胞膜 分子药理 

分 类 号：R966[医药卫生—药理学]