单羰基姜黄素类似物抗肿瘤机制研究

Mechanism Study of Mono-carbonyl Curcumin Analogues

目的在前期单羰基姜黄素类似物合成的基础上,对其进行深入的抗肿瘤机理研究。方法通过碘化丙啶(PI)染色和Caspase-3活性检测姜黄素及姜黄素类似物诱导前列腺癌PC-3细胞凋亡。结果姜黄素类似物C8在诱导细胞凋亡方面较姜黄素及其他姜黄素类似物相比有显著的效果,通过Western blot实验,姜黄素类似物C8与对照组及姜黄素组相比可使Akt和Erk1/2显著减少。结论姜黄素类似物C8能够通过抑制Akt和Erk1/2蛋白表达来抑制前列腺癌的细胞增殖,有望成为有潜力的抗癌新药。

Based on the synthesis and anticancer activity research work of Mono-carbonyl curcumin analogues owned by previous studies, we select 8 compounds A5-A8 and C5-C8 for mechanism research, we found C8 had a significant effect in prostate cancer PC-3 cells by trypan blue assay, and the benzyl piperidone-containing compounds studied also stimulated apoptosis in PC-3 cells. Mechanistic studies indicate that the effects of both curcumin and C8 on PC-3 cells were associated with a decrease in phospho-Akt and phospho-Erk1/2. The present study indicates that C8 may have useful effects on human cancer ceils.