Obika S, Yu W, Shimoyama A, Uneda T, Minami T, Miyashita K, Doi T, Imanishi T
Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Japan.
Biol Pharm Bull. 1999 Feb;22(2):187-90. doi: 10.1248/bpb.22.187.
Cationic lipid N-[3-[2-(1,3-dioleoyloxy)propoxy-carbonyl]propyl]-N,N,N-trimethyla mmonium iodide (YKS-220) having a symmetrical and biodegradable structure was employed for the preparation of cationic liposomes with dioleoylphosphatidylethanolamine (DOPE). The stability, transfection activity in several cell lines and cytotoxicity of YKS-220 cationic liposomes were studied. It was found the YKS-220 cationic liposomes were very stable and their transfection activity remained even after storage at 4 degrees C for 12 months. The transfection activity of these liposomes was assayed using CHO, COS, and HepG2 cells and found to be comparable with, or better than, that of other cationic liposomes, such as N-[1-(2,3-dioleoyloxy)propyl]-N,N,N-trimethylammonium methylsulfate (DOTAP) liposome, N-[1-(2,3-dioleyloxy)propyl]-N,N,N-trimethylammonium chloride (DOTMA) liposome (Lipofectin), and 2,3-dioleyloxy-N-[2-(sperminecarboxamido)ethyl]-N,N-dimethyl -1-propanaminium trifluoroacetate (DOSPA) liposome (LipofectAMINE). In addition, the cytotoxicity of YKS-220 cationic liposomes was far lower than that of other cationic liposomes.
具有对称且可生物降解结构的阳离子脂质N-[3-[2-(1,3-二油酰氧基)丙氧基羰基]丙基]-N,N,N-三甲基碘化铵(YKS-220)被用于与二油酰磷脂酰乙醇胺(DOPE)制备阳离子脂质体。研究了YKS-220阳离子脂质体的稳定性、在几种细胞系中的转染活性和细胞毒性。发现YKS-220阳离子脂质体非常稳定，即使在4℃储存12个月后其转染活性仍保持。使用CHO、COS和HepG2细胞测定了这些脂质体的转染活性，发现其与其他阳离子脂质体相当或更好，如N-[1-(2,3-二油酰氧基)丙基]-N,N,N-三甲基硫酸甲酯铵(DOTAP)脂质体、N-[1-(2,3-二油酰氧基)丙基]-N,N,N-三甲基氯化铵(DOTMA)脂质体(Lipofectin)和2,3-二油酰氧基-N-[2-(精胺甲酰胺基)乙基]-N,N-二甲基-1-丙胺三氟乙酸盐(DOSPA)脂质体(LipofectAMINE)。此外，YKS-220阳离子脂质体的细胞毒性远低于其他阳离子脂质体。
