摘要
目的 :探讨乳糖酰磷脂酰乙醇胺修饰的阿霉素脂质体对肝癌细胞的杀伤作用。方法 :在NaBH4 还原作用下连接乳糖和磷脂酰乙醇胺制备乳糖酰乙醇胺 (Lac_PE) ,反应 40 0h测定偶联率为 48.6 % ,硅酸柱层析得到纯品。用 10 %的Lac_PE整合到超声法制备的小单层脂质体 (由PC :chol:PE以 7∶2∶1摩尔比组成 )脂膜上。结果 :其插入率为 99.6 % ,乳糖脂阿霉素脂质体体外杀瘤试验 (MTT法 )表明 :48h细胞毒试验乳糖脂阿霉素脂质体对人肝癌细胞系SMMC - 772 1的杀伤作用显著优于无糖脂脂质体 (P <0 .0 1) ,以IC50 计 ,乳糖脂脂质体的杀伤作用是对照组的 16 .3倍 ,而对非靶细胞 (B16黑色素瘤细胞 )的杀伤作用二者相近。 0 .5h预处理试验表明 :缩短药物与细胞接触时间后 ,乳糖脂阿霉素脂质体仍保持较强的杀伤肝癌作用 ,IC50 为 2 .74μg/ml,而对照组为 48.7μg/ml。 结论 :表明乳糖脂阿霉素脂质体的杀伤作用来自半乳糖基配体的特异性介导和人肝癌细胞上肝凝集素的识别内吞作用。
Objective:To probe into the effects of lactosylphatitylethanolamine_modified ADM Liposomes on hepatic carcinoma cells in vitro.Method:Lactosylphosphatidylethanolamine(Lac_PE) was synthesized with lactose and L_2_phosphatidylethanlamine under reduction of NaBH4,and coupling rate at 400h was 48.6%.Pure products were gained by silicic acid column chromatography and Small Unilamellar Vesicles(SUV) were prepared by ultra_sonication at the rate of L_2PC,CHOL:L_2_PE(7∶2∶1 molar ratio) with 10% Lac_PE.Results:The incorporation rate of L_2_PC was 99.6%.The findings of 48_hour cytotoxity experiment suggested that the killing effects of lactolipid ADM Liposomes on human hepatic carcinoma cells were much better than that of non_glycolipid Liposomes(P<0.01).As it was counted as IC 50 ,the killing effects of lactolipid Liposomes were 16.3 times as much as that of the control group.while the killing effects of both on non_target cells(B 16 melanoma cells) were almost same.The results of 0.5hour pretreatment assay demonstrated that lactolipid ADM Liposomes still maintained high killing effects on hepatic carcinoma cells after the contacting time between medicine and hepatic carcinoma cells was shortened,IC 50 was 2.74μg/ml while the control group was 48.7μg/ml.Conclusion:Antitumour activity of lactolipid ADM Liposomes on hepatic carcinoma cells line SMMC-7721 in vitro was due to specific killing effects of gametocyte of galactose group on cancerous cells and the endocytosis of hepatic lectin on human hepatic carcinoma cells. [
出处
《开封医专学报》
2000年第3期6-8,共3页
Journal of Henan University(Medical Science)
关键词
乳糖酰磷脂酰乙醇胺
脂质体
肝癌
阿霉素
lactosylphosphatidylethanolamine(Lac_PE)
Liposome
heptic lectin,hepatic carcinorna cell line SMMC- *'7721
