Lupeol及其衍生／修饰物H2抗肝细胞肝癌作用及其机制的初步研究

目的：探讨lupeol及其结构改造后衍生／修饰物H2抗肝细胞肝癌作用及机制。方法：对lupeol进行化学结构修饰，然后应用MTT方法检测lupeol及其衍生／修饰物H2对HepG2和SMMC7721细胞增殖的作用，流式细胞术检测lupeol、H2对SMMC7721细胞凋亡的诱导作用，Western blot方法检测cleaved—PARP剪切活化水平。结果：MTT数据显示，H2大大提高了luped抗肝细胞肝癌效果。lupeol的IC50为45 μmol／L （SMMC7721）和485μmol／L（HepG2），H2的IC50为30μmol／L（SMMC7721和HepG2）。流式细胞术结果显示，20μmol／LH2作用后诱导SMMC7721细胞发生凋亡。Western blot结果显示，20μmol／LH2作用后诱导SMMC7721细胞内cleaved—PARP剪切活化增多，而20μmol／L lupeol作用后无此效果。结论：lupeol结构改造后的H2，显著提高了其抗肝细胞肝癌活性。

Anti - hepatocellular carcinoma effect of lupeol and its modified compound H2 and the mechanisms

Objectlve：To investigate the anti - hepatocellular carcinoma effect of lupeol arid its modified compound, H2, and the mechanisms. Methods：The structure of lupeol was modified. MTT assay modified compound,H2. Flow cytometry analysis was used to detect the apoptosis induced by lupeol/H2. Western blot analysis was used to detect the expression level of cleaved - PARP protein. Results： MTT result demonstrated that H2 greatly improved the anti - hepatoeellular carcinoma effect of lupeol, IC50 of lupeol were 45μmol/L （for 5MMC7721 ） and 48.5μmol/L （for HepG2） ,while IC50 of H2 was 30μmol/L （for both SMMC7721 and HepG2）. Flow cytometry result showed that 20μmol/L H2 induced apoptosis of SMMC7721 cells,and Western blot results indicated that 20μmol/L H2 increased the expression level of cleaved - PARP in 5MMC7721 cells,whereas 20μmol/L lupeol had little function. Conclusion ： Modified compound of lupeol, H2, significantly improved anti - hepatoeellular carcinoma effect.