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太白山乌头中一种新的C19 - 二萜生物碱太白乌头碱A对HepG2人肝癌细胞系的抗肿瘤作用及机制

The antitumor effect and mechanism of taipeinine A, a new C19-diterpenoid alkaloid from Aconitum taipeicum, on the HepG2 human hepatocellular carcinoma cell line.

作者信息

Zhang Hui, Guo Zengjun, Han Ling, You Xiaojuan, Xu Ying

机构信息

School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, China.

出版信息

J BUON. 2014 Jul-Sep;19(3):705-12.

Abstract

PURPOSE

To investigate whether taipeinine A (JNQ2), a C19-diterpenoid alkaloid prepared from the roots of Aconitum taipeicum, has anticancer effects on hepatocellular carcinoma (HCC) and to study its probable anticancer mechanisms.

METHODS

JNQ2 activities were assessed on human HCC cell line (HepG2) by proliferative assay, cell cycle arrest assay, apoptosis analysis, cell invasion assay and Western blot analysis.

RESULTS

The antitumor activity tests showed that JNQ2 inhibited the proliferation of HepG2 cells in a dose- and time-dependent manner and blocked the cell cycle at the G1/S phase. High dosage of JNQ2 induced significant apoptosis of tumor cells. The invasiveness of HepG2 cells was also inhibited by JNQ2. The mechanism of JNQ2 antitumor effect at the molecular level was presumed to be the upregulation of the protein expression of Bax and Caspase-3 and the downregulation of the protein expression of Bcl-2 and CCND1.

CONCLUSION

Our study suggests that JNQ2 has anticancer effects on HepG2 cells and it is a potential reagent for the treatment of HCC that merits further investigation.

摘要

目的

研究从太白山乌头根中提取的C19 - 二萜生物碱太白乌头碱A(JNQ2)对肝细胞癌(HCC)是否具有抗癌作用,并探讨其可能的抗癌机制。

方法

通过增殖试验、细胞周期阻滞试验、凋亡分析、细胞侵袭试验和蛋白质免疫印迹分析,评估JNQ2对人肝癌细胞系(HepG2)的作用。

结果

抗肿瘤活性试验表明,JNQ2以剂量和时间依赖性方式抑制HepG2细胞的增殖,并将细胞周期阻滞在G1/S期。高剂量的JNQ2诱导肿瘤细胞显著凋亡。JNQ2还抑制了HepG2细胞的侵袭能力。推测JNQ2在分子水平上的抗肿瘤作用机制是上调Bax和Caspase - 3的蛋白表达,下调Bcl - 2和CCND1的蛋白表达。

结论

我们的研究表明,JNQ2对HepG2细胞具有抗癌作用,是一种值得进一步研究的潜在肝癌治疗药物。

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