摘要
以低密度脂蛋白（ＬＤＬ）为阿克拉霉素（ＡＣＭ）的载体，以游离ＡＣＭ为对照，体外研究ＬＤＬ－ＡＣＭ复合物对白血病细胞株Ｋ５６２的细胞毒作用及其影响因素。结果显示：（１）Ｋ５６２细胞对ＬＤＬ－ＡＣＭ复合物摄取较游离ＡＣＭ明显增加，在前３０ｍｉｎ摄取较快，随时间延长摄取逐渐减慢；（２）过量的天然ＬＤＬ、肝素及低温均可使细胞摄取复合物明显减少，而过量的ＨＤＬ则无影响，去脂蛋白血清预刺激的细胞摄取复合物明显增多；（３）对Ｋ５６２细胞的细胞毒作用随复合物浓度增加而逐渐增强，达１０ｍｇ／Ｌ以上时，增加药物浓度其细胞毒作用不再加强。
This study was to investigate the feasibility and effetiveness of LDL particles as a carrier for the targeted delivery of a lipophilic anthracycline drug aclacinomycin(ACM) to a chronic myelogenous leukemia in blastic crisis cell line K562.It was found that(1)the time course for LDLACM complex accumulation in K562 cells showed that its cellular uptake was rapid during the first 30 min followed by a slower plase;(2)the accumulation of LDLACM complex was greater than that of free ACM.In the cells drug accumulation was reduced when K562 cells were incubated in the presence of either of an excess of native LDL or heparin,incubated at 4℃.When cells were stimulated by LPDS,cellular drug accumulation obviously increased.But the presence of an excess of native HDL had no effect on cellular drug accumulation;(3)with LDL as a drug carrier,the cell growth inhibition was demonstrated through the experiments of cellular protein concentration,3HTdR incorporation test and cellular survival fraction.The results indicated that the LDLACM complex was more obvious than free ACM.Therefore the conclusion can be drawn that LDL may be used as a good carrier for lipophilic antineoplastic drugs.
出处
《山东医科大学学报》
1998年第1期27-30,共4页
Acta Academiae Medicinae Shandong
