新型姜黄素结构衍生物抗肝癌细胞增殖作用的研究

李于博; 文英; 马明亮; 吴良春; 文珂; 赵政

新型姜黄素结构衍生物抗肝癌细胞增殖作用的研究

1.
华东师范大学脑功能基因组学教育部重点实验室,上海市脑功能基因组学重点实验室,药理毒理研究室,上海 200062;
2.
华东师范大学脑功能基因组学教育部重点实验室,上海市脑功能基因组学重点实验室,超分子化学与药物化学研究室,上海 200062

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中图分类号: R962
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出版历程
- 收稿日期: 2011-03-01
- 修回日期: 2011-06-01
- 刊出日期: 2012-05-25

Antiproliferative and apoptotic activities of novel curcumin analogs in human liver cancer cell lines

1.
Division of Pharmacology and Toxicology, Key Laboratory of Brain Functional Genomics, Ministry of Education,Shanghai Key Laboratory of Brain Functional Genomics, East China Normal University, Shanghai 200062, China;
2.
Division of Supermolecular Chemistry and Medicinal Chemistry, Key Laboratory of Brain Functional Genomics, Ministry of Education, Shanghai Key Laboratory of Brain Functional Genomics, East China Normal University, Shanghai 200062, China

摘要

摘要: 采用MTT法对姜黄素结构衍生物（CCM系列化合物）进行抗人肝癌细胞Bel-7402和SMMC-7721活性筛选；利用流式细胞技术和荧光显微镜检测SMMC-7721细胞凋亡及周期分布；采用Western-Blot方法检测SMMC-7721中蛋白caspase-3和剪切后p17的表达.结果表明，化合物CCM-5和CCM-14抗肿瘤活性较好，其对SMMC-7721细胞的凋亡作用呈剂量依赖性，且凋亡率与阴性对照组相比有显著差异（P0.01）；化合物浓度增高时，G0/G1期细胞减少，S期以及G2/M期细胞增加，凋亡峰SubG1峰增大；两个化合物均可增强caspase-3的表达，随着浓度的提高，caspase-3的表达趋势减弱，而剪切形式p17亚基表达量逐渐提高.因此，姜黄素结构衍生物CCM-5和CCM-14能抑制人肝癌细胞SMMC-7721细胞的增殖，促进凋亡，其作用机制可能与化合物诱导caspase-3活性的增强有关.
- 姜黄素结构衍生物 /
- Bel-7402细胞 /
- SMMC-7721细胞 /
- 细胞凋亡 /
- 细胞周期 /
- Caspase-3
Abstract: Antiproliverative and apoptotic activities of the novel curcumin analogs (CCM series) against human liver carcinoma Bal-7402 and SMMC-7721 cells were investigated by MTT assay. The cell cycle distribution and apoptosis of SMMC-7721 cells induced by CCM-5 and CCM-14 were analyzed using flow cytometry. The expressions of caspase-3 and its activated form p17 in SMMC-7721 cells were further determined by western blot. CCM-5 and CCM-14 exhibited, in a concentration-dependent manner, the stronger antiproliferative role than those of curcumin and the other CCM compounds. Their apoptotic effects on the SMMC-7721 cells were also found to be significantly elevated as compared with the control group (P0.01). Cell cycle distribution appeared that, as the concentrations of the compounds increased in SMMC-7721 cells, the G0/G1 phase cells decreased while the S phase and the G2/M phase cells, and the SubG1 peak increased. Furthermore, both CCM-5 and CCM-14 could activate caspase-3 expression in the SMMC-7721 cells. Collectively, our data suggest that CCM-5 and CCM-14 can restrain proliferation and promote apoptosis in SMMC-7721 cell, and the molecular mechanism underlying these actions against the cancer cells of the compounds may involve in the activation of caspase-3.
- curcumin analogs /
- Bel-7402 cells /
- SMMC-7721 cells /
- apoptosis /
- cell cycle /
- caspase-3

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参考文献(1)

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