Partitioning and structural effects of the antitumor drug daunomycin on model membranes.
Partitioning and structural effects of the antitumor drug daunomycin on model membranes.
复制标题
抗肿瘤药物道诺霉素对模型膜的分配和结构影响。
DOI：
10.1016/s0024-3205(98)00462-7
复制
发表时间：
1998
期刊：
影响因子：
6.1
通讯作者：
Subczynski,WK
中科院分区：
文献类型：
--
作者：
Pezeshk,A;Wojas,J;Subczynski,WK
采用电子顺磁共振自旋标记法研究了抗肿瘤药物道诺霉素对磷脂酰胆碱膜相变和动力学性质的影响。采用饱和二myristoyl磷脂酰胆碱和不饱和蛋黄磷脂酰胆碱制备的多层脂质体。在道霉素的作用下，饱和双分子层的主相变明显变宽。在饱和膜的流体相中，道诺霉素导致自旋探针16-羟基硬脂酸（16-SASL）的旋转运动减少。这种效应通过提高温度而大大减弱。在不饱和膜中，没有观察到道诺霉素对16-SASL旋转运动的影响。提出中性形态的道诺霉素可以在脂质双分子层中分裂，扩散到膜的更深的疏水区域，并减少烷基链的运动。
The effects of the antitumor drug daunomycin on the phase transition and dynamic properties of phosphatidylcholine membranes were investigated using the electron paramagenetic resonance spin labeling method. Multilamellar liposomes made of saturated dimyristoylphosphatidylcholine and unsaturated egg yolk phosphatidylcholine were used. The main phase transition of saturated bilayer was significantly broadened in the presence of daunomycin. In the fluid phase of saturated membranes, daunomycin caused a decrease in the rotational motion of the spin probe 16-doxylstearic acid (16-SASL). This effect was strongly diminished by raising the temperature. In unsaturated membranes no influence of daunomycin on the rotational motion of 16-SASL was observed. It is proposed that the neutral form of daunomycin can partition into lipid bilayer where it can diffuse into deeper hydrophobic regions of the membrane and decrease the motion of alkyl chains.