| 姜胜男,朱欣婷,刘 云,李三华,雷欣睿,晏 容,李晓飞.三种去甲基斑蝥素衍生物体外对人肝癌HepG-2细胞增殖的抑制作用[J].,2017,17(20):3831-3835 |
| 三种去甲基斑蝥素衍生物体外对人肝癌HepG-2细胞增殖的抑制作用 |
| Inhibitory Effect of Three Norcantharidin Derivativeson HepG-2 Cells in Vitro |
| 投稿时间：2016-12-29 修订日期：2017-01-25 |
| DOI：10.13241/j.cnki.pmb.2017.20.007 |
| 中文关键词: 去甲基斑蝥素酸钠 去甲基斑蝥素酸钾 去甲基斑蝥素酸钙 人肝癌HepG-2细胞 抑制作用 |
| 英文关键词: Sodium Norcantharidate Potassium Norcantharidate Calcium Norcantharidate Human hepatocellular carcinoma HepG-2 cells Inhibitory effect |
| 基金项目:国家自然科学基金项目（81260488, 81660611）；贵州省科技合作计划项目（黔科合LH字[2015]7516号，黔科合LH字[2015]7509号）；贵州省卫计委科学基金项目（gzwjk2015-1-013）；贵州省教育厅特色重点实验室建设项目（黔教合KY字[2014]212)；贵州省遵义市汇川区科技计划项目（遵汇科合201630） |
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| 中文摘要: |
| 摘要 目的：探讨去甲基斑蝥素酸钠、去甲基斑蝥素酸钾、去甲基斑蝥素酸钙体外对人肝癌HepG-2细胞增殖的影响。方法：采用磺酰罗丹明（SRB法）、细胞集落形成实验、流式细胞技术检测三种去甲基斑蝥素衍生物对HepG-2细胞增殖和凋亡的影响。qRT-PCR技术考察三种去甲基斑蝥素衍生物对HepG-2细胞Bcl-2、Bax mRNA表达的影响。结果：三种去甲基斑蝥素衍生物能明显抑制HepG-2细胞的增殖，其抑制率呈剂量时效依赖性；与空白对照组相比，三种去甲基斑蝥素衍生物能显著性减少HepG-2细胞集落形成数量，并且可诱导HepG-2细胞的凋亡，凋亡率分别为8±0.56%、6.93±0.91%、6.16±0.37%；qRT-PCR显示，三种去甲基斑蝥素衍生物能抑制HepG-2细胞Bcl-2mRNA的表达，增强Bax mRNA的表达。结论：三种去甲基斑蝥素衍生物可通过下调Bcl-2 mRNA表达，上调Bax mRNA表达，诱导HepG-2细胞的凋亡，从而抑制HepG-2细胞的增殖；三种衍生物中，去甲基斑蝥素酸钠对HepG-2细胞的增殖的抑制作用最强。 |
| 英文摘要: |
| ABSTRACT Objective: To explore the inhibitory effect of three norcantharidin derivatives which were named sodium norcantharidate, potassium norcantharidate and calcium norcantharidate on human hepatocellular carcinoma HepG-2 cells. Methods: The effect of three norcantharidate derivatives on HepG-2 cells proliferation was assessed with SRB assay. The cell colony forming experiment test was adopted to observe the impact of derivatives on colony formation ability of HepG-2 cells. The flow cytometry was used to examine the effect on HepG-2 cellsapoptosis, and mRNA levels of Bcl-2 and Bax were measured with RT-qPCR. Results: Three norcantharidate derivatives inhibited the proliferation of HepG-2 cells with a time and dose dependent relation. Compared with the blank control group, derivatives were able to obviously inhibit cell colony formation and induce apoptosis of HepG-2 cells. The apoptosis rate were 8±0.56%, 6.93±0.91%, 6.16±0.37%, respectively. Base on the results of RT-qPCR, three norcantharidate derivatives had the ability to reduce the mRNA levels of Bcl-2 and improve the mRNA levels of Bax. Conclusion: The three kinds of norcantharidate derivatives could inhibit the proliferation and induce apoptosis of HepG-2 cells which involve in down-regulating the mRNA levels of Bcl-2 and up-regulating the mRNA levels of Bax. Among three derivatives, sodium cantharidinate shows the strongest inhibitory activity on HepG-2 cells. |
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