酯键链接增韧基团增强姜黄素对肿瘤细胞靶向性作用

The effect of toughening genes with ester key on targeting to tumor cells of curcumin

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： Produced curcumin＇s precursors with toughen genes with ester key,to observe its different effect on growing cells between prostates＇ and the normal diploid＇s.Methods： Human prostatic cancer DU-145 cells were cultured and incubated with Boc-phenylalanine-curcumin（BPC） for 6-24 h.Cell viability was detected by MTT.Cell apoptosis rate was detected by flow cytometry.DU-145 cells were cultured and incubated with BPC for 1-7 d for cell grow curve detected by counting process.The people aortic smooth muscle cells（HASMC） acted as control.Results： After treatment with 10～40 μmol/L BPC for 6-24 h,the growth inhibition of DU-145 cells was 7.37%～66.87%（P 0.05）,in dose-time-dependent manners.Partial cancer cells presented morph-ological characters of apoptosis,with FSC-SSC scatter diagram.After treatment for 24 h,the cell apoptosis rate was 37.84%～47.12%（P 0.05）.Compared with curcumin of same concentrations,the control group HASMC apoptosis rate was 0.94%～4.23%（P 0.05）.Conclusion： The prodrug of curcumin could induce apoptosis of prostatic cancer DU-145 cells,and reduce the side effects on normal diploid cells.This provided a novel strategy for further exploration of tumor-targeted chemotherapeutic drugs.