摘要
目的制备赖氨熊果酸并探讨其增溶作用及对肝癌Bel7402细胞增殖的抑制作用。方法采用共研磨法制备赖氨熊果酸,采用粉末X射线衍射法(PXRD)、红外光谱(IR)法对赖氨熊果酸进行表征,采用高效液相色谱法(HPLC)测定赖氨熊果酸的增溶作用,采用噻唑蓝(MTT)法观察赖氨熊果酸对肝癌Bel7402细胞增殖的抑制效果。结果共研磨法制备赖氨熊果酸得率为95.2%,纯度为98.2%,赖氨熊果酸的溶解度为49.69μg/m L,明显高于赖氨酸-熊果酸物理混合物在水中的溶解度1.87μg/m L;赖氨熊果酸对肝癌Bel7402细胞增殖的抑制作用明显增强,在浓度10、20μmol/L时,与相同浓度5-FU(阳性对照)比较,赖氨熊果酸对肝癌Bel7402细胞的抑制作用差异无统计学意义(P>0.05)。结论赖氨熊果酸增溶作用明显,对肝癌细胞增殖具有明显抑制作用,作为新一代高效低毒的抗肿瘤药物具有一定开发价值。
Objective To prepare and characterize ursolic acid lysinate, and to study the antitumor effect of ursolic acid lysinate on human hepatoma cell line Bel7402. Methods Ursolic acid lysinate was prepared by co-grinding 1： 1 molar mixture of ursolic acid and lysine for 12 hours. Characterization of ursolic acid lysinate was achieved by powder X-ray diffraction and infrared spectroscopy techniques. High performance liquid chromatography （HPLC）method was used to study the solubilization of ursolic acid lysinate. The 3-（ 4, 5-dimethylthiazol-2-yl ）-2,5-diphenyltetrazolium bromide （MTT） method was used to assay the antitumor activity of ursolic acid lysinate. Results The solubility of ursolic acid lysinate was improved significantly as compared to ursolic acid in water. The antitumor activity on human hepatoma cell line Bel7402 of ursolic acid lysinate was enhanced significantly than that of ursolic acid. Conclusion The water solubility and antitumor effect on human hepatoma cell line of ursolic acid lysinate may be potentially useful for its application as a new pharmaceutical formulation in cancer treatment in the future.
出处
《中国公共卫生》
CAS
CSCD
北大核心
2016年第10期1322-1325,共4页
Chinese Journal of Public Health
基金
北京市教育委员会科技发展计划面上项目(KM200910025014)
首都医科大学燕京医学院科研启动基金(2015)
