【摘要】 目的　以人急性单核细胞白血病细胞株THP 1为靶细胞 ,以正常骨髓有核细胞作对照 ,体外比较研究低密度脂蛋白 阿克拉霉素 (LDL ACR)复合物与游离阿克拉霉素 (F ACR)的细胞毒作用。方法　采用温育交换法制备LDL ACR复合物 ,荧光分光光度法测定细胞内阿克拉霉素 (ACR)含量 ,细胞蛋白定量法及3 H TdR掺入法观察药物的细胞毒作用。结果　LDL可使细胞对复合物的摄取减少 ,而甲基化LDL无明显影响。LDL ACR复合物对THP 1细胞的生长抑制作用明显比正常骨髓有核细胞抑制作用强。THP 1细胞对LDL ACR复合物的摄取较游离ACR明显增多。LDL ACR复合物较游离ACR能更强地抑制细胞DNA合成。结论　以LDL为载体 ,不仅提高了ACR的抗癌效力 ,而且可减轻ACR对正常细胞的毒性。更多还原

【Abstract】 Objective To investigate the feasibility and effectiveness of low density lipoprotein(LDL) particles as a carrier of a lipophilic anthracycline drug aclarubicin (ACR) for targeting delivery to an acute monocytic leukemia cell line THP 1. Methods LDL ACR complex was prepared by incubating LDL with ACR. The intrace llular ACR content was assayed fluorometrically. Cytotoxicity was studied by cell protein measurement and 3?H TdR incorporation test. Results Intracellular accumulation of LDL ACR was reduced when THP 1 cells were incubated in the presence of native LDL, but methylated LDL had no effect on the cellular LDL ACR accumulation. The LDL ACR complex caused a greater inhibition of the growth of THP 1 cells than that of normal bone marrow nucleated cells. The cellular accumulation of LDL ACR complex was much more than that of free ACR. The 3 H TdR incorporation test showed that the complex was more effective in the inhibition of DNA synthesis than that of the free drug. Conclusion The potency of ACR to tumor cells increased and its toxicity to normal cells decreased when LDL was used as a carrier.更多还原