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探讨新型环磷酰胺类衍生物4,6-二苯基环磷酰胺(9b)的体内外抗肿瘤活性及其作用机制。体外采用MTT法观察9b对人肝癌细胞株HepG2、人乳腺癌细胞株MCF-7、人白血病细胞株K562的增殖抑制作用;流式细胞仪观察细胞的凋亡率和细胞周期的变化;体内建立肝癌H22荷瘤小鼠模型,观察9b的抑瘤效果。结果表明,9b对体外培养的HepG2、MCF-7、K562细胞有抑制增殖作用,且具有剂量和时间依赖性,9b处理HepG2、MCF-7、K562细胞48 h的IC50分别为32.34、87.07、149.10μmol·L-1;9b使HepG2、MCF-7细胞的G0/G1期细胞和K562细胞的G0/G1和G2/M期细胞明显增加,细胞凋亡率随药物浓度增加亦呈增长趋势;9b对H22实体瘤具有明显的抑制作用。结果提示,9b具有明显的体内外抗肿瘤活性,其抑瘤机制可能与细胞周期改变和诱导肿瘤细胞凋亡相关。
To investigate the antitumor activity and its mechanism of 4-diphenyl cyclophosphamide (9b), a novel cyclophosphamide derivative, in vitro and in vivo. MTT assay was used to observe the inhibitory effect of 9b on the proliferation of human hepatocellular carcinoma cell line HepG2, human breast cancer cell line MCF-7 and human leukemia cell line K562. The changes of cell apoptosis and cell cycle were observed by flow cytometry. Liver cancer H22 tumor-bearing mouse model to observe the inhibitory effect of 9b. The results showed that 9b inhibited the proliferation of HepG2, MCF-7 and K562 cells in a dose-and time-dependent manner. The IC50 of 9b treated HepG2, MCF-7 and K562 cells for 48 h were 32.34, 87.07 and 149.10 9b increased the number of G0 / G1 and G2 / M phases in G0 / G1 phase cells and K562 cells in HepG2 and MCF-7 cells, and the apoptosis rate increased with the increase of drug concentration. 9b H22 solid tumor has obvious inhibitory effect. The results suggest that 9b has obvious anti-tumor activity in vitro and in vivo, and its anti-tumor mechanism may be related to the change of cell cycle and the induction of tumor cell apoptosis.