Epand R M, Epand R F, McKenzie R C
J Biol Chem. 1987 Feb 5;262(4):1526-9.
Cyclosporin A, benzyloxycarbonyl-D-Phe-L-Phe-Gly, and amantadine inhibit the dilution of fluorescently labeled lipids, as measured with the resonance energy exchange assay for membrane fusion. The fusion was studied using sonicated vesicles containing 1,2-dioleoyl-sn-glycero(3)phosphoethanolamine, egg (3-sn-phosphatidyl)choline, and cholesterol in a 1:1:1.3 molar ratio. All three antiviral agents inhibited myelin basic protein-induced membrane fusion when present at low concentrations in the membrane. The mechanism by which these agents affect membrane properties was investigated. The effect of these agents on the bilayer to hexagonal phase transition of 1,2-dielaidoyl-sn-glycero(3)phosphoethanolamine was determined using both differential scanning calorimetry and 31P NMR. Benzyloxycarbonyl-D-Phe-L-Phe-Gly is particularly effective in raising the bilayer to hexagonal phase transition temperature while cyclosporin promotes the greatest amount of broadening of the 31P NMR signal. Both effects are suggested to be related to the inhibitory activity of these substances on membrane fusion and possibly also to their antiviral activity.
环孢菌素A、苄氧羰基-D-苯丙氨酸-L-苯丙氨酸-甘氨酸和金刚烷胺可抑制荧光标记脂质的稀释，这是通过用于膜融合的共振能量交换测定法测得的。使用含有摩尔比为1:1:1.3的1,2-二油酰基-sn-甘油（3）-磷酸乙醇胺、鸡蛋（3-sn-磷脂酰）胆碱和胆固醇的超声处理囊泡研究融合过程。当这三种抗病毒药物以低浓度存在于膜中时，它们均能抑制髓鞘碱性蛋白诱导的膜融合。研究了这些药物影响膜特性的机制。使用差示扫描量热法和31P核磁共振法测定了这些药物对1,2-二芥酰基-sn-甘油（3）-磷酸乙醇胺从双层相转变为六方相的影响。苄氧羰基-D-苯丙氨酸-L-苯丙氨酸-甘氨酸在提高双层相到六方相的转变温度方面特别有效，而环孢菌素能使31P核磁共振信号产生最大程度的展宽。这两种效应都被认为与这些物质对膜融合的抑制活性有关，也可能与它们的抗病毒活性有关。
