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龙胆苦苷通过诱导细胞周期停滞、线粒体介导的凋亡以及抑制细胞迁移,对人卵巢癌细胞(SKOV3)发挥出令人信服的抗肿瘤作用。

Gentiopicroside exerts convincing antitumor effects in human ovarian carcinoma cells (SKOV3) by inducing cell cycle arrest, mitochondrial mediated apoptosis and inhibition of cell migration.

作者信息

Li Xiaohao, Yang Chenglin, Shen Hao

机构信息

Department of Gynaecology, The People's Hospital of Tongzhou District, Nantong City, Nantong, Jiangsu, 226300, China.

出版信息

J BUON. 2019 Jan-Feb;24(1):280-284.

PMID:30941981
Abstract

PURPOSE

Gentiopicroside is an important plant secondary metabolite and has been reported to exhibit tremendous pharmacological potential. In the present study we investigated the anticancer effects of gentiopicroside against ovarian SKOV3 cancer cells.

METHODS

Anticancer effects were determined by MTT assay. Apoptosis was investigated by DAPI and annexin V/propidium iodide (PI) double staining. Mitochondrial membrane potential (MMP) determination and cell cycle analysis were carried out by flow cytometry. Protein expression was examined by western blotting.

RESULTS

The results showed that gentiopicroside exerted anticancer effects on SKOV3 cancer cells in a dose-dependent manner. The IC50 of gentiopicroside was 20 µM against the SKOV3 cancer cells. The anticancer effects were mainly found to be due to loss of MMP and induction of apoptosis. The Bax/Bcl-2 expression ratio was also altered upon gentiopicroside treatment. Furthermore, gentiopicroside could arrest the SKOV3 cells in G2/M phase of the cell cycle and prevent their migration and invasion.

CONCLUSIONS

These results indicate that gentiopicroside could prove a potential lead molecule in the treatment and management of ovarian cancer.

摘要

目的

龙胆苦苷是一种重要的植物次生代谢产物,据报道具有巨大的药理潜力。在本研究中,我们研究了龙胆苦苷对卵巢SKOV3癌细胞的抗癌作用。

方法

通过MTT法测定抗癌作用。通过DAPI和膜联蛋白V/碘化丙啶(PI)双重染色研究细胞凋亡。通过流式细胞术进行线粒体膜电位(MMP)测定和细胞周期分析。通过蛋白质印迹法检测蛋白质表达。

结果

结果表明,龙胆苦苷对SKOV3癌细胞具有剂量依赖性的抗癌作用。龙胆苦苷对SKOV3癌细胞的IC50为20μM。发现抗癌作用主要是由于MMP丧失和细胞凋亡诱导。在龙胆苦苷处理后,Bax/Bcl-2表达比率也发生了改变。此外,龙胆苦苷可使SKOV3细胞停滞在细胞周期的G2/M期,并阻止其迁移和侵袭。

结论

这些结果表明,龙胆苦苷可能是治疗和管理卵巢癌的潜在先导分子。

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