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Radiosensitizing Effect of Schinifoline from Zanthoxylum schinifolium Sieb et Zucc on Human Non-Small Cell Lung Cancer A549 Cells: A Preliminary in Vitro Investigation

1
China CDC Key Laboratory of Radiological Protection and Nuclear Emergency, National Institute for Radiological Protection, Chinese Center for Disease Control and Prevention, Beijing 100088, China
2
State Key Laboratory of Earth Surface Processes and Resource Ecology, Beijing Normal University, Beijing 100875, China
*
Author to whom correspondence should be addressed.
Molecules 2014, 19(12), 20128-20138; https://doi.org/10.3390/molecules191220128
Received: 23 October 2014 / Revised: 17 November 2014 / Accepted: 26 November 2014 / Published: 1 December 2014
(This article belongs to the Section Medicinal Chemistry)
Schinifoline (SF), a 4-quinolinone derivative, was found in Zanthoxylum schinifolium for the first time. 4-Quinolinone moieties are thought to have cytotoxic activity and are often used as a tubulin polymerization inhibitors, heterogeneous enzyme inhibitors and antiplatelet agents. However, very little information respect to radiosensitization has focused on SF. This work aimed to investigate the radiosensitizing effect of SF on A549 cells. The cell viability results indicated cytotoxicity of SF on A549 cells, with IC50 values of 33.7 ± 2.4, 21.9 ± 1.9 and 16.8 ± 2.2 μg/mL, respectively, after 6, 12, 24 h treatment with different concentrations, and the 10% or 20% IC50 concentration during 12 h was applied in later experiments. The results of cell proliferative inhibition and clonogenic assay showed that SF enhanced the radiosensitivity of A549 cells when applied before 60Co γ-irradiation and this effect was mainly time and concentration dependent. The flow cytometric data indicated that SF treatment before the irradiation increased the G2/M phase, thus improving the radiosensitivity of A549, leading to cell apoptosis. This paper is the first study that describes the in vitro radiosensitising, cell cycle and apoptotic-inducing effects of schinifoline. View Full-Text
Keywords: schinifoline; Zanthoxylum schinifolium; radiosensitization; A549; apoptosis; cytofluorimetry schinifoline; Zanthoxylum schinifolium; radiosensitization; A549; apoptosis; cytofluorimetry
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Wang, C.-F.; Fan, L.; Tian, M.; Qi, X.-S.; Liu, J.-X.; Feng, J.-B.; Du, S.-S.; Su, X.; Wang, Y.-Y. Radiosensitizing Effect of Schinifoline from Zanthoxylum schinifolium Sieb et Zucc on Human Non-Small Cell Lung Cancer A549 Cells: A Preliminary in Vitro Investigation. Molecules 2014, 19, 20128-20138.

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