Chaim-Matyas A, Borkow G, Ovadia M
Department of Zoology, George S. Wise Faculty of Life Sciences, Tel Aviv University, Ramat Aviv, Israel.
Biotechnol Appl Biochem. 1993 Feb;17(1):31-6.
Cytotoxin P4 isolated from the venom of the cobra Naja nigricollis nigricollis was encapsulated in liposomes by the reverse-phase evaporation method using phosphatidylcholine, cholesterol and phosphatidylethanolamine at molar ratios of 3:1:1. Cytotoxicity examination on murine melanoma B16F10 revealed that the activity of the entrapped cytotoxin did not change significantly and remained stable for at least 1 year at 4 degrees C without any significant leak from the liposomes (< 1%). Moreover, the activity of the cytotoxic liposomes was 20-fold higher towards human erythrocytes. Whereas 45 micrograms of the free cytotoxin/ml were needed for total haemolysis, the cytotoxic liposomes brought about the same effect at cytotoxin concentrations of 2-2.5 micrograms/ml, indicating the potential of the liposomes as a delivery system for the snake toxin.
采用反相蒸发法,以摩尔比为3:1:1的磷脂酰胆碱、胆固醇和磷脂酰乙醇胺,将从眼镜蛇黑颈眼镜蛇毒液中分离出的细胞毒素P4包裹于脂质体中。对小鼠黑色素瘤B16F10进行细胞毒性检测发现,包封的细胞毒素活性没有显著变化,在4℃下至少可稳定保存1年,脂质体无明显渗漏(<1%)。此外,细胞毒性脂质体对人红细胞的活性高20倍。游离细胞毒素/ml需要45微克才能实现完全溶血,而细胞毒性脂质体在细胞毒素浓度为2 - 2.5微克/ml时就能产生相同效果,表明脂质体作为蛇毒素递送系统的潜力。