一种具有转运催化特征的菲克扩散传输过程。阿霉素在人红细胞中的转运。
A Fickian diffusion transport process with features of transport catalysis. Doxorubicin transport in human red blood cells.
作者信息
Dalmark M, Storm H H
出版信息
J Gen Physiol. 1981 Oct;78(4):349-64. doi: 10.1085/jgp.78.4.349.
The transport of the antineoplastic drug doxorubicin (Adriamycin) in human red blood cells was investigated by measuring the net efflux from loaded cells. Previous data indicated that doxorubicin transport was a Fickian diffusion transport process of the electrically neutral molecule through the lipid domain of the cell membrane (Dalmark, 1981 [In press]). However, doxorubicin transport showed saturation kinetics and a concentration-dependent temperature dependence with nonlinear Arrhenius plots. The two phenomena were related to the doxorubicin partition coefficient between 1-octanol and a water phase. This relationship indicated that the two phenomena were caused by changes in the physiochemical properties of doxorubicin in the aqueous phase and were not caused by interaction of doxorubicin with cell membrane components. The physicochemical properties of doxorubicin varied with concentration and temperature because of the ability of doxorubicin to form polymers by self-association in aqueous solution like other planar aromatic molecules through pi-electron orbital interaction. The hypothesis is proposed that doxorubicin transport across cell membranes takes place by simple Fickian diffusion.
通过测量加载细胞的净流出量，研究了抗肿瘤药物阿霉素（阿霉素）在人红细胞中的转运。先前的数据表明，阿霉素的转运是电中性分子通过细胞膜脂质结构域的菲克扩散转运过程（达尔马克，1981年[即将出版]）。然而，阿霉素的转运表现出饱和动力学以及浓度依赖性温度依赖性，阿累尼乌斯图呈非线性。这两种现象与阿霉素在正辛醇和水相之间的分配系数有关。这种关系表明，这两种现象是由水相中阿霉素物理化学性质的变化引起的，而不是由阿霉素与细胞膜成分的相互作用引起的。由于阿霉素能够像其他平面芳香分子一样通过π电子轨道相互作用在水溶液中通过自缔合形成聚合物，其物理化学性质随浓度和温度而变化。提出的假设是，阿霉素跨细胞膜的转运是通过简单的菲克扩散进行的。
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