青蒿素增敏复方抑制肿瘤细胞增殖及延缓荷瘤裸鼠移植肿瘤生长的研究

Studies on Artemisinin Sensitizing Compound in Inhibiting Tumor Cell Proliferation and Suppressing Transplanted Tumor Growth in Tumor-bearing Nude Mice

【目的】提高青蒿素抗肿瘤效率,阐明青蒿素增敏复方的抑瘤增敏机理。【方法】采用四甲基偶氮唑盐(MTT)法测定各药物对人肝癌细胞株HepG2细胞的生长抑制率;经皮下接种HepG2细胞进行荷瘤裸鼠造模,测定给药15 d后瘤体质量,计算抑瘤率。【结果】青蒿琥酯配伍马来酸二乙酯、巯基琥珀酸和氨基三唑后,肿瘤细胞的生长抑制率较相同浓度的青蒿琥酯单方高43.84%,抑瘤率较青蒿琥酯单方提高近3倍。HepG2细胞中抗氧化剂含量及抗氧化酶活性测定结果表明,空白组的测定值均高于单方组和复方组,而复方组的测定值低于单方组。【结论】青蒿素增敏复方可能通过降低抗氧化剂含量及抑制抗氧化酶活性发挥抗肿瘤增敏作用。

Objective To enhance the anti-tumor efficiency of artemisinin and to explore the anti-tumor and sensitivity-enhancing mechanism of Artemisinin Sensitizing Compound（ASC）.Methods The growth-inhibition rate of HepG2 cells was determined by methyl thiazolyl tetrazolium（MTT） method.Tumor-bearing nude mice were given inoculation of HepG2 cells subcutaneously.After treatment for 15 days,the tumor-inhibition rate was calculated according to the tumor mass weight.Results The growth-inhibition rate of tumor cells in ASC group（artesunate combined with diethyl maleate,mercaptosuccinic acid and aminotriazole）,was increased 43.84%,and the tumor-inhibition rate was three times as much as that in artesunate alone group with the same titer.The amount of antioxidant agents and the activity of antioxidant enzymes were higher in the control group than those in the artesunate alone group and ASC group,while were lower in ASC group than those in the artesunate alone group.Conclusion ASC has anti-tumor and sensitivity-enhancing effect through decreasing the amount of anti-oxidant agents and inhibiting activities of anti-oxidant enzymes.