摘要
目的：合成ｎ十六烷酰１硫代βＤ半乳糖苷（ＣｅｔｙｌＧａｌ），并用其修饰阿霉素脂质体表面，观察体外对人肝癌细胞系ＳＭＭＣ７７２１的杀伤作用。方法：半乳糖经化学反应制备ＣｅｔｙｌＧａｌ，用１０％摩尔的糖脂整合到超声法制备的小单层阿霉素脂质体脂膜上进行体外杀瘤研究，ＭＴＴ法检测杀瘤活性。结果：４８小时细胞毒试验糖脂阿霉素脂质体对人肝癌细胞系ＳＭＭＣ７７２１的杀伤作用优于无糖脂阿霉素脂质体（Ｐ＜００５），而对非靶细胞（Ｂ１６黑色素瘤细胞）的杀伤作用糖脂和无糖脂阿霉素脂质体两者相近。０５ｈ预处理实验表明：缩短药物与细胞接触时间后，糖脂阿霉素脂质体仍保持较强的杀伤肝癌细胞作用。结论：半乳糖阿霉素脂质体对人肝癌细胞杀伤作用较无糖脂组及非靶细胞组为强。
Objective: To study the antitumor activity of neogalactolipidmodified
adriamycin(ADM) liposomes on SMMC7721 in vitro.Method:nCetyl1thioDgalactoside(Cetylgal)
was synthesized by a series of reaction from galactose and incorporated into Small Unilamellar
Vesicles(SUV) which was prepared by sonication at the ratio of LPC:Chol:LPE(721 molar ratio)
with or without 10 mol%Cetylgal. Cytotoxicity assay on SMMC7721 in vitro was performed.
Results: Results of 48h cytotoxicity assay with MTT method showed that specific cytotoxicity of
galactolipid groups to SMMC7721 were 24 fold more effective than the control nongalactolipid
group, but with very similar cytotoxicity to nontargeted B16 melanoma cells.05h pretreatment
assay demonstrated that cytotoxicity of free ADM on SMMC7721 decreased
remarkably(IC50=789mol/L),but galactolipid ADM liposomes remain higher
activity(IC50=688mol/L) than control nongalactplipid group (IC50>100mol/L) after reducing the
contact time(to 05h) between drugs and cells. Conclusions:Results indicated that cytotoxicity of
galactolipidmodified ADM liposome on SMMC7721 was higher than on nontargeted cell B16
melanoma and higher than nongalactolipid modified ADM liposome and free ADM group were
observed.
出处
《癌症》
SCIE
CAS
CSCD
北大核心
1999年第3期281-284,共4页
Chinese Journal of Cancer
基金
国家自然科学基金
