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Molecules 2016, 21(3), 356; doi:10.3390/molecules21030356

Isoquercitrin Inhibits Hydrogen Peroxide-Induced Apoptosis of EA.hy926 Cells via the PI3K/Akt/GSK3β Signaling Pathway

1
Department of Pharmacy Shanxi, College of Traditional Chinese Medicine, No. 121 University Avenue, Taiyuan 030619, China
2
Shanxi Province Academy of Traditional Chinese Medicine, No. 46 Bingzhou West Road, Taiyuan 030012, China
3
School of Pharmaceutical Science, Shanxi Medical University, No. 56 Xinjian South Road, Taiyuan 030001, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Maurizio Battino
Received: 23 January 2016 / Revised: 1 March 2016 / Accepted: 9 March 2016 / Published: 21 March 2016
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Oxidative stress plays a critical role in endothelial injury and the pathogenesis of diverse cardiovascular diseases, including atherosclerosis. Isoquercitrin (quercetin-3-glucoside), a flavonoid distributed widely in plants, exhibits many biological activities, including anti-allergic, anti-viral, anti-inflammatory, and anti-oxidative effects. In the present study, the inhibitory effect of isoquercitrin on H2O2-induced apoptosis of EA.hy926 cells was evaluated. MTT assays showed that isoquercitrin significantly inhibited H2O2-induced loss of viability in EA.hy926 cells. Hoechst33342/PI and Annexin V-FITC/PI fluorescent double staining indicated that isoquercitrin inhibited H2O2-induced apoptosis of EA.hy926 cells. Western blotting demonstrated that isoquercitrin prevented H2O2-induced increases in cleaved caspase-9 and cleaved caspase-3 expression, while increasing expression of anti-apoptotic protein Mcl-1. Additionally, isoquercitrin significantly increased the expression of p-Akt and p-GSK3β in a dose-dependent manner in EA.hy926 cells. LY294002, a PI3K/Akt inhibitor, inhibited isoquercitrin-induced GSK3β phosphorylation and increase of Mcl-1 expression, which indicated that regulation of isoquercitrin on Mcl-1 expression was likely related to the modulation of Akt activation. These results demonstrated that the anti-apoptotic effect of isoquercitrin on H2O2-induced EA.hy926 cells was likely associated with the regulation of isoquercitrin on Akt/GSK3β signaling pathway and that isoquercitrin could be used clinically to interfere with the progression of endothelial injury-associated cardiovascular disease. View Full-Text
Keywords: isoquercitrin; EA.hy926 cells; apoptosis; oxidative stress; PI3K/Akt/GSK3β isoquercitrin; EA.hy926 cells; apoptosis; oxidative stress; PI3K/Akt/GSK3β
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MDPI and ACS Style

Zhu, M.; Li, J.; Wang, K.; Hao, X.; Ge, R.; Li, Q. Isoquercitrin Inhibits Hydrogen Peroxide-Induced Apoptosis of EA.hy926 Cells via the PI3K/Akt/GSK3β Signaling Pathway. Molecules 2016, 21, 356.

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