酯键链接增韧基团增强姜黄素对肿瘤细胞靶向性作用
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国家自然科学基金(30860284),贵阳市科学技术攻关项目(2009筑科农合同字第3-009号)资助


The effect of toughening genes with ester key on targeting to tumor cells of curcumin
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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:10~40 μmol/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-

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    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.

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任德帅,陈方敏,石家齐,严 波,汤 磊,杨 燕,常傲霜,李登宝,肖 锋.酯键链接增韧基团增强姜黄素对肿瘤细胞靶向性作用[J].南京医科大学学报(自然科学版),2011,(10):1403-1406

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  • 收稿日期:2011-05-08
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