We previously showed that cationic liposomes composed of cholesteryl-3β-carboxyamidoethylene-N-hydroxyethylamine (OH-Chol) and 1,2-dioleoyl-sn-glycero-3-phosphatidylethanolamine (DOPE) inhibited mast cell degranulation mediated by the cross-linking of high-affinity IgE receptors (FcεRI). In this study, we prepared three kinds of cationic liposomes composed of OH-Chol and DOPE in different ratios (0.28, 0.60, and 0.86 of OH-Chol in mol ratio, named as L-liposome, M-liposome, and H-liposome, respectively) and investigated their effects on mast cell activation. We found that mast cell degranulation evoked with antigen was inhibited by pretreatment with cationic liposomes in the composite ratio-dependent manner of OH-Chol and that the H-liposome showed the highest inhibitory effect on degranulation among three kinds of liposomes. Store-operated Ca²⁺ entry, phosphorylation of PI3K and Akt, and IL-4 secretion after antigen stimulation were reduced in dose-dependent manner of each liposome, but there were no differences between H-liposome and M-liposome. Meanwhile, microtubule acetylation, which is involved in the secretory granule transport, was significantly suppressed by H-liposome compared with M-liposome. These data suggested that the lipid composition in cationic liposomes themselves largely influenced the inhibition of mast cell activation as well as the efficiency of gene transfection.

先前我们显示了由胆固醇3β-羧酰胺基乙烯-N-羟乙胺（OH-Chol）和1,2-二油酰基-sn组成的阳离子脂质体-甘油-3-磷脂酰乙醇胺（DOPE）抑制由高亲和力IgE受体（FcεRI）交联介导的肥大细胞脱粒。在本研究中，我们制备了三种不同比例的由OH-Chol和DOPE组成的阳离子脂质体（摩尔比为0.28、0.60和0.86的OH-Chol），分别称为L-脂质体，M-脂质体和H-脂质体。 ），并研究它们对肥大细胞活化的影响。我们发现，通过阳离子脂质体的预处理以OH-Chol的复合比例依赖性方式抑制了抗原诱发的肥大细胞脱粒，并且在三种脂质体中，H-脂质体对脱粒的抑制作用最高。储运钙²⁺每种脂质体的剂量依赖性方式降低了抗原进入后，PI3K和Akt的磷酸化，PI3K和Akt的磷酸化以及IL-4的分泌，但H-脂质体和M-脂质体之间没有差异。同时，与M-脂质体相比，H-脂质体显着抑制了参与分泌性颗粒运输的微管乙酰化。这些数据表明阳离子脂质体本身中的脂质组成极大地影响了肥大细胞活化的抑制以及基因转染的效率。