Rustenbeck I, Reiter H, Lenzen S
Institute of Pharmacology and Toxicology, University of Gottingen, Germany.
Biochem Mol Biol Int. 1996 Apr;38(5):1003-11.
The aliphatic polyamine bis(hexamethylene)triamine, a spermidine analogue, was found to lack the enhancing effect on mitochondrial Ca(2+) accumulation which is typical for the natural polyamines, spermidine and spermine. However, like spermine and spermidine, this compound had a significant inhibitory effect on the Ca(2+) and Pi-induced mitochondrial permeability transition. By chromatographic determination of the amount of polyamines bound to mitochondria after a 2 min incubation, it was found that the binding affinity was spermine > or = bis(hexamethylene)triamine > spermidine. There was no competition between binding of spermine and of bis(hexamethylene)triamine. It is concluded that membrane binding sites of bis(hexamethylene)triamine are different from those of spermine. This different membrane interaction is apparently caused by the elongated hydrophobic spans in bis(hexamethylene)triamine and leads to a loss of the effect on Ca(2+) uptake but leaves intact the inhibitory effect on membrane permeability transition.
脂肪族多胺双（六亚甲基）三胺是一种亚精胺类似物，已发现它对线粒体Ca(2+)积累缺乏增强作用，而这种作用是天然多胺亚精胺和精胺所特有的。然而，与精胺和亚精胺一样，该化合物对Ca(2+)和Pi诱导的线粒体通透性转变具有显著抑制作用。通过色谱法测定2分钟孵育后与线粒体结合的多胺量，发现结合亲和力为精胺>或 = 双（六亚甲基）三胺>亚精胺。精胺和双（六亚甲基）三胺的结合之间没有竞争。得出的结论是，双（六亚甲基）三胺的膜结合位点与精胺的不同。这种不同的膜相互作用显然是由双（六亚甲基）三胺中延长的疏水跨度引起的，并导致对Ca(2+)摄取的作用丧失，但对膜通透性转变的抑制作用保持不变。
