Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells
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 hepat...
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Sciendo
2016-12-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.1515/acph-2016-0046 |
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| author | Karakurt Sedar |
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| author_sort | Karakurt Sedar |
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| description | 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. |
| format | Article |
| id | doaj-art-b1a7fe5a851c44dfafe524c32c697d41 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2016-12-01 |
| publisher | Sciendo |
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| series | Acta Pharmaceutica |
| spelling | doaj-art-b1a7fe5a851c44dfafe524c32c697d412025-02-02T12:11:59ZengSciendoActa Pharmaceutica1846-95582016-12-0166449150210.1515/acph-2016-0046acph-2016-0046Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cellsKarakurt Sedar0Department of Biochemistry, Faculty of Science, Selcuk University, Konya, TurkeyExpression 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.https://doi.org/10.1515/acph-2016-0046rutincytochrome p450sphase ii enzymescell proliferationhepg2 |
| spellingShingle | Karakurt Sedar Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells Acta Pharmaceutica rutin cytochrome p450s phase ii enzymes cell proliferation hepg2 |
| title | Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells |
| title_full | Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells |
| title_fullStr | Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells |
| title_full_unstemmed | Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells |
| title_short | Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells |
| title_sort | modulatory effects of rutin on the expression of cytochrome p450s and antioxidant enzymes in human hepatoma cells |
| topic | rutin cytochrome p450s phase ii enzymes cell proliferation hepg2 |
| url | https://doi.org/10.1515/acph-2016-0046 |
| work_keys_str_mv | AT karakurtsedar modulatoryeffectsofrutinontheexpressionofcytochromep450sandantioxidantenzymesinhumanhepatomacells |