Xanthohumol inhibits the extracellular signal regulated kinase (ERK) signalling pathway and suppresses cell growth of lung adenocarcinoma cells
作者： Adrianna Sławińska-Brych , Barbara Zdzisińska , Magdalena Dmoszyńska-Graniczka , Witold Jeleniewicz , Jacek Kurzepa
DOI: 10.1016/J.TOX.2016.06.008
关键词: Xanthohumol 、 Downregulation and upregulation 、 Cyclin D1 、 Cell biology 、 Cell cycle 、 Biology 、 Cell growth 、 Kinase 、 Cancer cell 、 Cancer research 、 MAPK/ERK pathway
摘要: Aberrant activation of the Ras/MEK/ERK signaling pathway has been frequently observed in non-small-cell lung carcinoma (NSCLC) and its important role cancer progression malignant transformation documented. Hence, ERK1/2 kinase cascade becomes a potential molecular target treatment. Xanthohumol (XN, prenylated chalcone derived from hope cones) is known to possess broad spectrum chemopreventive anticancer activities. In our studies, MTT BrdU assays revealed that XN demonstrated greater antiproliferative activity against A549 adenocarcinoma cells than H1563 cell line. We was able suppress activities p90RSK kinases, followed by inhibition phosphorylation CREB protein. Additionally, treatment caused upregulation key cycle regulators p53 p21 as well downregulation cyclin D1. As result, cytotoxic effect attributed arrest at G1 phase induction apoptosis indicated increased caspase-3 activity. Thus, might be promising drug candidate carcinomas.
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