Gao X P, Noda Y, Rubinstein I, Paul S
Department of Anesthesiology, University of Nebraska Medical Center, Omaha 68198-6830.
Life Sci. 1994;54(15):PL247-52. doi: 10.1016/0024-3205(94)00425-0.
The purpose of this study was to determine whether encapsulation of vasoactive intestinal peptide (VIP) in liposomes enhances its vasoactive effects. Liposomes were formed from a solution of VIP in phospholipids and cholesterol, resulting in incorporation of 0.008 mole peptide/mole phospholipid. Leakage of VIP from the liposomes was undetectable over several days of incubation at 4 degrees C in 0.15 M sodium chloride. Under conditions permitting rapid hydrolysis of VIP by trypsin, there was no breakdown of the encapsulated peptide. Increasing concentrations of the liposome-encapsulated VIP administered intravenously to anesthetized hamsters produced a concentration-dependent decrease in the mean arterial blood pressure. The duration and magnitude of the hypotensive effect of the encapsulated VIP was significantly greater (p < 0.05) compared to equivalent concentrations of the unencapsulated peptide. Infusion of empty liposomes was without significant effect on the mean arterial blood pressure. We conclude that encapsulation of VIP in liposomes potentiates the blood pressure-lowering effect of the peptide.
本研究的目的是确定将血管活性肠肽(VIP)包裹于脂质体中是否会增强其血管活性作用。脂质体由VIP在磷脂和胆固醇中的溶液形成,导致每摩尔磷脂中掺入0.008摩尔肽。在0.15M氯化钠中于4℃孵育数天,未检测到VIP从脂质体中泄漏。在允许胰蛋白酶快速水解VIP的条件下,包裹的肽未发生降解。将脂质体包裹的VIP以递增浓度静脉注射给麻醉的仓鼠,导致平均动脉血压呈浓度依赖性下降。与同等浓度的未包裹肽相比,包裹的VIP的降压作用持续时间和幅度显著更大(p<0.05)。输注空脂质体对平均动脉血压无显著影响。我们得出结论,将VIP包裹于脂质体中可增强该肽的降压作用。