在5ml无水氯仿/甲醇/三乙胺溶剂混合物(4.5:0.5:0.05 v/v)中,用20倍摩尔过量的NHS/EDC(1:1摩尔比)活化6毫克MAL-PEG(3000)-MMP2-COH过夜。在4°C氮气保护下,使活化的MAL-PEG(3000)-MMP2-NHS与10倍摩尔过量的DOPE反应2小时。使用氯仿/甲醇(4:1 v/v)作为流动相,在制备型铝TLC板(硅胶60 F254,20 x 20 cm,Merck)上纯化反应。纯化冷冻干燥的残留物,并在−20°C下储存,以获得产品1,2-二油酰-SN-甘油-3-磷酰乙醇胺。
IC50: helper lipid for liposome
In this study, each siRNA is encapsulated in LNP (cationic lipid-A: PEG2000-DMPE: DOPE = 47.8: 5.18: 47.1 molar percent).With the neutral lipid for the LNP is DOPE , LNP exerts knock-down (KD) effecton macrophages and DCs and Liposome-containing DOPE shows fusogenicity.LNP/siRNA significantly suppresses CD45 protein expression at an inhibition rate of 30% on macrophages and DCs but not on monocytes, neutrophils, plasmacytoid DCs, or B cells.LNP has the potential to be an efficient siRNA delivery system not only for murine but also for human macrophages and DCs.