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黄芩素抑制非小细胞肺癌细胞增殖、侵袭和 Notch 信号通路。

Baicalein suppresses non small cell lung cancer cell proliferation, invasion and Notch signaling pathway.

机构信息

Department of Thoracic Surgery, the Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan 250014, Shandong, China.

Department of Pharmacy, Qilu Hospital of Shandong University, Jinan 250012, Shandong, China.

出版信息

Cancer Biomark. 2018;22(1):13-18. doi: 10.3233/CBM-170673.

Abstract

BACKGROUND

Baicalein is an important Chinese herbal medicine and has multiple pharmacological activities. However, the biological mechanisms of the anti-tumor effects of Baicalein on non small cell lung cancer (NSCLC) still need to be understood.

METHODS

Human NSCLC A549 and H1299 cells were pretreated with Baicalein or DMSO. Cells viability and transwell cell invasion assays were performed to assess cell proliferation and invasion. QRT-PCR assay was used to analyze mRNA expression levels of Twist1, E-cadhertin, Vimentin, Notch1 and hes-1. Western blot analysis was also performed to determine protein expression.

RESULTS

In the study, we found that Baicalein had a significantly inhibited effect on proliferation ability of A549 and H1299 cells. Cells treated with Baicalein showed a down-regulated expression of CyclinD1 and CDK1 in A549 and H1299 cells. Furthermore, we found that Baicalein significantly inhibited cell invasion and Epithelial-Mesenchymal Transition (EMT) by up-regulating the mRNA and protein expression of E-cadherin and down-regulated the Twist1 and Vimentin expression, Moreover, Treatment of Baicalein down-regulated Notch1 and hes-1 expression in A549 and H1299 cells, which indicated that Baicalein could suppress the Notch signaling pathway.

CONCLUSION

Our studies suggest that Baicalein may be a potential phytochemical flavonoid for therapeutics of NSCLC and serve as a molecular target for NSCLC.

摘要

背景

黄芩素是一种重要的中草药,具有多种药理活性。然而,黄芩素对非小细胞肺癌(NSCLC)的抗肿瘤作用的生物学机制仍需要进一步了解。

方法

用黄芩素或 DMSO 预处理人 NSCLC A549 和 H1299 细胞。通过细胞活力和 Transwell 细胞侵袭实验评估细胞增殖和侵袭。采用 QRT-PCR 分析 Twist1、E-cadhertin、Vimentin、Notch1 和 hes-1 的 mRNA 表达水平。还进行了 Western blot 分析以确定蛋白质表达。

结果

在这项研究中,我们发现黄芩素对 A549 和 H1299 细胞的增殖能力有明显的抑制作用。黄芩素处理的细胞中 A549 和 H1299 细胞中的 CyclinD1 和 CDK1 表达下调。此外,我们发现黄芩素通过上调 E-cadherin 的 mRNA 和蛋白表达,显著抑制细胞侵袭和上皮-间充质转化(EMT),而下调 Twist1 和 Vimentin 的表达。此外,黄芩素处理下调了 A549 和 H1299 细胞中 Notch1 和 hes-1 的表达,表明黄芩素可以抑制 Notch 信号通路。

结论

我们的研究表明,黄芩素可能是治疗 NSCLC 的潜在植物化学类黄酮,并可作为 NSCLC 的分子靶点。

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