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General Physiology and Biophysics Vol.36, No.1, p.31–39, 2017 |
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Title: Esculetin exerts anti-proliferative effects against non-small-cell lung carcinoma by suppressing specificity protein 1 in vitro | ||
Author: Ra H. Lee, Young-Joo Jeon, Jin H. Cho, Jeong-Yun Jang, Il-Keun Kong, Seok-Ho Kim, MinSeok S. Kim, Hak-Jae Chung, Keon B. Oh, Seon-Min Park, Jae-Cheon Shin, Jae-Min Seo, Sungho Ko, Jung-Hyun Shim, Jung-Il Chae | ||
Abstract: Esculetin, a coumarin derivative, is a phenolic compound isolated from Artemisia capillaris, Citrus limonia, and Euphorbia lathyris. Although it has been reported to have anti-inflammatory, anti-oxidant, and anti-proliferative activities in several human cancers, its anti-proliferative activity against non-small-cell lung carcinoma (NSCLC) and the molecular mechanisms involved have not been adequately elucidated. In this study, we used two NSCLC cell lines (NCI-H358 and NCI-H1299) to investigate the anti-proliferative activity and apoptotic effect of esculetin. Our data showed that esculetin-treated cells exhibited reduced proliferation and apoptotic cell morphologies. Intriguingly, the transcription factor specificity protein 1 (Sp1) was significantly suppressed by esculetin in a dose- and time-dependent manner. Furthermore, the levels of p27 and p21, two key regulators of the cell cycle, were up-regulated by the esculetin-mediated down-regulation of Sp1; the level of a third cell-cycle regulator, survivin, was decreased, resulting in caspase-dependent apoptosis. Therefore, we conclude that esculetin could be a potent anti-proliferative agent in patients with NSCLC. |
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Keywords: Apoptosis — Esculetin — Non-small-cell lung carcinoma — Specificity protein 1 | ||
Published online: 28-Dec-2016 | ||
Year: 2017, Volume: 36, Issue: 1 | Page From: 31, Page To: 39 | |
doi:10.4149/gpb_2016024 |
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