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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 the ursolic acid and to investigate its inhibitory effect on the proliferation of Bel7402 hepatocellular carcinoma cells. Methods Laminar ursolic acid was prepared by co-grinding method, and its structure was characterized by powder X-ray diffraction (XRD) and infrared spectroscopy (IR). The levamisole was determined by high performance liquid chromatography (HPLC) The effect of lysine ursolic acid on the proliferation of Bel7402 cells was observed by MTT assay. Results The total yield of rapeseed ursolic acid was 95.2% and the purity was 98.2%. The solubility of ramin ursolic acid was 49.69μg / m L, which was significantly higher than that of the lysine-ursolic acid physical mixture in water Solubility 1.87μg / m L; Ursolic acid on the proliferation of Bel7402 cells significantly inhibited the proliferation, at the concentration of 10,20μmol / L, with the same concentration of 5-FU (positive control), lysine ursolic acid The inhibitory effect of Bel7402 cells was not statistically significant (P> 0.05). CONCLUSION: Ursolic acid solubilizes obviously and has obvious inhibitory effect on the proliferation of hepatocellular carcinoma cells. It has certain development value as a new generation of anti-tumor drugs with high efficiency and low toxicity.