Trombe M C, Beaubestre C, Sautereau A M, Labarre J F, Laneelle G, Tocanne J F
Biochem Pharmacol. 1984 Sep 1;33(17):2749-53. doi: 10.1016/0006-2952(84)90691-9.
Interactions of the antitumoral drug SOAz with natural and model membranes are described. Biological studies were carried out with the bacterium Streptococcus pneumoniae taken as a model system. They reveal that SOAz is able to reduce delta psi and the delta psi-dependent amino acid transports without being cytotoxic for the bacteria. With respect to model membranes, leakage studies carried out with Na+ and K+ loaded lipid vesicles demonstrated that SOAz exhibits no ionophore activity. In contrast, the drug is shown to decrease the surface potential of monolayers of acidic phospholipids but without penetrating within the film. The possibility that SOAz might alter the delta psi part of the proton motive force by decreasing the outside surface potential of the bacterial membrane is discussed.
描述了抗肿瘤药物SOAz与天然膜和模型膜的相互作用。以肺炎链球菌为模型系统进行了生物学研究。研究表明,SOAz能够降低Δψ以及依赖于Δψ的氨基酸转运,而对细菌没有细胞毒性。关于模型膜,用装载Na+和K+的脂质囊泡进行的渗漏研究表明,SOAz没有离子载体活性。相反,该药物被证明可降低酸性磷脂单层的表面电位,但不会穿透膜层。讨论了SOAz可能通过降低细菌膜的外表面电位来改变质子动力的Δψ部分的可能性。