<abstract xmlns="http://www.w3.org/1999/xhtml"> Expression of a drug and xenobiotic metabolizing enzymes, cytochrome P450s (CYPs), and antioxidant enzymes can be modulated by various factors. The flavonoid rutin was investigated for its anti-carcinogen and protective effects as well as modulatory action on CYPs and phase II enzymes in human hepatocellular carcinoma cells. Rutin inhibited proliferation of HEPG2 cells in a dose-dependent manner with the IC50 value of 52.7 μmol L-1 and invasion of HEPG2 cells (21.6 %, p = 0.0018) and colony formation of those invaded cells (57.4 %, p &lt; 0.0001). Rutin treatment also significantly increased early/late-stage apoptosis in HEPG2 cells (28.9 %, p &lt; 0.001). Treatment by rutin significantly inhibited protein expressions of cytochrome P450-dependent CYP3A4 (75.3 %, p &lt; 0.0001), elevated CYP1A1 enzymes (1.7-fold, p = 0.0084) and increased protein expressions of antioxidant and phase II reaction catalyzing enzymes, NQO1 (2.42-fold, p &lt; 0.0001) and GSTP1 (2.03-fold, p &lt; 0.0001). Besides, rutin treatment significantly inhibited mRNA expression of CYP3A4 (73.2 %, p=0.0014). Also, CYP1A1, NQO1 and GSTP1 mRNA expressions were significantly increased 2.77-fold (p = 0.029), 4.85- fold (p = 0.0051) and 9.84-fold (p &lt; 0.0001), respectively.</abstract>

Expression of a drug and xenobiotic metabolizing enzymes, cytochrome P450s (CYPs), and antioxidant enzymes can be modulated by various factors. The flavonoid rutin was investigated for its anti-carcinogen and protective effects as well as modulatory action on CYPs and phase II enzymes in human hepatocellular carcinoma cells. Rutin inhibited proliferation of HEPG2 cells in a dose-dependent manner with the IC50 value of 52.7 μmol L-1 and invasion of HEPG2 cells (21.6 %, p = 0.0018) and colony formation of those invaded cells (57.4 %, p < 0.0001). Rutin treatment also significantly increased early/late-stage apoptosis in HEPG2 cells (28.9 %, p < 0.001). Treatment by rutin significantly inhibited protein expressions of cytochrome P450-dependent CYP3A4 (75.3 %, p < 0.0001), elevated CYP1A1 enzymes (1.7-fold, p = 0.0084) and increased protein expressions of antioxidant and phase II reaction catalyzing enzymes, NQO1 (2.42-fold, p < 0.0001) and GSTP1 (2.03-fold, p < 0.0001). Besides, rutin treatment significantly inhibited mRNA expression of CYP3A4 (73.2 %, p=0.0014). Also, CYP1A1, NQO1 and GSTP1 mRNA expressions were significantly increased 2.77-fold (p = 0.029), 4.85- fold (p = 0.0051) and 9.84-fold (p < 0.0001), respectively.

Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells

Department of Biochemistry, Faculty of Science, Selcuk University, Konya,

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Expression of a drug and xenobiotic metabolizing enzymes, cytochrome P450s (CYPs), and antioxidant enzymes can be modulated by various factors. The flavonoid...

Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells

Published Online: Oct 15, 2016

Page range: 491 - 502

Accepted: Jul 27, 2016

DOI: https://doi.org/10.1515/acph-2016-0046

Keywords
rutin, cytochrome P450s, phase II enzymes, cell proliferation, HEPG2

© by Sedar Karakurt

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells

Published Online: Oct 15, 2016

Page range: 491 - 502

Accepted: Jul 27, 2016

DOI: https://doi.org/10.1515/acph-2016-0046

Keywordsrutin, cytochrome P450s, phase II enzymes, cell proliferation, HEPG2

© by Sedar Karakurt

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Keywords
rutin, cytochrome P450s, phase II enzymes, cell proliferation, HEPG2