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目的:以酯键链接增强基团,制备姜黄素前体,观察其对前列腺癌细胞和正常二倍体细胞生长活性影响的差异。方法:叔丁氧羰基(Boc)-苯丙氨酸酯姜黄素单酯(BPC)作用于人前列腺癌DU-145细胞6～24 h后,MTT试验检测细胞生长活性,流式细胞术检测细胞凋亡率。计数法测定1～7天细胞生长曲线。人主动脉平滑肌(people aortic smooth muscle cells,HASMC)细胞作为对照组。结果:10～40μmol/L的BPC作用于DU-145细胞6～24 h后,DU-145细胞生长抑制率为7.37%～66.87%(P<0.05),呈浓度﹑时间依赖性;部分细胞出现凋亡形态学改变,FSC-SSC散点图可见24 h DU-145细胞凋亡比率为37.84%～47.12%(P<0.05)。对照组HASMC细胞凋亡比率为0.94%～4.23%(P<0.05),较同浓度姜黄素降低。结论:BPC能在体外有效诱导人前列腺癌DU-145细胞凋亡,对正常二倍体细胞的抑制作用较低,为深入研究泌尿系肿瘤靶向性治疗提供了新的途径。
OBJECTIVE: To synthesize curcumin precursors by ester linkages, and observe the effect on the growth of prostate cancer cells and normal diploid cells. METHODS: Boc-poly (phenylalanine) curcumin monoester (BPC) was applied to human prostate cancer DU-145 cells for 6-24 h. MTT assay was used to detect cell growth activity. Flow cytometry Apoptosis rate. Counting method for measuring cell growth curve from 1 to 7 days. Human aortic smooth muscle cells (HASMC) were used as the control group. Results: The DU-145 cell growth inhibition rate was 7.37% ~ 66.87% (P <0.05) after treated with 10 ~ 40μmol / L BPC for 6 ~ 24 h in a dose-and time-dependent manner. Some cells appeared The morphological changes of apoptosis showed that the percentage of apoptotic cells in DU-145 cells was 37.84% -47.12% (P <0.05) on the FSC-SSC scattergram. The apoptosis ratio of HASMC in control group was 0.94% -4.23% (P <0.05), which was lower than that of curcumin at the same concentration. CONCLUSION: BPC can effectively induce the apoptosis of human prostate cancer DU-145 cells in vitro and has a low inhibitory effect on normal diploid cells, providing a new way for further research on targeted therapy of urinary tumors.