Dipartimento di Scienze del Farmaco Università G. d'Annunzio Via dei Vestini, 66013 Chieti, Italy.
Small. 2010 Apr 23;6(8):952-9. doi: 10.1002/smll.200902306.
The effect of the luminescent heteroaromatic electron acceptor N,N'-dimethyl-2,7-diazapyrenium dichloride (DM-DAP(2+)) on the stability of 1-palmitoyl-2-oleoylphosphatydilcholine (POPC) liposomes is determined on the basis of the rate of release of different fluorescent probes entrapped within the liposome. The experiments show that DM-DAP(2+) exerts a substantial destabilizing action on the liposomal bilayer, particularly at low concentrations. Molecular dynamics simulations suggest that the activity of DM-DAP(2+) is related to its tendency to surround itself with water molecules, conceivably favoring the formation of transient pores across the bilayer.
基于不同荧光探针在脂质体中释放的速率，确定了发荧光的杂芳族电子受体 N,N'-二甲基-2,7-二氮杂芘二氯化物 (DM-DAP(2+)) 对 1-棕榈酰基-2-油酰基磷脂酰胆碱 (POPC) 脂质体稳定性的影响。实验表明，DM-DAP(2+) 对脂质体双层具有显著的去稳定作用，特别是在低浓度下。分子动力学模拟表明，DM-DAP(2+) 的活性与其与水分子形成配合物的趋势有关，这可能有利于跨双层形成瞬时孔。
