Zaslavsky B Y, Ossipov N N, Krivich V S, Baholdina L P, Rogozhin S V
Biochim Biophys Acta. 1978 Feb 2;507(1):1-7. doi: 10.1016/0005-2736(78)90368-1.
The hemolytic action of commercially available nonionic surfactants and synthesized polyoxyethylene fatty acids and mercaptans on human erythrocytes was measured. It is shown that the hemolytic power of the detergents depends on the mutual effect of the hydrophobic and hydrophylic fragments of the agent molecule and does not depend on the hydrophile-lipophile balance of the compounds. A graphical image of the structure-activity relationship obtained in the study is similar to the one found in the literature when studying the analgesic effect of imidazoline derivatives on rats in vivo. This fact is discussed on the basis of assumption that the mechanism of both processes in vivo and in vitro is related to influence of the agents on cellular membranes. It is suggested that the role of the polyoxyethylene chain is its effect on the dipole moment and the relative lipophilicity of the compound or in the participation of the fragment in the interaction with the surface components when the agent is sorbed on the membrane. It is concluded that when the correlation between the hydrophile-lipophile balance values and a membrane effect the capacity of the surfactants this indicates that the effect is caused not by destruction of the membrane but by some rearrangement of the membrane structure accompanying the surfactant adsorption.
测定了市售非离子表面活性剂以及合成的聚氧乙烯脂肪酸和硫醇对人体红细胞的溶血作用。结果表明,洗涤剂的溶血能力取决于其分子疏水和亲水片段的相互作用,而不取决于化合物的亲水亲油平衡。该研究中获得的结构-活性关系的图形与文献中研究咪唑啉衍生物对大鼠体内镇痛作用时发现的图形相似。基于体内和体外这两个过程的机制都与药物对细胞膜的影响有关这一假设,对这一事实进行了讨论。有人认为,聚氧乙烯链的作用在于它对化合物偶极矩和相对亲脂性的影响,或者在于当药物吸附在膜上时该片段参与与表面成分的相互作用。得出的结论是,当亲水亲油平衡值与表面活性剂的膜效应之间存在相关性时,这表明该效应不是由膜的破坏引起的,而是由伴随表面活性剂吸附的膜结构的某种重排引起的。