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巨球壳菌素抑制人肺癌细胞的上皮-间质转化过程。

Gigantol Inhibits Epithelial to Mesenchymal Process in Human Lung Cancer Cells.

作者信息

Unahabhokha Thitita, Chanvorachote Pithi, Sritularak Boonchoo, Kitsongsermthon Jutarat, Pongrakhananon Varisa

机构信息

Cell-Based Drug and Health Product Development Research Unit, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.

Cell-Based Drug and Health Product Development Research Unit, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand; Department of Pharmacology and Physiology, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.

出版信息

Evid Based Complement Alternat Med. 2016;2016:4561674. doi: 10.1155/2016/4561674. Epub 2016 Aug 29.

Abstract

Lung cancer remains a leading public health problem as evidenced by its increasing death rate. The main cause of death in lung cancer patients is cancer metastasis. The metastatic behavior of lung cancer cells becomes enhanced when cancer cells undergo epithelial to mesenchymal transition (EMT). Gigantol, a bibenzyl compound extracted from the Thai orchid, Dendrobium draconis, has been shown to have promising therapeutic potential against cancer cells, which leads to the hypothesis that gigantol may be able to inhibit the fundamental EMT process in cancer cells. This study has demonstrated for the first time that gigantol possesses the ability to suppress EMT in non-small cell lung cancer H460 cells. Western blot analysis has revealed that gigantol attenuates the activity of ATP-dependent tyrosine kinase (AKT), thereby inhibiting the expression of the major EMT transcription factor, Slug, by both decreasing its transcription and increasing its degradation. The inhibitory effects of gigantol on EMT result in a decrease in the level of migration in H460 lung cancer cells. The results of this study emphasize the potential of gigantol for further development against lung cancer metastasis.

摘要

肺癌死亡率不断上升,这表明它仍是一个主要的公共卫生问题。肺癌患者的主要死因是癌症转移。当癌细胞发生上皮-间质转化(EMT)时,肺癌细胞的转移行为会增强。从泰国兰花石斛中提取的联苄化合物巨花远志,已显示出对癌细胞有良好的治疗潜力,这导致了一个假设,即巨花远志可能能够抑制癌细胞中基本的EMT过程。这项研究首次证明,巨花远志具有抑制非小细胞肺癌H460细胞中EMT的能力。蛋白质印迹分析表明,巨花远志减弱了ATP依赖性酪氨酸激酶(AKT)的活性,从而通过减少主要EMT转录因子Slug的转录并增加其降解来抑制其表达。巨花远志对EMT的抑制作用导致H460肺癌细胞迁移水平降低。这项研究的结果强调了巨花远志在对抗肺癌转移方面进一步开发的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/65f9/5019934/7728b8091aae/ECAM2016-4561674.001.jpg

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