摘要
以低密度脂蛋白 (L DL)为化疗药物阿克拉霉素 (ACM)的载体 ,用游离 ACM为对照 ,体外研究 L DL- ACM复合物对慢性急变细胞株 K562 的细胞毒作用及影响因素。结果显示 :1.K562 细胞对 L DL- ACM复合物在开始 30 min摄取较快 ,以后速度逐渐减慢 ;2 .细胞对复合物的摄取较游离 ACM明显增多 ;3.过量的天然 L DL、肝素及低温均可使细胞对复合物的摄取明显减少 ,而过量 HDL则无影响 ,去脂蛋白血清予刺激的细胞摄取复合物明显增多 ;4 .复合物对 K562 细胞生长的抑制作用 ,从细胞存活率、细胞内蛋白质含量和 DNA合成等方面进行观察 ,发现随复合物浓度增加而逐渐增强。当药物浓度达
The 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 K 562 was studied The results indicated that 1, The time course for LDL ACM complex accumulation in K 562 cells showed that its cellular uptake was rapid during the first 30 min followed by a slower phase 2, the accumulation of LDL ACM complex was greater than that of free ACM In the cells drug accumulation was reduced when K 562 cells were incubated in the presence of either of an excess of native LDL of heparin ,incubated at 4℃ When cells were stimulated by LPDS,cellular drug accumulation was abviously increase But the presence of an excess of native HDL had no effect on cellular drug accumulation 3 The LDL as a drug carrier the cell growth inhibition was demonstrated through the experiments of cellular protein concentration, 3H TdR incorporation test and cellular survival rate The results were that the LDL ACM complex was more obvious than free ACM Therefore we concluded that LDL may be used as a good carrier for lipophilic antineoplastic drugs
出处
《药物生物技术》
CAS
CSCD
1997年第3期169-173,共5页
Pharmaceutical Biotechnology