Effect of Oregon grape root extracts on P-glycoprotein mediated transport in in vitro cell lines
Purpose: This study aims to investigate the potential of Oregon grape root extracts to modulate the activity of P-glycoprotein.Methods: We performed 3H-CsA or 3H-digoxin transport experiments in the absence or presence of two sources of Oregon grape root extracts (E1 and E2), berberine or berbamine...
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2024-01-01
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| Series: | Journal of Pharmacy & Pharmaceutical Sciences |
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| Online Access: | https://www.frontierspartnerships.org/articles/10.3389/jpps.2023.11927/full |
| _version_ | 1797222368979976192 |
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| author | Ying Fan Zhu Zhou Lei Zhang |
| author_facet | Ying Fan Zhu Zhou Lei Zhang |
| author_sort | Ying Fan |
| collection | DOAJ |
| description | Purpose: This study aims to investigate the potential of Oregon grape root extracts to modulate the activity of P-glycoprotein.Methods: We performed 3H-CsA or 3H-digoxin transport experiments in the absence or presence of two sources of Oregon grape root extracts (E1 and E2), berberine or berbamine in Caco-2 and MDCKII-MDR1 cells. In addition, real time quantitative polymerase chain reaction (RT-PCR) was performed in Caco-2 and LS-180 cells to investigate the mechanism of modulating P-glycoprotein.Results: Our results showed that in Caco-2 cells, Oregon grape root extracts (E1 and E2) (0.1–1 mg/mL) inhibited the efflux of CsA and digoxin in a dose-dependent manner. However, 0.05 mg/mL E1 significantly increased the absorption of digoxin. Ten µM berberine and 30 µM berbamine significantly reduced the efflux of CsA, while no measurable effect of berberine was observed with digoxin. In the MDCKII-MDR1 cells, 10 µM berberine and 30 µM berbamine inhibited the efflux of CsA and digoxin. Lastly, in real time RT-PCR study, Oregon grape root extract (0.1 mg/mL) up-regulated mRNA levels of human MDR1 in Caco-2 and LS-180 cells at 24 h.Conclusion: Our study showed that Oregon grape root extracts modulated P-glycoprotein, thereby may affect the bioavailability of drugs that are substrates of P-glycoprotein. |
| first_indexed | 2024-04-24T13:20:14Z |
| format | Article |
| id | doaj.art-4b63e927cd5048539e98f06d6696e0de |
| institution | Directory Open Access Journal |
| issn | 1482-1826 |
| language | English |
| last_indexed | 2024-04-24T13:20:14Z |
| publishDate | 2024-01-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Journal of Pharmacy & Pharmaceutical Sciences |
| spelling | doaj.art-4b63e927cd5048539e98f06d6696e0de2024-04-04T15:10:17ZengFrontiers Media S.A.Journal of Pharmacy & Pharmaceutical Sciences1482-18262024-01-012610.3389/jpps.2023.1192711927Effect of Oregon grape root extracts on P-glycoprotein mediated transport in in vitro cell linesYing Fan0Zhu Zhou1Lei Zhang2Division of Clinical Review, Office of Safety and Clinical Evaluation, Office of Generic Drugs, Center for Drug Evaluation and Research, U.S. Food and Drug Administration, Silver Spring, MD, United StatesYork College, The City University of New York, Jamaica, NY, United StatesOffice of Research and Standards, Office of Generic Drugs, Center for Drug Evaluation and Research, U.S. Food and Drug Administration, Silver Spring, MD, United StatesPurpose: This study aims to investigate the potential of Oregon grape root extracts to modulate the activity of P-glycoprotein.Methods: We performed 3H-CsA or 3H-digoxin transport experiments in the absence or presence of two sources of Oregon grape root extracts (E1 and E2), berberine or berbamine in Caco-2 and MDCKII-MDR1 cells. In addition, real time quantitative polymerase chain reaction (RT-PCR) was performed in Caco-2 and LS-180 cells to investigate the mechanism of modulating P-glycoprotein.Results: Our results showed that in Caco-2 cells, Oregon grape root extracts (E1 and E2) (0.1–1 mg/mL) inhibited the efflux of CsA and digoxin in a dose-dependent manner. However, 0.05 mg/mL E1 significantly increased the absorption of digoxin. Ten µM berberine and 30 µM berbamine significantly reduced the efflux of CsA, while no measurable effect of berberine was observed with digoxin. In the MDCKII-MDR1 cells, 10 µM berberine and 30 µM berbamine inhibited the efflux of CsA and digoxin. Lastly, in real time RT-PCR study, Oregon grape root extract (0.1 mg/mL) up-regulated mRNA levels of human MDR1 in Caco-2 and LS-180 cells at 24 h.Conclusion: Our study showed that Oregon grape root extracts modulated P-glycoprotein, thereby may affect the bioavailability of drugs that are substrates of P-glycoprotein.https://www.frontierspartnerships.org/articles/10.3389/jpps.2023.11927/fullOregon grape rootberberineberbamineP-glycoprotein (P-gp)cyclosporin A (CsA)digoxin |
| spellingShingle | Ying Fan Zhu Zhou Lei Zhang Effect of Oregon grape root extracts on P-glycoprotein mediated transport in in vitro cell lines Journal of Pharmacy & Pharmaceutical Sciences Oregon grape root berberine berbamine P-glycoprotein (P-gp) cyclosporin A (CsA) digoxin |
| title | Effect of Oregon grape root extracts on P-glycoprotein mediated transport in in vitro cell lines |
| title_full | Effect of Oregon grape root extracts on P-glycoprotein mediated transport in in vitro cell lines |
| title_fullStr | Effect of Oregon grape root extracts on P-glycoprotein mediated transport in in vitro cell lines |
| title_full_unstemmed | Effect of Oregon grape root extracts on P-glycoprotein mediated transport in in vitro cell lines |
| title_short | Effect of Oregon grape root extracts on P-glycoprotein mediated transport in in vitro cell lines |
| title_sort | effect of oregon grape root extracts on p glycoprotein mediated transport in in vitro cell lines |
| topic | Oregon grape root berberine berbamine P-glycoprotein (P-gp) cyclosporin A (CsA) digoxin |
| url | https://www.frontierspartnerships.org/articles/10.3389/jpps.2023.11927/full |
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