Esculetin exerts anti-proliferative effects against non-small-cell lung carcinoma by suppressing specificity protein 1 in vitro

Autor: Il-Keun Kong, Minseok Kim, Ko Sungho, Jung-Hyun Shim, Jae-Cheon Shin, Young Joo Jeon, Ra Ham Lee, Jeong-Yun Jang, Seon-Min Park, Jung-Il Chae, Seokho Kim, Hak-Jae Chung, Keon Bong Oh, Jae-Min Seo, Jin H Cho
Rok vydání: 2016
Předmět:
Zdroj: General physiology and biophysics. 36(1)
ISSN: 0231-5882
Popis: 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.
Databáze: OpenAIRE