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Screening of cytotoxic or cytostatic flavonoids with quantitative Fluorescent Ubiquitination-based Cell Cycle Indicator-based cell cycle assay
Young-Hyun Go, 1 Hyo-Ju Lee, 1 Hyeon-Joon Kong, 1 Ho-Chang Jeong, 1 Dong Young Lee, 2 Soon-Ki Hong, 2 Sang Hyun Sung, 2 Ok-Seon Kwon 2 , Hyuk-Jin Cha 2
1  College of Natural Sciences, Department of Life Sciences, Sogang University, Seoul, Republic of Korea
2  College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, Republic of Korea

Published: 19 December 2018 by The Royal Society in Royal Society Open Science
The Royal Society, Volume 5; 10.1098/rsos.181303
Abstract: The Fluorescent Ubiquitination-based Cell Cycle Indicator (FUCCI) system can be used not only to study gene expression at a specific cell cycle stage, but also to monitor cell cycle transitions in real time. In this study, we used a single clone of FUCCI-expressing HeLa cells (FUCCI-HeLa cells) and monitored the cell cycle in individual live cells over time by determining the ratios between red fluorescence (RF) of RFP-Cdt1 and green fluorescence (GF) of GFP-Geminin. Cytotoxic and cytostatic compounds, the latter of which induced G2 or mitotic arrest, were identified based on periodic cycling of the RF/GF and GF/RF ratios in FUCCI-HeLa cells treated with anti-cancer drugs. With this cell cycle monitoring system, ten flavonoids were screened. Of these, apigenin and luteolin, which have a flavone backbone, were cytotoxic, whereas kaempferol, which has a flavonol backbone, was cytostatic and induced G2 arrest. In summary, we developed a system to quantitatively monitor the cell cycle in real time. This system can be used to identify novel compounds that modulate the cell cycle and to investigate structure–activity relationships.
Keywords: SAR, Screening, Cell cycle, flavonoid, G2 Arrest, FUCCI
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