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化学学报
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化学学报 ›› 1999, Vol. 57 ›› Issue (7): 659-666. 上一篇    下一篇

研究论文

人红细胞摄取环己二胺合铂(Ⅱ)配合物的手性选择性研究

高愈希;李荣昌;吴刚;卢景芬;王夔   

  1. 北京医科大学生物无机及无机药物化学系;北京医科大学天然药物与仿生药物国 家重点实.北京(100083)
  • 发布日期:1999-07-15

Studies on the chiral selectivity of transmembrane transport of the pt(Ⅱ)complexeswith 1,2--diaminocyclohexane as carrier ligand into human erythrocytes

Gao Yuxi;Li Rongchang;Wu Gang;Lu Jingfen;Wang Kui   

  1. Beijing Med Univ., Laboratory of Natural and Bionic Drugs.Beijing (100083)
  • Published:1999-07-15

PDF

440

被引次数

35

合成了六种以不同手性的1,2-环己二胺(1,2-dach)作为载体配体的铂(Ⅱ)配合物,用元素分析、红外及分子图形方法对其组成和结构进行了表征.测定了它们跨人红细胞膜的一级反应动力学常数.用膜蛋白巯基滴定、荧光标记、自旋标记ESR谱等方法研究了它们与膜蛋白、膜脂的相互作用;用脂质体模拟了这些配合物的细胞摄入.结果表明:这些配合物主要通过简单扩散进入红细胞,其跨膜速率对环己二胺的手性具有明显的选择性.这种选择性主要来源于配合物与膜脂作用过程中的手性识别。

关键词: 红细胞, 环己二胺, 铂络合物, 元素分析, 红外分光光度法, 分子图形, 脂质体, 摄取, 抗癌活性

Six Pt(Ⅱ) complexes with chital 1,2 --diaminocyclohexane as carrier ligand were synthesized, their compositions and strctures were characterized by elemental analysis,IR spectroscopy and molecular modeling. The first -order rate constants for the transmembrane transport of the complxes into human erythrocytes were detemined and the mechanism was studied on the basis of the interactions of these complexes with cellular membranes and liposome by ESR,fluorescence technique, mercapto measurement and gelchromatography. The results show that the transmembrane transport of the complexes studied exhibited a chiral selectivity, and the selectivity is mainly due to chiral recognition of membrane phospholipid with the chiral complexes.

Key words: ERYTHROCYTES, PLATINUM COMPLEX, ELEMENTAL ANALYSIS, INFRARED SPECTROPHOTOMETRY, LIPOSOME, UPTAKE

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