In vitro antitumor effect of cucurbitacin E on human lung cancer cell line and its molecular mechanism

文献类型： 外文期刊

第一作者： Jing Si-Yuan

作者： Jing Si-Yuan;Wu Zi-Dan;Zhang Tie-Hua;Zhang Jie;Wei Zheng-Yi

作者机构：

关键词： Cucurbitacin E; Antitumor effect; Lung cancer cell; Apoptosis; Cell cycle arrest

期刊名称：CHINESE JOURNAL OF NATURAL MEDICINES （ 影响因子：3.0； 五年影响因子：2.869 ）

ISSN： 2095-6975

年卷期： 2020 年 18 卷 7 期

页码：

收录情况： SCI

摘要： Cucurbitacin E (CuE) is previously reported to exhibit antitumor effect by several means. In this study, CuE acted as a tyrosine kinase inhibitor interfering with the epidermal growth factor receptor/mitogen-activated protein kinase (EGFR/MAPK) signaling pathway and subsequently induced apoptosis and cell cycle arrest in non-small-cell lung cancer (NSCLC) cell line A549. The apoptosis regulators, cleaved Caspases-3 and Caspases-9, were observed to be increased with the treatment of CuE. The activated transcription factor STAT3 and the apoptosis inhibitor protein survivin were also observed to be reduced. The cell cycle regulators, CyclinA2, cylinB1, CyclinD1 and CyclinE, were also investigated and the results suggested that the cell cycle was arrested at GI/GO phase. Treatment of CuE also altered the existence status of most of the participants in the EGFR/MAPK signaling. Phosphorylation of EGFR enhanced significantly, leading to the alteration of members downstream, either total amount or phosphorylation level, notably, MEK1/2 and ERK1/2. Moreover, the results of molecular simulation brought an insight on the interaction mechanism between CuE and EGFR. In summary, CuE exhibited anti-proliferative effect against A549 cells by targeting the EGFR/MAPK signaling pathway.

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