The cytotoxicity and apoptotic effect of phytoceramide IV （N-palmitoyl-phytospingosine） were investigated by preparaing the ceramide containing liposomes using cholesteryl hemisuccinate （CHEMS） and methoxypolyethy...The cytotoxicity and apoptotic effect of phytoceramide IV （N-palmitoyl-phytospingosine） were investigated by preparaing the ceramide containing liposomes using cholesteryl hemisuccinate （CHEMS） and methoxypolyethylene glycol （2000） cholesteryl succinate （PEGCHS）. The ceramide-containing liposomes prepared using ultrasonication contained CHEMS and the phytoceramide IV at a molar ratio of 1：1. Gel chromatography and high performance liquid chromatography equipped with an evaporative light-scattering detection （HPLC-ELSD） were used to analyze the liposomes. The results show that the ceramide entrapment efficiency is over 90% and the molar ratio of phytoceramide IV to CHEMS is 1：1.4. The ratio of ceramide to CHEMS as well as the ultrasonication duration affects the liposome properties. The phytoceramide Ⅳ encapsulated in the liposomes reduces the cellular activity of the murine mastocytoma cell line P815 in a dose-dependent manner and the reduction of cellular activity is due to cell apoptosis. 4. 6-diamidino- 2-phenylindole dihydrochloride （DAPI） staining further supports this result. The encapsulation of highly hydrophobic ceramides into liposomal formulations could become a potential candidate for enhanced apoptosis.展开更多
基金the National Natural Science Foundation of China (Nos. 30170017 and 50436040)the National Natural Science Foundation for Outstanding Young Investigator (No. 30225001)
文摘The cytotoxicity and apoptotic effect of phytoceramide IV （N-palmitoyl-phytospingosine） were investigated by preparaing the ceramide containing liposomes using cholesteryl hemisuccinate （CHEMS） and methoxypolyethylene glycol （2000） cholesteryl succinate （PEGCHS）. The ceramide-containing liposomes prepared using ultrasonication contained CHEMS and the phytoceramide IV at a molar ratio of 1：1. Gel chromatography and high performance liquid chromatography equipped with an evaporative light-scattering detection （HPLC-ELSD） were used to analyze the liposomes. The results show that the ceramide entrapment efficiency is over 90% and the molar ratio of phytoceramide IV to CHEMS is 1：1.4. The ratio of ceramide to CHEMS as well as the ultrasonication duration affects the liposome properties. The phytoceramide Ⅳ encapsulated in the liposomes reduces the cellular activity of the murine mastocytoma cell line P815 in a dose-dependent manner and the reduction of cellular activity is due to cell apoptosis. 4. 6-diamidino- 2-phenylindole dihydrochloride （DAPI） staining further supports this result. The encapsulation of highly hydrophobic ceramides into liposomal formulations could become a potential candidate for enhanced apoptosis.
