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探讨化合物肉桂酰胺格尔德霉素(CDG)的体内外抗肿瘤活性。采用MTT法检测肿瘤细胞增殖,免疫荧光法和Annexin V-FITC/PI双染法检测肿瘤细胞凋亡,Transwell法检测肿瘤细胞迁移能力,Western blotting法检测肿瘤细胞中RAF-1、EGFR、AKT、CDK4、HER-2蛋白水平。使用异种移植瘤裸鼠模型检测CDG对人乳腺癌MCF-7细胞的生长抑制作用。结果表明:CDG对不同肿瘤细胞增殖具有抑制作用,IC50为13.6~67.4μg·mL 1;CDG能够诱导肿瘤细胞凋亡,引起多种细胞形态学改变;同时,CDG还可降低肿瘤细胞迁移能力,减少RAF-1、EGFR、AKT、CDK4、HER-2蛋白水平;体内实验结果显示,CDG毒性明显低于格尔德霉素(GDM),并且能够抑制人乳腺癌MCF-7裸鼠移植瘤生长。
To investigate the antitumor activity of compound cinnamide geldanamycin (CDG) in vitro and in vivo. Tumor cell proliferation was detected by MTT assay. Apoptosis of tumor cells was detected by immunofluorescence and Annexin V-FITC / PI double staining. Transwell assay was used to detect the migration of tumor cells. The expressions of RAF-1, EGFR, AKT, CDK4, HER-2 protein levels. The growth inhibition of CDG on human breast cancer MCF-7 cells was examined using a xenografted nude mouse model. The results showed that: CDG can inhibit the proliferation of different tumor cells with the IC50 of 13.6 ~ 67.4μg · mL 1; CDG can induce apoptosis of tumor cells, causing a variety of cell morphological changes; the same time, CDG can also reduce tumor cell migration, Reduce the levels of RAF-1, EGFR, AKT, CDK4 and HER-2 protein in vivo. The results of in vivo experiments showed that CDG toxicity was significantly lower than that of geldanamycin (GDM) and inhibited the growth of human breast cancer MCF- .