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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。
Objective To compare the effects of LDL ACR complex with free clarithromycin (F (superscript 2 +)) in human acute myelomonocytic leukemia cell line THP 1 as target cells and normal bone marrow as control ACR) cytotoxicity. Methods The LDL ACR complex was prepared by incubation and exchange method. The content of aclacinomycin (ACR) was determined by fluorescence spectrophotometry. The cytotoxicity of the drug was observed by the method of cellular protein quantification and 3 H TdR incorporation. Results LDL decreased cellular uptake of the complex, whereas methylated LDL had no significant effect. The inhibitory effect of LDL ACR complex on THP 1 cells was significantly stronger than that of normal bone marrow cells. THP 1 cells uptake of LDL ACR complex significantly increased compared with free ACR. LDL ACR complex more strongly inhibited cellular DNA synthesis than free ACR. Conclusion LDL as a carrier, not only increased the anti-cancer efficacy of ACR, but also reduce the toxicity of ACR on normal cells.